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Identification
NameImatinib
Accession NumberDB00619  (APRD01028, EXPT02967, DB03261)
TypeSmall Molecule
GroupsApproved
DescriptionImatinib is a small molecule kinase inhibitor used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally referred to as CGP57148B or STI571 (especially in older publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.
Structure
Thumb
Synonyms
4-(4-METHYL-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide
alpha-(4-Methyl-1-piperazinyl)-3'-((4-(3-pyridyl)-2-pyrimidinyl)amino)-P-toluidide
Imatinib
Imatinib Methansulfonate
Imatinibum
STI 571
External Identifiers
  • CGP-57148B
  • STI-571
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act ImatinibTablet100 mgOralActavis Pharma Company2014-04-29Not applicableCanada
Act ImatinibTablet400 mgOralActavis Pharma Company2014-04-29Not applicableCanada
GleevecTablet100 mg/1OralNovartis Pharma Produktions Gmb H2001-05-15Not applicableUs
GleevecTablet400 mg/1OralNovartis Pharmaceuticals Corporation2014-12-23Not applicableUs
GleevecTablet100 mg/1OralAvera Mc Kennan Hospital2015-03-01Not applicableUs
GleevecTablet100 mgOralNovartis Pharmaceuticals Canada Inc2005-04-05Not applicableCanada
GleevecTablet100 mg/1OralNovartis Pharmaceuticals Corporation2001-05-15Not applicableUs
GleevecCapsule100 mgOralNovartis Pharmaceuticals Canada Inc2001-09-262008-09-24Canada
GleevecTablet400 mgOralNovartis Pharmaceuticals Canada Inc2004-10-25Not applicableCanada
GleevecTablet400 mg/1OralNovartis Pharmaceuticals Corporation2001-05-15Not applicableUs
GlivecTablet, film coated100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule50 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated400 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated400 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated400 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecTablet, film coated100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
GlivecCapsule100 mgOralNovartis Europharm Ltd2001-11-07Not applicableEu
Mylan-imatinibTablet100 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Mylan-imatinibTablet400 mgOralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
PMS-imatinibTablet100 mgOralPharmascience Inc2015-05-26Not applicableCanada
PMS-imatinibTablet400 mgOralPharmascience Inc2015-05-26Not applicableCanada
Ran-imatinibTablet100 mgOralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Ran-imatinibTablet400 mgOralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Teva-imatinibTablet400 mgOralTeva Canada Limited2013-05-22Not applicableCanada
Teva-imatinibTablet100 mgOralTeva Canada Limited2013-04-02Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-imatinibTablet100 mgOralApotex Inc2013-04-19Not applicableCanada
Apo-imatinibTablet400 mgOralApotex Inc2013-04-19Not applicableCanada
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Ltd2013-07-01Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule50 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule50 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisTablet, film coated100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule400 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib ActavisCapsule100 mgOralActavis Group Ptc Ehf2013-04-17Not applicableEu
Imatinib MedacCapsule100 mgOralMedac2013-09-25Not applicableEu
Imatinib MedacCapsule400 mgOralMedac2013-09-25Not applicableEu
Imatinib MesylateTablet, film coated100 mg/1OralSun Pharma Global FZE2016-02-01Not applicableUs
Imatinib MesylateTablet, film coated400 mg/1OralAv Kare, Inc.2016-08-10Not applicableUs
Imatinib MesylateTablet, film coated400 mg/1OralSun Pharma Global FZE2016-02-01Not applicableUs
Imatinib MesylateTablet, film coated100 mg/1OralTeva Pharmaceuticals Usa, Inc.2016-08-04Not applicableUs
Imatinib MesylateTablet, film coated100 mg/1OralApotex Corp2016-08-05Not applicableUs
Imatinib MesylateTablet, film coated400 mg/1OralTeva Pharmaceuticals Usa, Inc.2016-08-04Not applicableUs
Imatinib MesylateTablet, film coated100 mg/1OralAmerican Health Packaging2016-02-15Not applicableUs
Imatinib MesylateTablet, film coated400 mg/1OralApotex Corp2016-08-05Not applicableUs
Imatinib MesylateTablet, film coated100 mg/1OralAv Kare, Inc.2016-08-10Not applicableUs
Imatinib MesylateTablet, film coated400 mg/1OralAmerican Health Packaging2016-02-15Not applicableUs
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated400 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaTablet, film coated100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule100 mgOralTeva B.V.2013-01-08Not applicableEu
Imatinib TevaCapsule400 mgOralTeva B.V.2013-01-08Not applicableEu
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CelonibCelon
EnlivenOrion
GlivecNovartis
ImatibGrey Inversiones
MesylonibMiracalus
MitinabGlenmark
PlivatinibPliva
ShantinibShantha
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Imatinib Mesylate
Thumb
  • InChI Key: YLMAHDNUQAMNNX-UHFFFAOYSA-N
  • Monoisotopic Mass: 589.247123333
  • Average Mass: 589.708
DBSALT000098
Categories
UNIIBKJ8M8G5HI
CAS number152459-95-5
WeightAverage: 493.6027
Monoisotopic: 493.259008649
Chemical FormulaC29H31N7O
InChI KeyKTUFNOKKBVMGRW-UHFFFAOYSA-N
InChI
InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
IUPAC Name
N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]benzamide
SMILES
CN1CCN(CC2=CC=C(C=C2)C(=O)NC2=CC(NC3=NC=CC(=N3)C3=CN=CC=C3)=C(C)C=C2)CC1
Pharmacology
IndicationFor the treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML), Ph+ acute lymphoblastic leukaemia, myelodysplastic/myeloproliferative diseases, aggressive systemic mastocytosis, hypereosinophilic syndrome and/or chronic eosinophilic leukemia (CEL), dermatofibrosarcoma protuberans, and malignant gastrointestinal stromal tumors (GIST).
Structured Indications
PharmacodynamicsImatinib is an antineoplastic agent used to treat chronic myelogenous leukemia. Imatinib is a 2-phenylaminopyrimidine derivative that functions as a specific inhibitor of a number of tyrosine kinase enzymes. In chronic myelogenous leukemia, the Philadelphia chromosome leads to a fusion protein of Abl with Bcr (breakpoint cluster region), termed Bcr-Abl. As this is now a continuously active tyrosine kinase, Imatinib is used to decrease Bcr-Abl activity.
Mechanism of actionImatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the Bcr-Abl tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML). It inhibits proliferation and induces apoptosis in Bcr-Abl positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib also inhibits the receptor tyrosine kinases for platelet derived growth factor (PDGF) and stem cell factor (SCF) - called c-kit. Imatinib was identified in the late 1990s by Dr Brian J. Druker. Its development is an excellent example of rational drug design. Soon after identification of the bcr-abl target, the search for an inhibitor began. Chemists used a high-throughput screen of chemical libraries to identify the molecule 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib.
TargetKindPharmacological actionActionsOrganismUniProt ID
BCR/ABL fusion protein isoform X9Proteinyes
inhibitor
HumanA9UF02 details
Mast/stem cell growth factor receptor KitProteinyes
antagonist
multitarget
HumanP10721 details
RET proto-oncogeneProteinyes
inhibitor
HumanO43519 details
High affinity nerve growth factor receptorProteinunknown
antagonist
HumanP04629 details
Macrophage colony-stimulating factor 1 receptorProteinunknown
antagonist
HumanP07333 details
Platelet-derived growth factor receptor alphaProteinunknown
antagonist
HumanP16234 details
Epithelial discoidin domain-containing receptor 1Proteinunknown
antagonist
HumanQ08345 details
Tyrosine-protein kinase ABL1Proteinunknown
inhibitor
HumanP00519 details
Platelet-derived growth factor receptor betaProteinunknown
antagonist
HumanP09619 details
Related Articles
AbsorptionThe pharmacokinetics in CML and GIST patients are similar. Imatinib is well absorbed with mean absolute bioavailability is 98% and maximum plasma levels achieved within 2-4 hours of dosing
Volume of distributionNot Available
Protein binding95% protein bound, mostly to albumin and alpha-1-acid glycoprotein.
Metabolism

Primarily hepatic via CYP3A4. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. This metabolite is similar in potency to the parent compound.

SubstrateEnzymesProduct
Imatinib
N-desmethylimatinib (CGP74588)Details
Imatinib
AFN911Details
Imatinib
CGP71422Details
Imatinib
CGP72383Details
Imatinib
Not Available
n-demethylated piperazineDetails
Route of eliminationImatinib elimination is predominately in the feces, mostly as metabolites. 81% of the dose is eliminated within 7 days, in feces (68% of the dose) and urine (13% of the dose). Unchanged imatinib accounted for 25% of the dose (5% urine, 20% faces), the remainder being metabolites.
Half lifeFollowing oral administration in healthy volunteers, the elimination half-lives of imatinib and its major active metabolite, the N-demethyl derivative (CGP74588) are approximately 18 and 40 hours, respectively.
Clearance
  • 8 L/h [50-year-old CML and GIST patient weighing 50 kg]
  • 14 L/h [50-year-old CML and GIST patient weighing 100 kg]
ToxicityThe most frequently reported adverse reactions (>30%) were edema, nausea, vomiting, muscle cramps, musculoskeletal pain, diarrhea, rash, fatigue and abdominal pain.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Imatinib can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Imatinib.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Imatinib.Approved
AcetaminophenAcetaminophen may increase the hepatotoxic activities of Imatinib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Imatinib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Imatinib.Approved, Vet Approved
AdinazolamThe metabolism of Adinazolam can be decreased when combined with Imatinib.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Imatinib.Approved
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Imatinib.Approved, Vet Approved
AlclometasoneThe metabolism of Alclometasone can be decreased when combined with Imatinib.Approved
AldosteroneThe serum concentration of Imatinib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Imatinib can be increased when it is combined with Alectinib.Approved
AlfentanilThe metabolism of Alfentanil can be decreased when combined with Imatinib.Approved, Illicit
AlfuzosinThe metabolism of Alfuzosin can be decreased when combined with Imatinib.Approved, Investigational
AliskirenThe metabolism of Aliskiren can be decreased when combined with Imatinib.Approved, Investigational
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Imatinib.Approved, Investigational
AllylestrenolThe metabolism of Allylestrenol can be decreased when combined with Imatinib.Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Imatinib.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Imatinib.Approved
AlosetronThe metabolism of Alosetron can be decreased when combined with Imatinib.Approved, Withdrawn
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Imatinib.Approved, Illicit, Investigational
ALT-110The risk or severity of adverse effects can be increased when Imatinib is combined with ALT-110.Investigational
AmantadineThe serum concentration of Imatinib can be increased when it is combined with Amantadine.Approved
AmbrisentanThe metabolism of Ambrisentan can be decreased when combined with Imatinib.Approved, Investigational
AmbroxolThe metabolism of Ambroxol can be decreased when combined with Imatinib.Approved
Aminohippuric acidThe serum concentration of Imatinib can be increased when it is combined with Aminohippuric acid.Approved
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Imatinib.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Imatinib.Approved
AmiodaroneThe serum concentration of Imatinib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Imatinib.Approved
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Imatinib.Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Imatinib.Approved
AmsacrineThe serum concentration of Imatinib can be increased when it is combined with Amsacrine.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Imatinib.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Imatinib.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Imatinib.Approved
ApremilastThe metabolism of Apremilast can be decreased when combined with Imatinib.Approved, Investigational
AprepitantThe serum concentration of Imatinib can be increased when it is combined with Aprepitant.Approved, Investigational
ArgatrobanThe metabolism of Argatroban can be decreased when combined with Imatinib.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Imatinib.Approved, Investigational
ArmodafinilThe metabolism of Imatinib can be decreased when combined with Armodafinil.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Imatinib.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Imatinib.Approved
AsenapineThe metabolism of Asenapine can be decreased when combined with Imatinib.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Imatinib.Approved, Withdrawn
AtazanavirThe serum concentration of Imatinib can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Imatinib can be increased when it is combined with Atenolol.Approved
AtomoxetineThe serum concentration of Imatinib can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe metabolism of Atorvastatin can be decreased when combined with Imatinib.Approved
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Imatinib.Approved
AxitinibThe metabolism of Axitinib can be decreased when combined with Imatinib.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Imatinib.Approved
AzithromycinThe metabolism of Azithromycin can be decreased when combined with Imatinib.Approved
BanoxantroneThe metabolism of Banoxantrone can be decreased when combined with Imatinib.Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Imatinib.Investigational
BedaquilineThe metabolism of Bedaquiline can be decreased when combined with Imatinib.Approved
BenzocaineThe serum concentration of Imatinib can be increased when it is combined with Benzocaine.Approved
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Imatinib.Approved, Illicit
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Imatinib.Approved
BepridilThe serum concentration of Imatinib can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Imatinib.Approved, Vet Approved
BetaxololThe metabolism of Imatinib can be decreased when combined with Betaxolol.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Imatinib.Approved, Investigational
BexaroteneThe serum concentration of Imatinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BezafibrateThe metabolism of Bezafibrate can be decreased when combined with Imatinib.Approved
BicalutamideThe metabolism of Bicalutamide can be decreased when combined with Imatinib.Approved
BiperidenThe serum concentration of Imatinib can be increased when it is combined with Biperiden.Approved
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Imatinib.Approved
BoceprevirThe serum concentration of Imatinib can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Imatinib can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Imatinib.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Imatinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Imatinib.Approved
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Imatinib.Approved
BrinzolamideThe metabolism of Brinzolamide can be decreased when combined with Imatinib.Approved
BromazepamThe metabolism of Bromazepam can be decreased when combined with Imatinib.Approved, Illicit
BromocriptineThe metabolism of Bromocriptine can be decreased when combined with Imatinib.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Imatinib.Approved
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Imatinib.Approved
BudesonideThe metabolism of Budesonide can be decreased when combined with Imatinib.Approved
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Imatinib.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Imatinib.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Imatinib can be decreased when combined with Bupropion.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Imatinib.Approved, Investigational
BusulfanThe metabolism of Busulfan can be decreased when combined with Imatinib.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Imatinib.Approved
CabergolineThe metabolism of Cabergoline can be decreased when combined with Imatinib.Approved
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Imatinib.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Imatinib.Approved
CalcitriolThe metabolism of Calcitriol can be decreased when combined with Imatinib.Approved, Nutraceutical
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Imatinib.Experimental
CanagliflozinThe metabolism of Canagliflozin can be decreased when combined with Imatinib.Approved
CandesartanThe serum concentration of Imatinib can be increased when it is combined with Candesartan.Approved
CapecitabineThe metabolism of Imatinib can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Imatinib can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Imatinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Imatinib.Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Imatinib.Approved
CariprazineThe metabolism of Cariprazine can be decreased when combined with Imatinib.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Imatinib.Approved, Investigational
CaspofunginThe serum concentration of Imatinib can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Imatinib is combined with CDX-110.Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Imatinib.Approved, Investigational
CeliprololThe metabolism of Celiprolol can be decreased when combined with Imatinib.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Imatinib.Approved, Vet Approved
CeritinibThe serum concentration of Imatinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe metabolism of Cerivastatin can be decreased when combined with Imatinib.Withdrawn
CevimelineThe metabolism of Cevimeline can be decreased when combined with Imatinib.Approved
Chenodeoxycholic acidThe metabolism of Chenodeoxycholic acid can be decreased when combined with Imatinib.Approved
ChloramphenicolThe metabolism of Imatinib can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Imatinib.Approved, Illicit
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Imatinib.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Imatinib.Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Imatinib.Approved, Vet Approved
ChlorpropamideThe serum concentration of Imatinib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Imatinib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Imatinib.Approved
CholecalciferolThe metabolism of Cholecalciferol can be decreased when combined with Imatinib.Approved, Nutraceutical
CholesterolThe serum concentration of Imatinib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Imatinib can be decreased when it is combined with Cholic Acid.Approved
CiclesonideThe metabolism of Ciclesonide can be decreased when combined with Imatinib.Approved, Investigational
CilazaprilThe serum concentration of Imatinib can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Imatinib.Approved
CimetidineThe serum concentration of Imatinib can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Imatinib can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Imatinib can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Imatinib.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Imatinib.Approved
CitalopramThe metabolism of Citalopram can be decreased when combined with Imatinib.Approved
ClarithromycinThe serum concentration of Imatinib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Imatinib can be increased when it is combined with Clemastine.Approved
ClindamycinThe metabolism of Clindamycin can be decreased when combined with Imatinib.Approved, Vet Approved
ClobazamThe metabolism of Clobazam can be decreased when combined with Imatinib.Approved, Illicit
ClofazimineThe metabolism of Clofazimine can be decreased when combined with Imatinib.Approved, Investigational
ClofibrateThe metabolism of Clofibrate can be decreased when combined with Imatinib.Approved
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Imatinib.Investigational
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Imatinib.Approved, Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Imatinib.Approved, Vet Approved
ClonazepamThe metabolism of Clonazepam can be decreased when combined with Imatinib.Approved, Illicit
ClonidineThe metabolism of Clonidine can be decreased when combined with Imatinib.Approved
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Imatinib.Approved, Nutraceutical
ClorazepateThe metabolism of Clorazepate can be decreased when combined with Imatinib.Approved, Illicit
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Imatinib.Approved, Illicit
ClotrimazoleThe serum concentration of Imatinib can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Imatinib is combined with Clozapine.Approved
CobicistatThe serum concentration of Imatinib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Imatinib.Approved
CocaineThe metabolism of Imatinib can be decreased when combined with Cocaine.Approved, Illicit
CodeineThe metabolism of Codeine can be decreased when combined with Imatinib.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Imatinib.Approved
ColforsinThe serum concentration of Imatinib can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Imatinib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe metabolism of Conjugated Equine Estrogens can be decreased when combined with Imatinib.Approved
Cortisone acetateThe metabolism of Cortisone acetate can be decreased when combined with Imatinib.Approved
CrizotinibThe serum concentration of Imatinib can be increased when it is combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Imatinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Imatinib.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Imatinib.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Imatinib can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
CytarabineThe metabolism of Cytarabine can be decreased when combined with Imatinib.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Imatinib.Approved
DabrafenibThe serum concentration of Imatinib can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe metabolism of Daclatasvir can be decreased when combined with Imatinib.Approved
DactinomycinThe serum concentration of Imatinib can be increased when it is combined with Dactinomycin.Approved
DantroleneThe metabolism of Dantrolene can be decreased when combined with Imatinib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Imatinib.Approved
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Imatinib.Investigational
DapsoneThe metabolism of Dapsone can be decreased when combined with Imatinib.Approved, Investigational
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Imatinib.Approved, Investigational
DarunavirThe serum concentration of Imatinib can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Imatinib.Approved
DasatinibThe serum concentration of Imatinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Imatinib.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Imatinib.Approved
DeferasiroxThe serum concentration of Imatinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Imatinib can be increased when it is combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Imatinib.Approved
DesipramineThe serum concentration of Imatinib can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Imatinib.Approved
DesloratadineThe serum concentration of Imatinib can be increased when it is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe metabolism of Desvenlafaxine can be decreased when combined with Imatinib.Approved
DexamethasoneThe serum concentration of Imatinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Imatinib.Approved
DextropropoxypheneThe metabolism of Dextropropoxyphene can be decreased when combined with Imatinib.Approved, Illicit, Withdrawn
DiazepamThe metabolism of Diazepam can be decreased when combined with Imatinib.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Imatinib.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Imatinib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Imatinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Imatinib.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Imatinib.Approved, Illicit
DihydroergotamineThe serum concentration of Imatinib can be increased when it is combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Imatinib.Illicit
DiltiazemThe serum concentration of Imatinib can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Imatinib can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Imatinib can be increased when it is combined with Dipyridamole.Approved
DisopyramideThe metabolism of Disopyramide can be decreased when combined with Imatinib.Approved
DisulfiramThe metabolism of Disulfiram can be decreased when combined with Imatinib.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Imatinib.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Imatinib.Approved
DolasetronThe metabolism of Dolasetron can be decreased when combined with Imatinib.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Imatinib.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Imatinib.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Imatinib.Approved
DoxazosinThe serum concentration of Imatinib can be increased when it is combined with Doxazosin.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Imatinib.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Imatinib.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Imatinib.Approved, Investigational
DoxycyclineThe serum concentration of Imatinib can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Imatinib.Approved, Illicit
DronedaroneThe serum concentration of Imatinib can be increased when it is combined with Dronedarone.Approved
DuloxetineThe metabolism of Imatinib can be decreased when combined with Duloxetine.Approved
DutasterideThe metabolism of Dutasteride can be decreased when combined with Imatinib.Approved, Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Imatinib.Approved
EfavirenzThe serum concentration of Imatinib can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Imatinib can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Imatinib.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Imatinib.Approved
EltrombopagThe serum concentration of Imatinib can be increased when it is combined with Eltrombopag.Approved
ElvitegravirThe metabolism of Elvitegravir can be decreased when combined with Imatinib.Approved
EnalaprilThe metabolism of Enalapril can be decreased when combined with Imatinib.Approved, Vet Approved
EnzalutamideThe serum concentration of Imatinib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Imatinib.Approved, Investigational
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Imatinib.Approved
ErgocalciferolThe metabolism of Ergocalciferol can be decreased when combined with Imatinib.Approved, Nutraceutical
Ergoloid mesylateThe metabolism of Ergoloid mesylate can be decreased when combined with Imatinib.Approved
ErgonovineThe metabolism of Ergonovine can be decreased when combined with Imatinib.Approved
ErgotamineThe metabolism of Ergotamine can be decreased when combined with Imatinib.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Imatinib.Approved, Investigational
ErythromycinThe serum concentration of Imatinib can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Imatinib.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Imatinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Esomeprazole can be decreased when combined with Imatinib.Approved, Investigational
EstazolamThe metabolism of Estazolam can be decreased when combined with Imatinib.Approved, Illicit
EstradiolThe metabolism of Estradiol can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
Estradiol valerate/DienogestThe metabolism of Estradiol valerate/Dienogest can be decreased when combined with Imatinib.Approved
EstramustineThe metabolism of Estramustine can be decreased when combined with Imatinib.Approved
EstriolThe serum concentration of Imatinib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe metabolism of Estrone can be decreased when combined with Imatinib.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Imatinib.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Imatinib.Approved
EthanolThe metabolism of Ethanol can be decreased when combined with Imatinib.Approved
Ethinyl EstradiolThe metabolism of Ethinyl Estradiol can be decreased when combined with Imatinib.Approved
EthosuximideThe metabolism of Ethosuximide can be decreased when combined with Imatinib.Approved
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Imatinib.Approved, Illicit
EtonogestrelThe metabolism of Etonogestrel can be decreased when combined with Imatinib.Approved, Investigational
EtoposideThe metabolism of Etoposide can be decreased when combined with Imatinib.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Imatinib.Approved, Investigational
EtravirineThe serum concentration of Imatinib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Imatinib.Approved
ExemestaneThe metabolism of Exemestane can be decreased when combined with Imatinib.Approved, Investigational
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Imatinib.Approved
FamciclovirThe metabolism of Famciclovir can be decreased when combined with Imatinib.Approved
FelbamateThe metabolism of Felbamate can be decreased when combined with Imatinib.Approved
FelodipineThe metabolism of Felodipine can be decreased when combined with Imatinib.Approved, Investigational
FenofibrateThe metabolism of Fenofibrate can be decreased when combined with Imatinib.Approved
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Imatinib.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Imatinib.Approved
FexofenadineThe serum concentration of Imatinib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Imatinib.Approved
FinasterideThe metabolism of Finasteride can be decreased when combined with Imatinib.Approved
FingolimodImatinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Imatinib.Approved
FloxuridineThe metabolism of Imatinib can be decreased when combined with Floxuridine.Approved
FluconazoleThe serum concentration of Imatinib can be increased when it is combined with Fluconazole.Approved
FludarabineImatinib may decrease the myelosuppressive activities of Fludarabine.Approved
FlunisolideThe metabolism of Flunisolide can be decreased when combined with Imatinib.Approved, Investigational
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Imatinib.Approved, Illicit
FluorometholoneThe metabolism of Fluorometholone can be decreased when combined with Imatinib.Approved
FluorouracilThe metabolism of Imatinib can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Imatinib can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Imatinib can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Imatinib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe metabolism of Flurazepam can be decreased when combined with Imatinib.Approved, Illicit
FlutamideThe metabolism of Flutamide can be decreased when combined with Imatinib.Approved
Fluticasone furoateThe metabolism of Fluticasone furoate can be decreased when combined with Imatinib.Approved
Fluticasone PropionateThe metabolism of Fluticasone Propionate can be decreased when combined with Imatinib.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Imatinib.Approved
FluvoxamineThe serum concentration of Imatinib can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Imatinib can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Imatinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Imatinib can be decreased when it is combined with Fosphenytoin.Approved
FulvestrantThe metabolism of Fulvestrant can be decreased when combined with Imatinib.Approved, Investigational
Fusidic AcidThe serum concentration of Imatinib can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Imatinib is combined with G17DT.Investigational
GalantamineThe metabolism of Galantamine can be decreased when combined with Imatinib.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Imatinib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Imatinib.Approved
GemfibrozilThe serum concentration of the active metabolites of Imatinib can be reduced when Imatinib is used in combination with Gemfibrozil resulting in a loss in efficacy.Approved
GenisteinThe serum concentration of Imatinib can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Imatinib is combined with GI-5005.Investigational
GlipizideThe metabolism of Glipizide can be decreased when combined with Imatinib.Approved
GlyburideThe metabolism of Glyburide can be decreased when combined with Imatinib.Approved
GlycerolThe serum concentration of Imatinib can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Imatinib can be increased when it is combined with Gramicidin D.Approved
GranisetronThe metabolism of Granisetron can be decreased when combined with Imatinib.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Imatinib.Approved
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Imatinib.Withdrawn
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Imatinib.Approved, Investigational
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Imatinib.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Imatinib.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Imatinib.Approved, Vet Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Imatinib.Approved
Histamine PhosphateThe metabolism of Histamine Phosphate can be decreased when combined with Imatinib.Approved
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Imatinib.Approved, Illicit
HydrocortisoneThe metabolism of Hydrocortisone can be decreased when combined with Imatinib.Approved, Vet Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Imatinib.Approved, Illicit
Hydroxyprogesterone caproateThe metabolism of Hydroxyprogesterone caproate can be decreased when combined with Imatinib.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Imatinib.Approved
IbuprofenThe serum concentration of Imatinib can be decreased when it is combined with Ibuprofen.Approved
IdelalisibThe serum concentration of Imatinib can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Imatinib resulting in a loss in efficacy.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Imatinib.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Imatinib.Approved, Investigational
IndacaterolThe metabolism of Indacaterol can be decreased when combined with Imatinib.Approved
IndapamideThe metabolism of Indapamide can be decreased when combined with Imatinib.Approved
IndinavirThe serum concentration of Imatinib can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Imatinib can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Imatinib is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Imatinib is combined with INGN 225.Investigational
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Imatinib.Approved
IrbesartanThe metabolism of Imatinib can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe metabolism of Irinotecan can be decreased when combined with Imatinib.Approved, Investigational
IsavuconazoniumThe serum concentration of Imatinib can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Imatinib can be decreased when combined with Isoniazid.Approved
Isosorbide DinitrateThe metabolism of Isosorbide Dinitrate can be decreased when combined with Imatinib.Approved
Isosorbide MononitrateThe metabolism of Isosorbide Mononitrate can be decreased when combined with Imatinib.Approved
IsradipineThe serum concentration of Imatinib can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Imatinib can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Imatinib.Approved
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Imatinib.Approved
IvermectinThe metabolism of Ivermectin can be decreased when combined with Imatinib.Approved, Vet Approved
IxabepiloneThe metabolism of Ixabepilone can be decreased when combined with Imatinib.Approved, Investigational
IxazomibThe metabolism of Ixazomib can be decreased when combined with Imatinib.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Imatinib.Approved, Vet Approved
KetazolamThe metabolism of Ketazolam can be decreased when combined with Imatinib.Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Imatinib.Approved
KetoconazoleThe serum concentration of Imatinib can be increased when it is combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Imatinib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Imatinib.Approved, Investigational
LansoprazoleLansoprazole may increase the dermatologic adverse activities of Imatinib.Approved, Investigational
LapatinibThe metabolism of Lapatinib can be decreased when combined with Imatinib.Approved, Investigational
LaquinimodThe metabolism of Laquinimod can be decreased when combined with Imatinib.Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Imatinib.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Imatinib is combined with Leflunomide.Approved, Investigational
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Imatinib.Approved
LenvatinibThe metabolism of Lenvatinib can be decreased when combined with Imatinib.Approved
LercanidipineThe metabolism of Lercanidipine can be decreased when combined with Imatinib.Approved, Investigational
LetrozoleThe metabolism of Letrozole can be decreased when combined with Imatinib.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Imatinib.Approved, Investigational
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Imatinib.Approved
LevocetirizineThe metabolism of Levocetirizine can be decreased when combined with Imatinib.Approved
LevofloxacinThe serum concentration of Imatinib can be increased when it is combined with Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe metabolism of Levomethadyl Acetate can be decreased when combined with Imatinib.Approved
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Imatinib.Approved
LevonorgestrelThe metabolism of Levonorgestrel can be decreased when combined with Imatinib.Approved, Investigational
LevothyroxineThe metabolism of Levothyroxine can be decreased when combined with Imatinib.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Imatinib.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Imatinib.Approved
LiothyronineThe serum concentration of Imatinib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Imatinib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Imatinib can be increased when it is combined with Lisinopril.Approved, Investigational
LisurideThe metabolism of Lisuride can be decreased when combined with Imatinib.Approved
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Imatinib.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Imatinib.Approved
LopinavirThe serum concentration of Imatinib can be increased when it is combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Imatinib.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Imatinib.Approved
LosartanThe metabolism of Losartan can be decreased when combined with Imatinib.Approved
LovastatinThe serum concentration of Imatinib can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Imatinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Imatinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Lumefantrine can be decreased when combined with Imatinib.Approved
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Imatinib.Approved
MacitentanThe metabolism of Macitentan can be decreased when combined with Imatinib.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Imatinib.Approved, Investigational
MaprotilineThe serum concentration of Imatinib can be increased when it is combined with Maprotiline.Approved
MaravirocThe metabolism of Maraviroc can be decreased when combined with Imatinib.Approved, Investigational
MebendazoleThe metabolism of Mebendazole can be decreased when combined with Imatinib.Approved, Vet Approved
Medroxyprogesterone acetateThe metabolism of Medroxyprogesterone acetate can be decreased when combined with Imatinib.Approved, Investigational
MefloquineThe metabolism of Mefloquine can be decreased when combined with Imatinib.Approved
Megestrol acetateThe serum concentration of Imatinib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Imatinib.Approved, Vet Approved
MeprobamateThe serum concentration of Imatinib can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Imatinib.Withdrawn
MethadoneThe metabolism of Methadone can be decreased when combined with Imatinib.Approved
MethaqualoneThe metabolism of Methaqualone can be decreased when combined with Imatinib.Illicit, Withdrawn
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Imatinib.Approved
MethotrimeprazineThe metabolism of Imatinib can be decreased when combined with Methotrimeprazine.Approved
MethoxsalenThe metabolism of Methoxsalen can be decreased when combined with Imatinib.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Imatinib.Approved, Vet Approved
MethylprednisoloneThe metabolism of Methylprednisolone can be decreased when combined with Imatinib.Approved, Vet Approved
MethyltestosteroneThe metabolism of Methyltestosterone can be decreased when combined with Imatinib.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Imatinib.Approved, Investigational
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Imatinib.Approved
MexiletineThe metabolism of Imatinib can be decreased when combined with Mexiletine.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Imatinib.Approved
MibefradilThe metabolism of Mibefradil can be decreased when combined with Imatinib.Withdrawn
MiconazoleThe metabolism of Miconazole can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
MidazolamThe metabolism of Midazolam can be decreased when combined with Imatinib.Approved, Illicit
MifepristoneThe serum concentration of Imatinib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Mirabegron can be decreased when combined with Imatinib.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Imatinib.Approved
MitomycinThe serum concentration of Imatinib can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Imatinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Imatinib can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Imatinib can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Imatinib can be decreased when it is combined with Modafinil.Approved, Investigational
MontelukastThe metabolism of Montelukast can be decreased when combined with Imatinib.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Imatinib.Approved, Investigational
Mycophenolate mofetilThe metabolism of Mycophenolate mofetil can be decreased when combined with Imatinib.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Imatinib.Approved
NafcillinThe serum concentration of Imatinib can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Imatinib.Approved
NaloxoneThe metabolism of Naloxone can be decreased when combined with Imatinib.Approved, Vet Approved
NaltrexoneThe serum concentration of Imatinib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Imatinib can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Imatinib is combined with Natalizumab.Approved, Investigational
NateglinideThe metabolism of Nateglinide can be decreased when combined with Imatinib.Approved, Investigational
NefazodoneThe serum concentration of Imatinib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Imatinib can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Imatinib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Imatinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Imatinib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe metabolism of Imatinib can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Imatinib.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Imatinib.Approved
NilotinibThe serum concentration of Imatinib can be increased when it is combined with Nilotinib.Approved, Investigational
NilvadipineThe metabolism of Nilvadipine can be decreased when combined with Imatinib.Approved
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Imatinib.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Imatinib.Approved
NisoldipineThe metabolism of Nisoldipine can be decreased when combined with Imatinib.Approved
NitrazepamThe metabolism of Nitrazepam can be decreased when combined with Imatinib.Approved
NitrendipineThe metabolism of Nitrendipine can be decreased when combined with Imatinib.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Imatinib.Approved
NorethisteroneThe metabolism of Norethisterone can be decreased when combined with Imatinib.Approved
NorgestrelThe metabolism of Norgestrel can be decreased when combined with Imatinib.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Imatinib.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Imatinib.Approved, Investigational
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Imatinib.Approved
OlopatadineThe metabolism of Olopatadine can be decreased when combined with Imatinib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Imatinib.Approved
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Imatinib.Approved
OrphenadrineThe metabolism of Orphenadrine can be decreased when combined with Imatinib.Approved
OsimertinibThe serum concentration of Imatinib can be increased when it is combined with Osimertinib.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Imatinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Imatinib.Approved
OxazepamThe metabolism of Oxazepam can be decreased when combined with Imatinib.Approved
OxybutyninThe metabolism of Oxybutynin can be decreased when combined with Imatinib.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Imatinib is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
P-NitrophenolThe serum concentration of Imatinib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Imatinib.Approved, Vet Approved
PalbociclibThe serum concentration of Imatinib can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Imatinib can be increased when it is combined with Palmitic Acid.Experimental
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Imatinib.Approved, Investigational
PanobinostatThe serum concentration of Imatinib can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Imatinib.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Imatinib.Approved
ParamethasoneThe metabolism of Paramethasone can be decreased when combined with Imatinib.Approved
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Imatinib.Approved
ParicalcitolThe metabolism of Paricalcitol can be decreased when combined with Imatinib.Approved, Investigational
ParitaprevirThe metabolism of Paritaprevir can be decreased when combined with Imatinib.Approved
ParoxetineThe metabolism of Imatinib can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Imatinib.Approved
Peginterferon alfa-2bThe serum concentration of Imatinib can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Imatinib.Approved
PentobarbitalThe serum concentration of Imatinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerampanelThe metabolism of Perampanel can be decreased when combined with Imatinib.Approved
PergolideThe metabolism of Pergolide can be decreased when combined with Imatinib.Approved, Vet Approved, Withdrawn
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Imatinib.Approved
PerindoprilThe serum concentration of Imatinib can be increased when it is combined with Perindopril.Approved
PermethrinThe metabolism of Permethrin can be decreased when combined with Imatinib.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Imatinib.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Imatinib.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Imatinib.Withdrawn
PhenobarbitalThe serum concentration of Imatinib can be decreased when it is combined with Phenobarbital.Approved
PhenoxybenzamineThe metabolism of Phenoxybenzamine can be decreased when combined with Imatinib.Approved
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Imatinib.Approved
PhenytoinThe serum concentration of Imatinib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PilocarpineThe metabolism of Pilocarpine can be decreased when combined with Imatinib.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Imatinib.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Imatinib.Approved
PinacidilThe metabolism of Pinacidil can be decreased when combined with Imatinib.Withdrawn
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Imatinib.Approved, Investigational
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Imatinib.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Imatinib.Approved
Platelet Activating FactorThe serum concentration of Imatinib can be decreased when it is combined with Platelet Activating Factor.Experimental
PodofiloxThe metabolism of Podofilox can be decreased when combined with Imatinib.Approved
PomalidomideThe metabolism of Pomalidomide can be decreased when combined with Imatinib.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Imatinib.Approved
PosaconazoleThe serum concentration of Imatinib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrasteroneThe metabolism of Prasterone can be decreased when combined with Imatinib.Approved, Nutraceutical
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Imatinib.Approved
PravastatinThe metabolism of Pravastatin can be decreased when combined with Imatinib.Approved
PrazepamThe metabolism of Prazepam can be decreased when combined with Imatinib.Approved, Illicit
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Imatinib.Approved, Vet Approved
PrazosinThe serum concentration of Imatinib can be increased when it is combined with Prazosin.Approved
PrednisoloneThe metabolism of Prednisolone can be decreased when combined with Imatinib.Approved, Vet Approved
PrednisoneThe metabolism of Prednisone can be decreased when combined with Imatinib.Approved, Vet Approved
PrimaquineThe metabolism of Primaquine can be decreased when combined with Imatinib.Approved
PrimidoneThe serum concentration of Imatinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Imatinib can be increased when it is combined with Probenecid.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Imatinib.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Imatinib.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Imatinib.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Imatinib.Approved, Vet Approved
PromethazineThe serum concentration of Imatinib can be increased when it is combined with Promethazine.Approved
PropacetamolPropacetamol may increase the hepatotoxic activities of Imatinib.Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Imatinib.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Imatinib.Approved, Investigational
ProtriptylineThe serum concentration of Imatinib can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Imatinib.Approved
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Imatinib.Approved
PyrimethamineThe metabolism of Imatinib can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamThe metabolism of Quazepam can be decreased when combined with Imatinib.Approved, Illicit
QuercetinThe serum concentration of Imatinib can be increased when it is combined with Quercetin.Experimental
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Imatinib.Approved
QuinacrineThe metabolism of Quinacrine can be decreased when combined with Imatinib.Approved
QuinidineThe metabolism of Imatinib can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Imatinib.Approved
RabeprazoleThe metabolism of Rabeprazole can be decreased when combined with Imatinib.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Imatinib is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Imatinib.Approved
RaloxifeneThe metabolism of Raloxifene can be decreased when combined with Imatinib.Approved, Investigational
RamelteonThe metabolism of Ramelteon can be decreased when combined with Imatinib.Approved, Investigational
RanitidineThe serum concentration of Imatinib can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Imatinib.Approved, Investigational
ReboxetineThe metabolism of Reboxetine can be decreased when combined with Imatinib.Approved, Investigational
RegorafenibThe metabolism of Regorafenib can be decreased when combined with Imatinib.Approved
RepaglinideThe metabolism of Repaglinide can be decreased when combined with Imatinib.Approved, Investigational
ReserpineThe serum concentration of Imatinib can be decreased when it is combined with Reserpine.Approved
RetapamulinThe metabolism of Retapamulin can be decreased when combined with Imatinib.Approved
RifabutinThe serum concentration of Imatinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Imatinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Imatinib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Imatinib.Approved, Investigational
RilpivirineThe metabolism of Rilpivirine can be decreased when combined with Imatinib.Approved
RimonabantThe metabolism of Rimonabant can be decreased when combined with Imatinib.Approved, Investigational
RiociguatThe metabolism of Riociguat can be decreased when combined with Imatinib.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Imatinib.Approved, Investigational
RitonavirThe serum concentration of Imatinib can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe metabolism of Rivaroxaban can be decreased when combined with Imatinib.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Imatinib.Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Imatinib.Approved
RolapitantThe serum concentration of Imatinib can be increased when it is combined with Rolapitant.Approved
RomidepsinThe metabolism of Romidepsin can be decreased when combined with Imatinib.Approved, Investigational
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Imatinib.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Imatinib.Approved
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Imatinib.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Imatinib.Approved
RoxithromycinThe metabolism of Roxithromycin can be decreased when combined with Imatinib.Approved, Withdrawn
RuxolitinibThe metabolism of Ruxolitinib can be decreased when combined with Imatinib.Approved
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Imatinib.Approved, Vet Approved
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Imatinib.Approved
SaquinavirThe serum concentration of Imatinib can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Imatinib.Approved
ScopolamineThe serum concentration of Imatinib can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Imatinib can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Imatinib.Approved, Investigational, Vet Approved
SelexipagThe metabolism of Selexipag can be decreased when combined with Imatinib.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Imatinib.Approved, Investigational
SertindoleThe metabolism of Sertindole can be decreased when combined with Imatinib.Approved, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Imatinib.Approved
SevofluraneThe metabolism of Sevoflurane can be decreased when combined with Imatinib.Approved, Vet Approved
SibutramineThe metabolism of Sibutramine can be decreased when combined with Imatinib.Approved, Illicit, Investigational, Withdrawn
SildenafilThe serum concentration of Imatinib can be increased when it is combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Imatinib.Approved
SiltuximabThe serum concentration of Imatinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Imatinib.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Imatinib.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Imatinib.Approved
SirolimusThe metabolism of Sirolimus can be decreased when combined with Imatinib.Approved, Investigational
SitagliptinThe metabolism of Sitagliptin can be decreased when combined with Imatinib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Imatinib.Approved
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Imatinib.Approved
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Imatinib.Approved, Investigational
SorafenibThe metabolism of Sorafenib can be decreased when combined with Imatinib.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Imatinib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Imatinib.Experimental
SpiramycinThe metabolism of Spiramycin can be decreased when combined with Imatinib.Approved
SpironolactoneThe serum concentration of Imatinib can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Imatinib is combined with SRP 299.Investigational
St. John's WortThe metabolism of Imatinib can be increased when combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Imatinib can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Imatinib can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Imatinib can be decreased when it is combined with Streptozocin.Approved
SufentanilThe metabolism of Sufentanil can be decreased when combined with Imatinib.Approved, Investigational
SulfadiazineThe metabolism of Imatinib can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Imatinib.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Imatinib.Approved
SulfisoxazoleThe serum concentration of Imatinib can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Imatinib is combined with Sulpiride.Approved
SumatriptanThe serum concentration of Imatinib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe metabolism of Sunitinib can be decreased when combined with Imatinib.Approved, Investigational
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Imatinib.Approved
Synthetic Conjugated Estrogens, AThe metabolism of Synthetic Conjugated Estrogens, A can be decreased when combined with Imatinib.Approved
Synthetic Conjugated Estrogens, BThe metabolism of Synthetic Conjugated Estrogens, B can be decreased when combined with Imatinib.Approved
TacrineThe serum concentration of Imatinib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Imatinib.Approved, Investigational
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Imatinib.Approved, Investigational
TadalafilThe metabolism of Tadalafil can be decreased when combined with Imatinib.Approved, Investigational
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Imatinib.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Imatinib.Approved, Investigational
TasosartanThe metabolism of Tasosartan can be decreased when combined with Imatinib.Approved
Taurochenodeoxycholic acidThe metabolism of Taurochenodeoxycholic acid can be decreased when combined with Imatinib.Experimental
Taurocholic AcidThe serum concentration of Imatinib can be increased when it is combined with Taurocholic Acid.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Imatinib.Approved
TelaprevirThe serum concentration of Imatinib can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Imatinib can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Imatinib can be increased when it is combined with Telmisartan.Approved, Investigational
TemazepamThe metabolism of Temazepam can be decreased when combined with Imatinib.Approved
TemsirolimusThe metabolism of Temsirolimus can be decreased when combined with Imatinib.Approved
TeniposideThe metabolism of Teniposide can be decreased when combined with Imatinib.Approved
TenofovirThe metabolism of Imatinib can be decreased when combined with Tenofovir.Approved, Investigational
TerazosinThe serum concentration of Imatinib can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Imatinib can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Imatinib.Withdrawn
TeriflunomideThe serum concentration of Imatinib can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Imatinib.Investigational
TestosteroneThe metabolism of Testosterone can be decreased when combined with Imatinib.Approved, Investigational
TetracyclineThe metabolism of Tetracycline can be decreased when combined with Imatinib.Approved, Vet Approved
TG4010The risk or severity of adverse effects can be increased when Imatinib is combined with TG4010.Investigational
TheophyllineThe metabolism of Theophylline can be decreased when combined with Imatinib.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Imatinib.Approved
ThiotepaThe metabolism of Thiotepa can be decreased when combined with Imatinib.Approved
TiagabineThe metabolism of Tiagabine can be decreased when combined with Imatinib.Approved
TicagrelorThe metabolism of Ticagrelor can be decreased when combined with Imatinib.Approved
TiclopidineThe serum concentration of Imatinib can be increased when it is combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Imatinib.Approved
TinidazoleThe metabolism of Tinidazole can be decreased when combined with Imatinib.Approved, Investigational
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Imatinib.Approved
TipranavirThe metabolism of Imatinib can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Imatinib can be decreased when it is combined with Tocilizumab.Approved
TofacitinibImatinib may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolbutamideThe metabolism of Imatinib can be decreased when combined with Tolbutamide.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Imatinib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Imatinib.Approved
TopiramateThe metabolism of Imatinib can be decreased when combined with Topiramate.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Imatinib.Approved, Investigational
ToremifeneThe metabolism of Toremifene can be decreased when combined with Imatinib.Approved, Investigational
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Imatinib.Approved, Investigational
TramadolThe metabolism of Tramadol can be decreased when combined with Imatinib.Approved, Investigational
TranylcypromineThe metabolism of Imatinib can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Imatinib.Approved, Investigational
Trastuzumab emtansineThe metabolism of Trastuzumab emtansine can be decreased when combined with Imatinib.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Imatinib.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Imatinib.Approved, Investigational, Nutraceutical
TriamcinoloneThe metabolism of Triamcinolone can be decreased when combined with Imatinib.Approved, Vet Approved
TriazolamThe metabolism of Triazolam can be decreased when combined with Imatinib.Approved
TrifluoperazineThe serum concentration of Imatinib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Imatinib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Imatinib.Approved
TrimethoprimThe metabolism of Trimethoprim can be decreased when combined with Imatinib.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Imatinib.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Imatinib.Withdrawn
TroleandomycinThe metabolism of Troleandomycin can be decreased when combined with Imatinib.Approved
UdenafilThe metabolism of Udenafil can be decreased when combined with Imatinib.Approved, Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Imatinib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Imatinib.Approved
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Imatinib.Investigational, Withdrawn
Valproic AcidThe metabolism of Imatinib can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Imatinib can be decreased when combined with Valsartan.Approved, Investigational
VandetanibThe metabolism of Vandetanib can be decreased when combined with Imatinib.Approved
VanoxerineThe metabolism of Vanoxerine can be decreased when combined with Imatinib.Investigational
VardenafilThe metabolism of Vardenafil can be decreased when combined with Imatinib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Imatinib.Approved
VemurafenibThe serum concentration of Imatinib can be increased when it is combined with Vemurafenib.Approved
VenetoclaxThe metabolism of Venetoclax can be decreased when combined with Imatinib.Approved
VenlafaxineThe serum concentration of Imatinib can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Imatinib can be increased when it is combined with Verapamil.Approved
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Imatinib.Investigational
VilanterolThe metabolism of Vilanterol can be decreased when combined with Imatinib.Approved
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Imatinib.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Imatinib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Imatinib.Approved, Investigational
VincristineThe metabolism of Vincristine can be decreased when combined with Imatinib.Approved, Investigational
VindesineThe serum concentration of Vindesine can be increased when it is combined with Imatinib.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Imatinib.Approved, Investigational
VismodegibThe metabolism of Vismodegib can be decreased when combined with Imatinib.Approved
VoriconazoleThe serum concentration of Imatinib can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Imatinib.Approved
WarfarinImatinib may increase the anticoagulant activities of Warfarin.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Imatinib.Approved, Vet Approved
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Imatinib.Approved, Investigational
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Imatinib.Approved
ZaleplonThe metabolism of Zaleplon can be decreased when combined with Imatinib.Approved, Illicit, Investigational
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Imatinib.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Imatinib.Approved, Investigational, Withdrawn
ZimelidineThe serum concentration of Imatinib can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe serum concentration of Imatinib can be increased when it is combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Imatinib.Approved
ZomepiracThe metabolism of Zomepirac can be decreased when combined with Imatinib.Withdrawn
ZonisamideThe metabolism of Zonisamide can be decreased when combined with Imatinib.Approved, Investigational
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Imatinib.Approved
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Imatinib.Approved, Investigational
Food Interactions
  • Take with food to reduce the incidence of gastric irritation. Follow with a large glass of water. A lipid rich meal will slightly reduce and delay absorption. Avoid grapefruit and grapefruit juice throughout treatment, grapefruit can significantly increase serum levels of this product.
References
Synthesis Reference

DrugSyn.org

US5521184
General References
  1. Deininger MW, Druker BJ: Specific targeted therapy of chronic myelogenous leukemia with imatinib. Pharmacol Rev. 2003 Sep;55(3):401-23. Epub 2003 Jul 17. [PubMed:12869662 ]
  2. Vigneri P, Wang JY: Induction of apoptosis in chronic myelogenous leukemia cells through nuclear entrapment of BCR-ABL tyrosine kinase. Nat Med. 2001 Feb;7(2):228-34. [PubMed:11175855 ]
  3. Droogendijk HJ, Kluin-Nelemans HJ, van Doormaal JJ, Oranje AP, van de Loosdrecht AA, van Daele PL: Imatinib mesylate in the treatment of systemic mastocytosis: a phase II trial. Cancer. 2006 Jul 15;107(2):345-51. [PubMed:16779792 ]
  4. Lassila M, Allen TJ, Cao Z, Thallas V, Jandeleit-Dahm KA, Candido R, Cooper ME: Imatinib attenuates diabetes-associated atherosclerosis. Arterioscler Thromb Vasc Biol. 2004 May;24(5):935-42. Epub 2004 Feb 26. [PubMed:14988091 ]
  5. Reeves PM, Bommarius B, Lebeis S, McNulty S, Christensen J, Swimm A, Chahroudi A, Chavan R, Feinberg MB, Veach D, Bornmann W, Sherman M, Kalman D: Disabling poxvirus pathogenesis by inhibition of Abl-family tyrosine kinases. Nat Med. 2005 Jul;11(7):731-9. Epub 2005 Jun 26. [PubMed:15980865 ]
External Links
ATC CodesL01XE01
AHFS Codes
  • 10:00.00
  • 92:00.00
PDB Entries
FDA labelDownload (129 KB)
MSDSDownload (217 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9865
Blood Brain Barrier+0.7624
Caco-2 permeable+0.5076
P-glycoprotein substrateSubstrate0.7863
P-glycoprotein inhibitor IInhibitor0.8107
P-glycoprotein inhibitor IINon-inhibitor0.5326
Renal organic cation transporterInhibitor0.5299
CYP450 2C9 substrateNon-substrate0.8287
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6547
CYP450 1A2 substrateNon-inhibitor0.6602
CYP450 2C9 inhibitorNon-inhibitor0.8813
CYP450 2D6 inhibitorNon-inhibitor0.7933
CYP450 2C19 inhibitorNon-inhibitor0.8516
CYP450 3A4 inhibitorNon-inhibitor0.9313
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7962
Ames testNon AMES toxic0.8134
CarcinogenicityNon-carcinogens0.919
BiodegradationNot ready biodegradable0.9819
Rat acute toxicity2.6013 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7709
hERG inhibition (predictor II)Inhibitor0.8887
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
CapsuleOral100 mg
TabletOral100 mg/1
TabletOral100 mg
TabletOral400 mg/1
TabletOral400 mg
Tablet, film coatedOral100 mg
Tablet, film coatedOral400 mg
CapsuleOral400 mg
CapsuleOral50 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral400 mg/1
Prices
Unit descriptionCostUnit
Gleevec 400 mg tablet174.38USD tablet
Gleevec 100 mg tablet41.69USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2093203 No2002-11-262013-04-01Canada
US5521184 Yes1995-07-042015-07-04Us
US6894051 Yes1999-11-232019-11-23Us
US6958335 Yes2002-06-192022-06-19Us
US7544799 Yes1999-01-162019-01-16Us
USRE43932 Yes1999-01-162019-01-16Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point226 °C (mesylate salt)Not Available
water solubilityVery soluble in water at pH < 5.5 (mesylate salt)Not Available
logP3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0146 mg/mLALOGPS
logP3.47ALOGPS
logP4.38ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)12.45ChemAxon
pKa (Strongest Basic)8.27ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area86.28 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity148.93 m3·mol-1ChemAxon
Polarizability55.54 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-phenylbenzamides. These are benzamides that are N-linked to a phenyl group via the carboxamide group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzamides
Direct ParentN-phenylbenzamides
Alternative Parents
Substituents
  • N-phenylbenzamide
  • Pyridinylpyrimidine
  • N-arylamide
  • Diaminotoluene
  • Benzoic acid or derivatives
  • Aminotoluene
  • Phenylmethylamine
  • Benzylamine
  • Benzoyl
  • Aralkylamine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Toluene
  • Pyrimidine
  • Pyridine
  • Piperazine
  • 1,4-diazinane
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Not Available
Gene Name:
BCR/ABL fusion
Uniprot ID:
A9UF02
Molecular Weight:
179321.835 Da
References
  1. Nadal E, Olavarria E: Imatinib mesylate (Gleevec/Glivec) a molecular-targeted therapy for chronic myeloid leukaemia and other malignancies. Int J Clin Pract. 2004 May;58(5):511-6. [PubMed:15206509 ]
  2. Waller CF: Imatinib mesylate. Recent Results Cancer Res. 2010;184:3-20. doi: 10.1007/978-3-642-01222-8_1. [PubMed:20072827 ]
  3. Croom KF, Perry CM: Imatinib mesylate: in the treatment of gastrointestinal stromal tumours. Drugs. 2003;63(5):513-22; discussion 523-4. [PubMed:12600228 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonistmultitarget
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1...
Gene Name:
KIT
Uniprot ID:
P10721
Molecular Weight:
109863.655 Da
References
  1. Lee JL, Kim JY, Ryu MH, Kang HJ, Chang HM, Kim TW, Lee H, Park JH, Kim HC, Kim JS, Kang YK: Response to imatinib in KIT- and PDGFRA-wild type gastrointestinal stromal associated with neurofibromatosis type 1. Dig Dis Sci. 2006 Jun;51(6):1043-6. [PubMed:16865565 ]
  2. Dy GK, Miller AA, Mandrekar SJ, Aubry MC, Langdon RM Jr, Morton RF, Schild SE, Jett JR, Adjei AA: A phase II trial of imatinib (ST1571) in patients with c-kit expressing relapsed small-cell lung cancer: a CALGB and NCCTG study. Ann Oncol. 2005 Nov;16(11):1811-6. Epub 2005 Aug 8. [PubMed:16087693 ]
  3. Rutkowski P, Nowecki ZI, Debiec-Rychter M, Grzesiakowska U, Michej W, Wozniak A, Siedlecki JA, Limon J, vel Dobosz AJ, Kakol M, Osuch C, Ruka W: Predictive factors for long-term effects of imatinib therapy in patients with inoperable/metastatic CD117(+) gastrointestinal stromal tumors (GISTs). J Cancer Res Clin Oncol. 2007 Sep;133(9):589-97. Epub 2007 Apr 26. [PubMed:17458563 ]
  4. De Giorgi U: KIT mutations and imatinib dose effects in patients with gastrointestinal stromal tumors. J Clin Oncol. 2007 Mar 20;25(9):1146-7; author reply 1147-8. [PubMed:17369583 ]
  5. Posadas EM, Kwitkowski V, Kotz HL, Espina V, Minasian L, Tchabo N, Premkumar A, Hussain MM, Chang R, Steinberg SM, Kohn EC: A prospective analysis of imatinib-induced c-KIT modulation in ovarian cancer: a phase II clinical study with proteomic profiling. Cancer. 2007 Jul 15;110(2):309-17. [PubMed:17559139 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
RET
Uniprot ID:
O43519
Molecular Weight:
2129.3 Da
References
  1. de Groot JW, Plaza Menacho I, Schepers H, Drenth-Diephuis LJ, Osinga J, Plukker JT, Links TP, Eggen BJ, Hofstra RM: Cellular effects of imatinib on medullary thyroid cancer cells harboring multiple endocrine neoplasia Type 2A and 2B associated RET mutations. Surgery. 2006 Jun;139(6):806-14. [PubMed:16782438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympathetic and nervous neurons. High affinity receptor for NGF which is its primary ligand, it can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 ...
Gene Name:
NTRK1
Uniprot ID:
P04629
Molecular Weight:
87496.465 Da
References
  1. Catani M, De Milito R, Simi M: [New orientations in the management of advanced, metastatic gastrointestinal stromal tumors (GIST): combination of surgery and systemic therapy with imatinib in a case of primary gastric location]. Chir Ital. 2005 Jan-Feb;57(1):127-33. [PubMed:15832750 ]
  2. Kovacs M, Nagy P, Pak G, Feher J: [Gastrointestinal stromal tumors (GISTs): clinical and pathological features]. Orv Hetil. 2005 Jun 26;146(26):1375-81. [PubMed:16052979 ]
  3. de Groot JW, Plaza Menacho I, Schepers H, Drenth-Diephuis LJ, Osinga J, Plukker JT, Links TP, Eggen BJ, Hofstra RM: Cellular effects of imatinib on medullary thyroid cancer cells harboring multiple endocrine neoplasia Type 2A and 2B associated RET mutations. Surgery. 2006 Jun;139(6):806-14. [PubMed:16782438 ]
  4. de Groot JW, Zonnenberg BA, van Ufford-Mannesse PQ, de Vries MM, Links TP, Lips CJ, Voest EE: A phase II trial of imatinib therapy for metastatic medullary thyroid carcinoma. J Clin Endocrinol Metab. 2007 Sep;92(9):3466-9. Epub 2007 Jun 19. [PubMed:17579194 ]
  5. Delbaldo C: [Pharmacokinetic-pharmacodynamics relationships of imatinib (Glivec)]. Therapie. 2007 Mar-Apr;62(2):87-90. Epub 2007 Jun 21. [PubMed:17582306 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor cells, especially mononuclear phagocytes, such as macrophages and monocytes. Promotes the release of proinflammatory chemokines in response to IL34 and CSF1, and thereby plays an important role in inn...
Gene Name:
CSF1R
Uniprot ID:
P07333
Molecular Weight:
107982.955 Da
References
  1. Dewar AL, Zannettino AC, Hughes TP, Lyons AB: Inhibition of c-fms by imatinib: expanding the spectrum of treatment. Cell Cycle. 2005 Jul;4(7):851-3. Epub 2005 Jul 28. [PubMed:15917650 ]
  2. Taylor JR, Brownlow N, Domin J, Dibb NJ: FMS receptor for M-CSF (CSF-1) is sensitive to the kinase inhibitor imatinib and mutation of Asp-802 to Val confers resistance. Oncogene. 2006 Jan 5;25(1):147-51. [PubMed:16170366 ]
  3. Dewar AL, Farrugia AN, Condina MR, Bik To L, Hughes TP, Vernon-Roberts B, Zannettino AC: Imatinib as a potential antiresorptive therapy for bone disease. Blood. 2006 Jun 1;107(11):4334-7. Epub 2006 Jan 31. [PubMed:16449525 ]
  4. Ando W, Hashimoto J, Nampei A, Tsuboi H, Tateishi K, Ono T, Nakamura N, Ochi T, Yoshikawa H: Imatinib mesylate inhibits osteoclastogenesis and joint destruction in rats with collagen-induced arthritis (CIA). J Bone Miner Metab. 2006;24(4):274-82. [PubMed:16816921 ]
  5. El Hajj Dib I, Gallet M, Mentaverri R, Sevenet N, Brazier M, Kamel S: Imatinib mesylate (Gleevec) enhances mature osteoclast apoptosis and suppresses osteoclast bone resorbing activity. Eur J Pharmacol. 2006 Dec 3;551(1-3):27-33. Epub 2006 Sep 16. [PubMed:17049513 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for...
Gene Name:
PDGFRA
Uniprot ID:
P16234
Molecular Weight:
122668.46 Da
References
  1. Yi ES, Strong CR, Piao Z, Perucho M, Weidner N: Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity. Appl Immunohistochem Mol Morphol. 2005 Jun;13(2):157-61. [PubMed:15894928 ]
  2. Borbenyi Z: [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]. Orv Hetil. 2005 May 1;146(18 Suppl 1):911-6. [PubMed:15921304 ]
  3. Corless CL, Schroeder A, Griffith D, Town A, McGreevey L, Harrell P, Shiraga S, Bainbridge T, Morich J, Heinrich MC: PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib. J Clin Oncol. 2005 Aug 10;23(23):5357-64. Epub 2005 May 31. [PubMed:15928335 ]
  4. Chen LL, Sabripour M, Andtbacka RH, Patel SR, Feig BW, Macapinlac HA, Choi H, Wu EF, Frazier ML, Benjamin RS: Imatinib resistance in gastrointestinal stromal tumors. Curr Oncol Rep. 2005 Jul;7(4):293-9. [PubMed:15946589 ]
  5. Tefferi A: Modern diagnosis and treatment of primary eosinophilia. Acta Haematol. 2005;114(1):52-60. [PubMed:15995325 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine kinase that functions as cell surface receptor for fibrillar collagen and regulates cell attachment to the extracellular matrix, remodeling of the extracellular matrix, cell migration, differentiation, survival and cell proliferation. Collagen binding triggers a signaling pathway that involves SRC and leads to the activation of MAP kinases. Regulates remodeling of the extracellular mat...
Gene Name:
DDR1
Uniprot ID:
Q08345
Molecular Weight:
101126.72 Da
References
  1. Gotlib J, Berube C, Growney JD, Chen CC, George TI, Williams C, Kajiguchi T, Ruan J, Lilleberg SL, Durocher JA, Lichy JH, Wang Y, Cohen PS, Arber DA, Heinrich MC, Neckers L, Galli SJ, Gilliland DG, Coutre SE: Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation. Blood. 2005 Oct 15;106(8):2865-70. Epub 2005 Jun 21. [PubMed:15972446 ]
  2. Xu L, Tong R, Cochran DM, Jain RK: Blocking platelet-derived growth factor-D/platelet-derived growth factor receptor beta signaling inhibits human renal cell carcinoma progression in an orthotopic mouse model. Cancer Res. 2005 Jul 1;65(13):5711-9. [PubMed:15994946 ]
  3. Neef M, Ledermann M, Saegesser H, Schneider V, Widmer N, Decosterd LA, Rochat B, Reichen J: Oral imatinib treatment reduces early fibrogenesis but does not prevent progression in the long term. J Hepatol. 2006 Jan;44(1):167-75. Epub 2005 Jul 12. [PubMed:16168515 ]
  4. Jubert C, Geoerger B, Grill J, Hartmann O, Vassal G: [Targeted therapies in pediatric oncology: a new therapeutic approach?]. Arch Pediatr. 2006 Feb;13(2):189-94. Epub 2005 Nov 17. [PubMed:16298518 ]
  5. Benjamin RS, Blanke CD, Blay JY, Bonvalot S, Eisenberg B: Management of gastrointestinal stromal tumors in the imatinib era: selected case studies. Oncologist. 2006 Jan;11(1):9-20. [PubMed:16401709 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Syntaxin binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 ...
Gene Name:
ABL1
Uniprot ID:
P00519
Molecular Weight:
122871.435 Da
References
  1. Hoerth E, Kodym R: Involvment of c-Abl in the radiation-induced inhibition of myoblast differentiation. Int J Radiat Biol. 2004 Oct;80(10):729-36. [PubMed:15799618 ]
  2. Dewar AL, Zannettino AC, Hughes TP, Lyons AB: Inhibition of c-fms by imatinib: expanding the spectrum of treatment. Cell Cycle. 2005 Jul;4(7):851-3. Epub 2005 Jul 28. [PubMed:15917650 ]
  3. Agirre X, Roman-Gomez J, Vazquez I, Jimenez-Velasco A, Larrayoz MJ, Lahortiga I, Andreu EJ, Marquez J, Beltran de Heredia JM, Odero MD, Prosper F, Calasanz MJ: Coexistence of different clonal populations harboring the b3a2 (p210) and e1a2 (p190) BCR-ABL1 fusion transcripts in chronic myelogenous leukemia resistant to imatinib. Cancer Genet Cytogenet. 2005 Jul 1;160(1):22-6. [PubMed:15949566 ]
  4. Brueggemeier SB, Wu D, Kron SJ, Palecek SP: Protein-acrylamide copolymer hydrogels for array-based detection of tyrosine kinase activity from cell lysates. Biomacromolecules. 2005 Sep-Oct;6(5):2765-75. [PubMed:16153117 ]
  5. Haberler C, Gelpi E, Marosi C, Rossler K, Birner P, Budka H, Hainfellner JA: Immunohistochemical analysis of platelet-derived growth factor receptor-alpha, -beta, c-kit, c-abl, and arg proteins in glioblastoma: possible implications for patient selection for imatinib mesylate therapy. J Neurooncol. 2006 Jan;76(2):105-9. [PubMed:16205964 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Vascular endothelial growth factor binding
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of peri...
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular Weight:
123966.895 Da
References
  1. Basciani S, Brama M, Mariani S, De Luca G, Arizzi M, Vesci L, Pisano C, Dolci S, Spera G, Gnessi L: Imatinib mesylate inhibits Leydig cell tumor growth: evidence for in vitro and in vivo activity. Cancer Res. 2005 Mar 1;65(5):1897-903. [PubMed:15753388 ]
  2. Jones RL, Judson IR: The development and application of imatinib. Expert Opin Drug Saf. 2005 Mar;4(2):183-91. [PubMed:15794712 ]
  3. Modi S, Seidman AD, Dickler M, Moasser M, D'Andrea G, Moynahan ME, Menell J, Panageas KS, Tan LK, Norton L, Hudis CA: A phase II trial of imatinib mesylate monotherapy in patients with metastatic breast cancer. Breast Cancer Res Treat. 2005 Mar;90(2):157-63. [PubMed:15803362 ]
  4. Johnson FM, Saigal B, Donato NJ: Induction of heparin-binding EGF-like growth factor and activation of EGF receptor in imatinib mesylate-treated squamous carcinoma cells. J Cell Physiol. 2005 Nov;205(2):218-27. [PubMed:15887238 ]
  5. Chen J, Rocken C, Nitsche B, Hosius C, Gschaidmeier H, Kahl S, Malfertheiner P, Ebert MP: The tyrosine kinase inhibitor imatinib fails to inhibit pancreatic cancer progression. Cancer Lett. 2006 Feb 28;233(2):328-37. [PubMed:15893416 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Davies A, Jordanides NE, Giannoudis A, Lucas CM, Hatziieremia S, Harris RJ, Jorgensen HG, Holyoake TL, Pirmohamed M, Clark RE, Mountford JC: Nilotinib concentration in cell lines and primary CD34(+) chronic myeloid leukemia cells is not mediated by active uptake or efflux by major drug transporters. Leukemia. 2009 Nov;23(11):1999-2006. doi: 10.1038/leu.2009.166. Epub 2009 Aug 27. [PubMed:19710702 ]
  2. Engler JR, Frede A, Saunders VA, Zannettino AC, Hughes TP, White DL: Chronic myeloid leukemia CD34+ cells have reduced uptake of imatinib due to low OCT-1 activity. Leukemia. 2010 Apr;24(4):765-70. doi: 10.1038/leu.2010.16. Epub 2010 Feb 11. [PubMed:20147974 ]
  3. Ahlin G, Karlsson J, Pedersen JM, Gustavsson L, Larsson R, Matsson P, Norinder U, Bergstrom CA, Artursson P: Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. J Med Chem. 2008 Oct 9;51(19):5932-42. doi: 10.1021/jm8003152. Epub 2008 Sep 13. [PubMed:18788725 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Davies A, Jordanides NE, Giannoudis A, Lucas CM, Hatziieremia S, Harris RJ, Jorgensen HG, Holyoake TL, Pirmohamed M, Clark RE, Mountford JC: Nilotinib concentration in cell lines and primary CD34(+) chronic myeloid leukemia cells is not mediated by active uptake or efflux by major drug transporters. Leukemia. 2009 Nov;23(11):1999-2006. doi: 10.1038/leu.2009.166. Epub 2009 Aug 27. [PubMed:19710702 ]
  2. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956 ]
  3. Hamada A, Miyano H, Watanabe H, Saito H: Interaction of imatinib mesilate with human P-glycoprotein. J Pharmacol Exp Ther. 2003 Nov;307(2):824-8. Epub 2003 Sep 15. [PubMed:12975485 ]
  4. Thomas J, Wang L, Clark RE, Pirmohamed M: Active transport of imatinib into and out of cells: implications for drug resistance. Blood. 2004 Dec 1;104(12):3739-45. Epub 2004 Aug 17. [PubMed:15315971 ]
  5. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662 ]
  6. Giannoudis A, Davies A, Lucas CM, Harris RJ, Pirmohamed M, Clark RE: Effective dasatinib uptake may occur without human organic cation transporter 1 (hOCT1): implications for the treatment of imatinib-resistant chronic myeloid leukemia. Blood. 2008 Oct 15;112(8):3348-54. doi: 10.1182/blood-2007-10-116236. Epub 2008 Jul 31. [PubMed:18669873 ]
  7. Breedveld P, Pluim D, Cipriani G, Wielinga P, van Tellingen O, Schinkel AH, Schellens JH: The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res. 2005 Apr 1;65(7):2577-82. [PubMed:15805252 ]
  8. Oka M, Fukuda M, Soda H: [Anticancer drugs and ABC transporters]. Gan To Kagaku Ryoho. 2005 May;32(5):585-92. [PubMed:15918555 ]
  9. Burger H, van Tol H, Brok M, Wiemer EA, de Bruijn EA, Guetens G, de Boeck G, Sparreboom A, Verweij J, Nooter K: Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52. Epub 2005 Jul 9. [PubMed:15970668 ]
  10. Galimberti S, Cervetti G, Guerrini F, Testi R, Pacini S, Fazzi R, Simi P, Petrini M: Quantitative molecular monitoring of BCR-ABL and MDR1 transcripts in patients with chronic myeloid leukemia during Imatinib treatment. Cancer Genet Cytogenet. 2005 Oct 1;162(1):57-62. [PubMed:16157201 ]
  11. Gardner ER, Burger H, van Schaik RH, van Oosterom AT, de Bruijn EA, Guetens G, Prenen H, de Jong FA, Baker SD, Bates SE, Figg WD, Verweij J, Sparreboom A, Nooter K: Association of enzyme and transporter genotypes with the pharmacokinetics of imatinib. Clin Pharmacol Ther. 2006 Aug;80(2):192-201. [PubMed:16890580 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Tanihara Y, Masuda S, Katsura T, Inui K: Protective effect of concomitant administration of imatinib on cisplatin-induced nephrotoxicity focusing on renal organic cation transporter OCT2. Biochem Pharmacol. 2009 Nov 1;78(9):1263-71. doi: 10.1016/j.bcp.2009.06.014. Epub 2009 Jun 18. [PubMed:19540211 ]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Houghton PJ, Germain GS, Harwood FC, Schuetz JD, Stewart CF, Buchdunger E, Traxler P: Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. Cancer Res. 2004 Apr 1;64(7):2333-7. [PubMed:15059881 ]
  2. An Y, Ongkeko WM: ABCG2: the key to chemoresistance in cancer stem cells? Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1529-42. doi: 10.1517/17425250903228834. [PubMed:19708828 ]
  3. Davies A, Jordanides NE, Giannoudis A, Lucas CM, Hatziieremia S, Harris RJ, Jorgensen HG, Holyoake TL, Pirmohamed M, Clark RE, Mountford JC: Nilotinib concentration in cell lines and primary CD34(+) chronic myeloid leukemia cells is not mediated by active uptake or efflux by major drug transporters. Leukemia. 2009 Nov;23(11):1999-2006. doi: 10.1038/leu.2009.166. Epub 2009 Aug 27. [PubMed:19710702 ]
  4. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956 ]
  5. Burger H, van Tol H, Boersma AW, Brok M, Wiemer EA, Stoter G, Nooter K: Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2. Epub 2004 Jul 13. [PubMed:15251980 ]
  6. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662 ]
  7. Breedveld P, Pluim D, Cipriani G, Wielinga P, van Tellingen O, Schinkel AH, Schellens JH: The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res. 2005 Apr 1;65(7):2577-82. [PubMed:15805252 ]
  8. Oka M, Fukuda M, Soda H: [Anticancer drugs and ABC transporters]. Gan To Kagaku Ryoho. 2005 May;32(5):585-92. [PubMed:15918555 ]
  9. Burger H, van Tol H, Brok M, Wiemer EA, de Bruijn EA, Guetens G, de Boeck G, Sparreboom A, Verweij J, Nooter K: Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52. Epub 2005 Jul 9. [PubMed:15970668 ]
  10. Yanase K, Tsukahara S, Mitsuhashi J, Sugimoto Y: Functional SNPs of the breast cancer resistance protein-therapeutic effects and inhibitor development. Cancer Lett. 2006 Mar 8;234(1):73-80. Epub 2005 Nov 21. [PubMed:16303243 ]
  11. Nakanishi T, Shiozawa K, Hassel BA, Ross DD: Complex interaction of BCRP/ABCG2 and imatinib in BCR-ABL-expressing cells: BCRP-mediated resistance to imatinib is attenuated by imatinib-induced reduction of BCRP expression. Blood. 2006 Jul 15;108(2):678-84. Epub 2006 Mar 16. [PubMed:16543472 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Plays an important role in the formation of pulmonary surfactant, probably by transporting lipids such as cholesterol.
Gene Name:
ABCA3
Uniprot ID:
Q99758
Molecular Weight:
191360.235 Da
References
  1. Chapuy B, Panse M, Radunski U, Koch R, Wenzel D, Inagaki N, Haase D, Truemper L, Wulf GG: ABC transporter A3 facilitates lysosomal sequestration of imatinib and modulates susceptibility of chronic myeloid leukemia cell lines to this drug. Haematologica. 2009 Nov;94(11):1528-36. doi: 10.3324/haematol.2009.008631. [PubMed:19880777 ]
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 03:54