Identification

Name
Imatinib
Accession Number
DB00619  (APRD01028, EXPT02967, DB03261)
Type
Small Molecule
Groups
Approved
Description

Imatinib 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
  • Imatinib
  • Imatinibum
  • α-(4-methyl-1-piperazinyl)-3'-((4-(3-pyridyl)-2-pyrimidinyl)amino)-p-toluidide
External IDs
CGP-57148B
Product Ingredients
IngredientUNIICASInChI Key
Imatinib mesylate8A1O1M485B220127-57-1YLMAHDNUQAMNNX-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GleevecTablet100 mgOralNovartis2005-04-05Not applicableCanada
GleevecTablet100 mg/1OralAvera McKennan Hospital2015-03-012018-07-05Us
GleevecCapsule100 mgOralNovartis2001-09-262008-09-24Canada
GleevecTablet400 mg/1OralNovartis Pharmaceuticals Corporation2001-05-152017-05-31Us
GleevecTablet100 mg/1OralPhysicians Total Care, Inc.2005-10-072013-06-30Us
GleevecTablet400 mgOralNovartis2004-10-25Not applicableCanada
GleevecTablet100 mg/1OralNovartis Pharmaceuticals Corporation2001-05-15Not applicableUs
GleevecTablet400 mg/1OralNovartis Pharmaceuticals Corporation2014-12-23Not applicableUs
GleevecTablet400 mg/1OralPhysicians Total Care, Inc.2005-11-092013-06-30Us
GlivecCapsule100 mgOralNovartis Europharm Limited2001-11-07Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-imatinibTablet100 mgOralApotex Corporation2013-04-19Not applicableCanada
Apo-imatinibTablet400 mgOralApotex Corporation2013-04-19Not applicableCanada
ImatinibTablet400 mg/1OralDr.Reddy's Laboratories Inc2018-08-13Not applicableUs
ImatinibTablet100 mg/1OralDr.Reddy's Laboratories Inc2018-08-13Not applicableUs
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
Imatinib AccordTablet, film coated100 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
Imatinib AccordTablet, film coated400 mgOralAccord Healthcare Limited2013-07-01Not applicableEu
International/Other Brands
Celonib (Celon) / Enliven (Orion) / Glivec (Novartis) / Imatib (Grey Inversiones) / Mesylonib (Miracalus) / Mitinab (Glenmark) / Plivatinib (Pliva) / Shantinib (Shantha)
Categories
UNII
BKJ8M8G5HI
CAS number
152459-95-5
Weight
Average: 493.6027
Monoisotopic: 493.259008649
Chemical Formula
C29H31N7O
InChI Key
KTUFNOKKBVMGRW-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

Indication

For 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).

Associated Conditions
Pharmacodynamics

Imatinib 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 action

Imatinib 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.

TargetActionsOrganism
ABCR/ABL fusion protein isoform X9
inhibitor
Human
AMast/stem cell growth factor receptor Kit
antagonist
multitarget
Human
ARET proto-oncogene
inhibitor
Human
UHigh affinity nerve growth factor receptor
antagonist
Human
UMacrophage colony-stimulating factor 1 receptor
antagonist
Human
UPlatelet-derived growth factor receptor alpha
antagonist
Human
UEpithelial discoidin domain-containing receptor 1
antagonist
Human
UTyrosine-protein kinase ABL1
inhibitor
Human
UPlatelet-derived growth factor receptor beta
antagonist
Human
Absorption

The 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 distribution
Not Available
Protein binding

95% 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.

Route of elimination

Imatinib 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 life

Following 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]
Toxicity

The 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
Pathways
PathwayCategory
Imatinib Inhibition of BCR-ABLDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Imatinib.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Imatinib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Imatinib is combined with 2-Methoxyethanol.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Imatinib.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Imatinib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Imatinib.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Imatinib.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Imatinib.
6-Deoxyerythronolide BThe metabolism of Imatinib can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe serum concentration of 6-O-benzylguanine can be increased when it is combined with Imatinib.
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
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
Human Metabolome Database
HMDB0014757
KEGG Drug
D01441
PubChem Compound
5291
PubChem Substance
46505055
ChemSpider
5101
BindingDB
13530
ChEBI
45783
ChEMBL
CHEMBL941
Therapeutic Targets Database
DNC001383
PharmGKB
PA10804
HET
STI
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Imatinib
ATC Codes
L01XE01 — Imatinib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
  • 92:00.00 — Miscellaneous Therapeutic Agents
PDB Entries
1iep / 1opj / 1t46 / 1xbb / 2hyy / 2oiq / 2pl0 / 3fw1 / 3gvu / 3hec
show 11 more
FDA label
Download (129 KB)
MSDS
Download (217 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentChronic Myeloid Leukemia (CML)1
1Active Not RecruitingTreatmentLeukemias1
1Active Not RecruitingTreatmentMalignancies, Hematologic1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers3
1CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Acute Undifferentiated Leukemia (AUL) / AIDS-related Peripheral/Systemic Lymphoma / AIDS-related Primary CNS Lymphoma / Anaplastic Large Cell Lymphoma / Angioimmunoblastic T-Cell Lymphoma / Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative / Blastic Phase Chronic Myelogenous Leukemia / Childhood Myelodysplastic Syndromes / Chronic Eosinophilic Leukemia (CEL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Myelomonocytic Leukemia / Chronic Neutrophilic Leukemia / Chronic Phase Chronic Myelogenous Leukemia / De Novo Myelodysplastic Syndromes / Essential Thrombocythemia (ET) / Extramedullary Plasmacytoma / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Gastrointestinal Stromal Tumors / Intraocular Lymphoma / Isolated Plasmacytoma of Bone / Leukemia, Prolymphocytic / Meningeal Chronic Myelogenous Leukemia / Monoclonal Gammopathy of Undetermined Significance (MGUS) / Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable / Nodal marginal zone B-cell lymphomas / Polycythemia Vera (PV) / Previously Treated Myelodysplastic Syndromes / Primary Central Nervous System Non-Hodgkin Lymphoma / Primary Myelofibrosis / Primary Systemic Amyloidosis / Progressive Hairy Cell Leukemia, Initial Treatment / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Adult Diffuse Small Cleaved Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult Immunoblastic Large Cell Lymphoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Adult T-Cell Leukemia/Lymphoma / Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Mycosis Fungoides/Sezary Syndrome / Recurrent Small Lymphocytic Lymphoma / Refractory Hairy Cell Leukemia / Refractory Multiple Myeloma / Relapsing Chronic Myelogenous Leukemia / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Secondary Myelodysplastic Syndromes / Small Intestine Lymphoma / Splenic Marginal Zone Lymphoma / Stage IV Adult Burkitt Lymphoma / Stage IV Adult Diffuse Large Cell Lymphoma / Stage IV Adult Diffuse Mixed Cell Lymphoma / Stage IV Adult Diffuse Small Cleaved Cell Lymphoma / Stage IV Adult Hodgkin Lymphoma / Stage IV Adult Immunoblastic Large Cell Lymphoma / Stage IV Adult Lymphoblastic Lymphoma / Stage IV Adult T-Cell Leukemia/Lymphoma / Stage IV Chronic Lymphocytic Leukemia / Stage IV Cutaneous T-Cell Non-Hodgkin Lymphoma / Stage IV Grade 1 Follicular Lymphoma / Stage IV Grade 2 Follicular Lymphoma / Stage IV Grade 3 Follicular Lymphoma / Stage IV Mantle Cell Lymphoma / Stage IV Marginal Zone Lymphoma / Stage IV Mycosis Fungoides/Sezary Syndrome / Stage IV Small Lymphocytic Lymphoma / T-Cell Large Granular Lymphocyte Leukemia / Unspecified Adult Solid Tumor, Protocol Specific / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Adult Acute Myeloid Leukemia / Untreated Hairy Cell Leukemia / Waldenström's Macroglobulinemia (WM)1
1CompletedTreatmentAcute Lung Injury (ALI)1
1CompletedTreatmentAdvanced Pancreatic Cancer1
1CompletedTreatmentBrain and Central Nervous System Tumors3
1CompletedTreatmentCancer, Breast1
1CompletedTreatmentChronic Myeloid Leukemia (CML)3
1CompletedTreatmentChronic Myeloid Leukemia (CML) / Gastrointestinal Stromal Tumors1
1CompletedTreatmentGastrointestinal Stromal Tumors1
1CompletedTreatmentGlioblastomas / Gliosarcoma2
1CompletedTreatmentHealthy Volunteers5
1CompletedTreatmentLeukemias6
1CompletedTreatmentLung Cancers2
1CompletedTreatmentMalignant Neoplasm of Stomach1
1CompletedTreatmentMesothelioma1
1CompletedTreatmentNeoplasms, Malignant / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentProstate Cancer2
1CompletedTreatmentRefractory Malignancy / Tumors, Solid1
1CompletedTreatmentThymic Carcinoma1
1CompletedTreatmentUnspecified Adult Solid Tumor1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific3
1CompletedTreatmentChronic Chronic myelogenous leukemia1
1Not Yet RecruitingTreatmentThyroid Papillary Carcinoma1
1RecruitingTreatmentAdvanced Cancers / Advanced Malignant Solid Neoplasm / C-KIT Tyrosine Kinase Protein Overexpression / Clinical Stage IV Cutaneous Melanoma AJCC v8 / Metastatic Gastrointestinal Stromal Tumor / Metastatic Malignant Solid Neoplasm / Metastatic Melanoma / Pathologic Stage IV Cutaneous Melanoma AJCC v8 / Unresectable Melanoma / Unresectable Solid Neoplasm1
1RecruitingTreatmentChronic Chronic myelogenous leukemia / Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia1
1TerminatedNot AvailableChronic Myeloid Leukemia (CML) / Other Glivec/Gleevec Indicated Hematological Disorders (HES, CEL, MDS/ MPN) / Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ ALL)1
1TerminatedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Blastic Phase Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Relapsing Chronic Myelogenous Leukemia1
1TerminatedTreatmentAdvanced Colorectal Cancer1
1TerminatedTreatmentGastrointestinal Stromal Tumors1
1TerminatedTreatmentMalignant Neoplasm of Pancreas1
1Unknown StatusTreatmentChordomas1
1Unknown StatusTreatmentGraft Versus Host Disease (GVHD)1
1WithdrawnTreatmentHealthy Volunteers1
1WithdrawnTreatmentPulmonary Hypertension (PH)1
1, 2Active Not RecruitingTreatmentAdult Anaplastic Oligodendroglioma / Adult Mixed Glioma / Adult Oligodendroglioma / Recurrent Adult Brain Neoplasm / Recurrent Adult Brain Tumor1
1, 2Active Not RecruitingTreatmentAdvanced Gastrointestinal Stromal Tumor (GIST)1
1, 2Active Not RecruitingTreatmentNeurofibromas / Neurofibromatosis1
1, 2CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Adult Acute Lymphoblastic Leukemia in Remission / Blastic Phase Chronic Myelogenous Leukemia / Childhood Acute Lymphoblastic Leukemia in Remission / Childhood Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Relapsing Chronic Myelogenous Leukemia / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
1, 2CompletedTreatmentAcute Myelogenous Leukaemia (AML) / Agnogenic Myeloid Metaplasia / Chronic Chronic myelogenous leukemia1
1, 2CompletedTreatmentAcute Undifferentiated Leukemia (AUL) / B-cell Adult Acute Lymphoblastic Leukemia / B-cell Childhood Acute Lymphoblastic Leukemia / L1 Adult Acute Lymphoblastic Leukemia / L1 Childhood Acute Lymphoblastic Leukemia / L2 Adult Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia / Philadelphia Chromosome Negative Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia / T-cell Adult Acute Lymphoblastic Leukemia / T-cell Childhood Acute Lymphoblastic Leukemia / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
1, 2CompletedTreatmentAdult Synovial Sarcoma / Recurrent Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
1, 2CompletedTreatmentAdvanced Melanoma / Melanoma1
1, 2CompletedTreatmentAlveolitis / Sclerosis, Progressive Systemic1
1, 2CompletedTreatmentBlastic Phase Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Relapsing Chronic Myelogenous Leukemia1
1, 2CompletedTreatmentBrain and Central Nervous System Tumors1
1, 2CompletedTreatmentCancer of the Ovary / Endometrial Cancers / Gastrointestinal Stromal Tumors / Sarcomas / Small Intestine Cancer1
1, 2CompletedTreatmentClear Cell Renal Cell Carcinoma1
1, 2CompletedTreatmentColorectal Cancers / Neoplasms, Colorectal1
1, 2CompletedTreatmentDermatofibrosarcoma1
1, 2CompletedTreatmentDesmoid Tumors1
1, 2CompletedTreatmentGastrointestinal Stromal Tumors1
1, 2CompletedTreatmentLeukemia, Myelogenous, Chronic, BCR-ABL Positive1
1, 2CompletedTreatmentLeukemias6
1, 2CompletedTreatmentPulmonary Veno Occlusive Disease1
1, 2CompletedTreatmentRecurrent Melanoma / Stage III Melanoma / Stage IV Melanoma / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentRefractory Desmoplastic Small Round Cell Tumors1
1, 2CompletedTreatmentScleroderma, Systemic1
1, 2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
1, 2CompletedTreatmentStage IV Colorectal Cancer1
1, 2CompletedTreatmentUterine Malignancies1
1, 2Not Yet RecruitingTreatmentGastrointestinal Stromal Tumors1
1, 2RecruitingTreatmentALK+ Anaplastic Large Cell Lymphoma1
1, 2RecruitingTreatmentChronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Myelogenous Leukemia, BCR-ABL1 Positive in Remission / Leukemias / Minimal Residual Disease / Philadelphia Chromosome Positive, BCR-ABL1 Positive Chronic Myelogenous Leukemia1
1, 2RecruitingTreatmentGastrointestinal Stromal Tumors (GISTs)1
1, 2RecruitingTreatmentLymphangioleiomyomatosis1
1, 2RecruitingTreatmentPlasmodium Falciparum Malaria1
1, 2RecruitingTreatmentStage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
1, 2TerminatedTreatmentBrain and Central Nervous System Tumors1
1, 2TerminatedTreatmentChronic Lymphocytic Leukaemia (CLL)1
1, 2TerminatedTreatmentChronic Myeloid Leukemia (CML)1
1, 2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2TerminatedTreatmentPhiladelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia1
1, 2TerminatedTreatmentProstate Cancer / Prostatic Neoplasms1
1, 2TerminatedTreatmentThyroid Cancers / Tumors, Solid1
1, 2Unknown StatusTreatmentLeukemias1
1, 2WithdrawnTreatmentChronic Myeloid Leukemia (CML)1
2Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
2Active Not RecruitingTreatmentAdult Acute Lymphoblastic Leukemia in Remission / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Blastic Phase / Blastic Phase Chronic Myelogenous Leukemia / Childhood Acute Lymphoblastic Leukemia in Remission / Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Chronic Phase of Disease / Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Disease / Relapsing Chronic Myelogenous Leukemia1
2Active Not RecruitingTreatmentAdvanced Chondrosarcoma / Advanced Desmoid Tumor1
2Active Not RecruitingTreatmentChronic Graft Versus Host Disease1
2Active Not RecruitingTreatmentChronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase of Disease1
2Active Not RecruitingTreatmentChronic Myeloid Leukemia (CML)1
2Active Not RecruitingTreatmentChronic Phase Chronic Myeloid Leukemia1
2Active Not RecruitingTreatmentGraft Versus Host Disease (GVHD)1
2Active Not RecruitingTreatmentLeukemias2
2Active Not RecruitingTreatmentMesothelioma, Malignant1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentTransplantation, Stem Cell / Treatments1
2CompletedNot AvailableDermatofibrosarcoma Protuberans1
2CompletedPreventionGastrointestinal Stromal Tumors1
2CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Blastic Phase Chronic Myelogenous Leukemia / Childhood Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Relapsing Chronic Myelogenous Leukemia1
2CompletedTreatmentAcral Lentiginous Malignant Melanoma / Recurrent Melanoma / Stage IIIA Melanoma / Stage IIIB Melanoma / Stage IIIc Melanoma / Stage IV Melanoma1
2CompletedTreatmentAcral/Lentiginous Melanoma / Chronically Sun Damaged Melanomas / Mucosal Melanoma1
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL)3
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Cromosome Philadelphia Positive1
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Philadelphia Chromosome1
2CompletedTreatmentAdult Acute Lymphoblastic Leukemia in Remission1
2CompletedTreatmentAdult Fibrosarcoma / Dermatofibrosarcoma Protuberans / Recurrent Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
2CompletedTreatmentAdult Grade I Meningioma / Adult Grade II Meningioma / Adult Grade III Meningioma / Adult Meningeal Hemangiopericytoma / Adult Meningioma / Recurrent Adult Brain Tumor1
2CompletedTreatmentAdvanced Gastric Cancer / Recurrent Gastric Cancer1
2CompletedTreatmentAdvanced Gastrointestinal Stromal Tumors1
2CompletedTreatmentAdvanced or Metastatic Cholangiocellular Carcinoma and Bile Duct1
2CompletedTreatmentAgnogenic Myeloid Metaplasia / Chronic Myelomonocytic Leukemia / Myeloid Metaplasia1
2CompletedTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / Cancer, Breast / Estrogen Receptor Positive / KIT Positive / One to five years postmenopausal / PDGFR Positive / Progesterone Receptor Positive / Prognostic Stage IV Breast Cancer AJCC v81
2CompletedTreatmentAntineoplastic Agents / Genital Diseases, Male / Genital Neoplasms, Male / Genitourinary tract neoplasm / Imatinib / Neoplasms / Neoplasms, Abdominal / Prostatic Diseases / Prostatic Neoplasms1
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentBlast Crisis / Chronic Myeloid Leukemia (CML) / Leukemia, Lymphocytic, Acute / Philadelphia Chromosome1
2CompletedTreatmentBrain and Central Nervous System Tumors1
2CompletedTreatmentCML / Imatinib1
2CompletedTreatmentCancer of the Ovary2
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer1
2CompletedTreatmentCancer of the Ovary / Primary Peritoneal Cancer1
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentChildhood Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia1
2CompletedTreatmentChildhood Desmoplastic Small Round Cell Tumor / Childhood Synovial Sarcoma / Gastrointestinal Stromal Tumors / Lung Cancer Metastatic / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Neuroblastoma / Recurrent Osteosarcoma1
2CompletedTreatmentChildhood Malignant Fibrous Histiocytoma of Bone / Sarcomas1
2CompletedTreatmentChordomas1
2CompletedTreatmentChronic Eosinophilic Leukemia (CEL) / Chronic Idiopathic Hypereosinophilia / Hypereosinophilic Syndromes1
2CompletedTreatmentChronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Relapsing Chronic Myelogenous Leukemia1
2CompletedTreatmentChronic Myeloid Leukemia (CML)5
2CompletedTreatmentChronic Myeloid Leukemia (CML) / Minimal Residual Disease1
2CompletedTreatmentChronic Myeloid Leukemia (CML) / Philadelphia-Positive Myeloid Leukemia1
2CompletedTreatmentChronic Myelomonocytic Leukemia / Dermatofibrosarcoma / Hypereosinophilic Syndromes / Systemic Mastocytosis1
2CompletedTreatmentChronic Myelomonocytic Leukemia / Essential Thrombocythemia (ET) / Polycythemia Vera (PV) / Primary Myelofibrosis1
2CompletedTreatmentChronic Chronic myelogenous leukemia / Chronic Myelomonocytic Leukemia1
2CompletedTreatmentDesmoid Tumors / Fibromatosis, Aggressive1
2CompletedTreatmentDiabetes Mellitus, Insulin-Dependent, 1 / Diabetes, Diabetes Mellitus Type 1 / Insulin-Dependent Diabetes Mellitus 1 / Type 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentFibromatosis1
2CompletedTreatmentGastrointestinal Stromal Tumors8
2CompletedTreatmentGastrointestinal Stromal Tumors (GISTs)2
2CompletedTreatmentGastrointestinal Stromal Tumors / Metastatic Cancers1
2CompletedTreatmentGastrointestinal Stromal Tumors / Sarcomas1
2CompletedTreatmentGlioblastomas / Gliosarcoma1
2CompletedTreatmentGraft Versus Host Disease (GVHD) / Scleroderma, Systemic1
2CompletedTreatmentHead and Neck Carcinoma1
2CompletedTreatmentHead and Neck Carcinoma / Squamous Cell Cancer1
2CompletedTreatmentHealth Care Evaluation / Health Care Quality1
2CompletedTreatmentImatinib Mesylate / Sclerotic Graft Versus Host Disease1
2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2CompletedTreatmentLeukemia, Myeloid, Chronic-Phase1
2CompletedTreatmentLeukemia, Other / Malignancies1
2CompletedTreatmentLeukemias12
2CompletedTreatmentLife Threatening Diseases1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2CompletedTreatmentLung Cancers4
2CompletedTreatmentMale Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentMalignant Pleural Effusions / Non-Small Cell Lung Cancer Recurrent / Stage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2CompletedTreatmentMelanoma / Skin Neoplasms1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer2
2CompletedTreatmentMetastatic Colon Cancer / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage IV Rectal Cancer1
2CompletedTreatmentMetastatic Melanoma1
2CompletedTreatmentMyelodysplastic Syndromes / Myeloid Leukemias1
2CompletedTreatmentMyeloid Leukemia, Chronic, Chronic-Phase1
2CompletedTreatmentNeurofibromatosis1
2CompletedTreatmentPhiladelphia Chromosome Positive Acute Lymphocytic Leukemia1
2CompletedTreatmentPhiladelphia Positive Chronic Myeloid Leukemia in Accelerated Phase, Acute Lymphoblastic Leukemia, Acute Myeloid Leukemia2
2CompletedTreatmentPhiladelphia Positive Chronic Myeloid Leukemia in Myeloid Blast Crisis1
2CompletedTreatmentPolycythemia Vera (PV)2
2CompletedTreatmentPrimary Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer1
2CompletedTreatmentPrimary Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer / Stage III Ovarian Epithelial Cancer / Stage IV Ovarian Epithelial Cancer1
2CompletedTreatmentProstate Cancer3
2CompletedTreatmentRecurrent Neuroendocrine Carcinoma of the Skin / Stage II Neuroendocrine Carcinoma of the Skin / Stage III Neuroendocrine Carcinoma of the Skin1
2CompletedTreatmentRecurrent Uterine Sarcoma / Uterine Carcinosarcoma1
2CompletedTreatmentRenal Cancers1
2CompletedTreatmentRheumatoid Arthritis1
2CompletedTreatmentSarcomas3
2CompletedTreatmentScleroderma, Localized / Scleroderma, Systemic1
2CompletedTreatmentSclerosis, Progressive Systemic1
2CompletedTreatmentSystemic Sclerosis, Scleroderma1
2CompletedTreatmentT Cell Non-Hodgkin's Lymphoma1
2CompletedTreatmentUnresectable or Metastatic Malignant Gastrointestinal Stromal Tumor (GIST)1
2CompletedTreatmentChronic Chronic myelogenous leukemia1
2CompletedTreatmentRefractory Small cell lung cancer1
2Not Yet RecruitingTreatmentCervical Spinal Cord Injury1
2Not Yet RecruitingTreatmentChronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Minimal Residual Disease1
2Not Yet RecruitingTreatmentLeukemia, Myelogenous, Chronic, BCR-ABL Positive1
2Not Yet RecruitingTreatmentLoaisis1
2RecruitingPreventionPatients Who Have Received Allo-HSCT1
2RecruitingTreatmentAdult Acute Lymphoblastic Leukemia / Adult Lymphoblastic Lymphoma / CD20 Positive / Philadelphia Chromosome Positive1
2RecruitingTreatmentAdvanced, Refractory Cancer1
2RecruitingTreatmentChronic Chronic myelogenous leukemia / Chronic Myeloid Leukemia (CML) / CML / Hematologic Diseases1
2RecruitingTreatmentChronic Myeloid Leukemia (CML)1
2RecruitingTreatmentChronic Myeloid Leukemia (CML) / Philadelphia Chromosome Positive CML1
2RecruitingTreatmentColonic Neoplasms1
2RecruitingTreatmentDisseminated Sclerosis1
2RecruitingTreatmentGastrointestinal Stromal Tumors1
2RecruitingTreatmentGastrointestinal Stromal Tumors (GISTs)1
2RecruitingTreatmentGastrointestinal Stromal Tumours1
2RecruitingTreatmentHypereosinophilic Syndromes1
2RecruitingTreatmentPlasmodium Falciparum Malaria (Drug Resistant)1
2RecruitingTreatmentPlexiform Neurofibroma1
2RecruitingTreatmentPlexiform Neurofibromas1
2RecruitingTreatmentRefractory Pediatric AML / Refractory Pediatric Solid Tumors / Relapsed Pediatric AML / Relapsed Pediatric Solid Tumors1
2SuspendedTreatmentAcute Lymphoblastic Leukemia (ALL) Philadelphia Chromosome-positive (Ph+)1
2TerminatedTreatmentAcute Lymphoblastic Leukaemias (ALL)1
2TerminatedTreatmentBlast Phase / Chronic Myeloid Leukemia (CML) / Myeloid Leukemia, Chronic, Accelerated-Phase / Myeloid Leukemia, Chronic, Chronic-Phase1
2TerminatedTreatmentCancer Brain / Gastrointestinal Stromal Tumors / Malignancies / Tumors, Solid1
2TerminatedTreatmentCancer of the Ovary1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentChronic Myeloid Leukemia (CML)2
2TerminatedTreatmentChronic Chronic myelogenous leukemia / Chronic Myeloid Leukemia (CML) / Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Leukemias1
2TerminatedTreatmentChronic Myeloproliferative Disorders1
2TerminatedTreatmentGIST / Metastatic Disease1
2TerminatedTreatmentGastric Adenocarcinoma1
2TerminatedTreatmentGastrointestinal Stromal Tumors1
2TerminatedTreatmentGlioblastomas1
2TerminatedTreatmentHypereosinophilic Syndromes1
2TerminatedTreatmentLeukemias5
2TerminatedTreatmentLeukemias / Malignant Lymphomas1
2TerminatedTreatmentLung Cancers1
2TerminatedTreatmentMalignancies1
2TerminatedTreatmentMelanoma1
2TerminatedTreatmentMetastatic Melanoma1
2TerminatedTreatmentMyelogenous Leukemia, Chronic, Chronic Phase1
2TerminatedTreatmentOvarian Dysgerminoma / Recurrent Malignant Testicular Germ Cell Tumor / Recurrent Ovarian Germ Cell Tumor / Stage II Malignant Testicular Germ Cell Tumor / Stage II Ovarian Germ Cell Tumor / Stage III Malignant Testicular Germ Cell Tumor / Stage III Ovarian Germ Cell Tumor / Testicular Seminoma1
2TerminatedTreatmentPulmonary Hypertension (PH)1
2TerminatedTreatmentRecurrent Glioblastoma Multiforme (GBM)1
2TerminatedTreatmentRenal Cancers1
2TerminatedTreatmentScleroderma1
2TerminatedTreatmentThyroid Cancers1
2TerminatedTreatmentChronic Chronic myelogenous leukemia1
2Unknown StatusNot AvailableAcute Lymphocytic Leukemia (ALL)1
2Unknown StatusNot AvailableChronic Myeloid Leukemia (CML)1
2Unknown StatusTreatmentBrain and Central Nervous System Tumors1
2Unknown StatusTreatmentCancers of the Head and Neck / Carcinoma, Adenoid Cystic1
2Unknown StatusTreatmentChronic Myeloid Leukemia (CML) With Philadelphia Chromosome-positive (Ph+)1
2Unknown StatusTreatmentGastrointestinal Stromal Tumors1
2Unknown StatusTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2Unknown StatusTreatmentLeukemias3
2Unknown StatusTreatmentLymphoid Blastic Phase of Chronic Myeloid Leukemia / Philadelphia Positive Acute Lymphoblastic Leukemia1
2Unknown StatusTreatmentMelanoma1
2Unknown StatusTreatmentSclerosis, Progressive Systemic1
2Unknown StatusTreatmentChronic Chronic myelogenous leukemia1
2Unknown StatusTreatmentNephrogenic systemic fibrosis (NSF)1
2WithdrawnTreatmentB Acute Lymphoblastic Leukemia / B Lymphoblastic Lymphoma / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent B Lymphoblastic Lymphoma / Recurrent T Lymphoblastic Leukemia/Lymphoma / Refractory B Lymphoblastic Lymphoma / Refractory T Lymphoblastic Lymphoma / T Acute Lymphoblastic Leukemia / T Lymphoblastic Lymphoma1
2WithdrawnTreatmentChronic Myeloid Leukemia, Blast Crisis / Leukemia Acute Myeloid Leukemia (AML)1
2WithdrawnTreatmentEosinophilia / Hypereosinophilic Syndromes1
2WithdrawnTreatmentMetastatic Solid Tumors1
2WithdrawnTreatmentChronic Chronic myelogenous leukemia1
2, 3CompletedEducational/Counseling/TrainingChronic Lung Diseases / Idiopathic Pulmonary Fibrosis (IPF) / Pulmonary Fibrosis1
2, 3CompletedTreatmentChronic Myeloid Leukemia (CML) / Gastrointestinal Stromal Tumors1
2, 3CompletedTreatmentPulmonary Arterial Hypertension (PAH)1
2, 3TerminatedTreatmentMalignant Peripheral Nerve Sheath Tumour (MPNST)1
3Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
3Active Not RecruitingTreatmentLeukemia, Myelogenous, Chronic, Breakpoint Cluster Region-Abelson Proto-oncogene (BCR-ABL) Positive1
3Active Not RecruitingTreatmentChronic Chronic myelogenous leukemia2
3CompletedTreatmentAstrocytomas / Glioblastoma Multiforme (GBM)1
3CompletedTreatmentBone Marrow Diseases / Hematologic Diseases / Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Leukemias / Myeloid Leukemias / Philadelphia Chromosome1
3CompletedTreatmentCML, CML-CP,MMR,TKI1
3CompletedTreatmentChildhood Acute Lymphoblastic Leukemia in Remission / Recurrent Childhood Acute Lymphoblastic Leukemia1
3CompletedTreatmentChronic Myelogenous Leukemia in Chronic Phase1
3CompletedTreatmentChronic Myeloid Leukemia (CML)5
3CompletedTreatmentGastrointestinal Stromal Tumors5
3CompletedTreatmentGastrointestinal Stromal Tumors (GISTs)1
3CompletedTreatmentLeukemia, Lymphocytic1
3CompletedTreatmentLeukemia, Myeloid, Chronic, BCR-ABL Positive1
3CompletedTreatmentLeukemias4
3CompletedTreatmentMyeloid Leukemia, Chronic, Chronic Phase1
3CompletedTreatmentPulmonary Arterial Hypertension (PAH)2
3CompletedTreatmentSarcomas1
3CompletedTreatmentChronic Chronic myelogenous leukemia3
3CompletedTreatmentNephrogenic systemic fibrosis (NSF)1
3Not Yet RecruitingDiagnosticGastrointestinal Stromal Tumors1
3Not Yet RecruitingTreatmentChronic Myeloid Leukemia, Chronic Phase1
3RecruitingPreventionGastrointestinal Stromal Tumors / High Risk of Recurrence / KIT + / KIT Gene Mutation / Non-metastatic / Resected Gastrointestinal Stromal Tumors1
3RecruitingTreatmentAcute Ischaemic Stroke1
3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Acute Lymphocytic Leukemia (ALL) / Leukaemia, Lymphoblastic / Leukemia, Lymphoblastic, Acute, Philadelphia-Positive / Lymphoblastic Leukemia, Acute, Adult / Ph1 Chromosome1
3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / B Acute Lymphoblastic Leukemia / B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / BCR-ABL1 Fusion Protein Expression / Minimal Residual Disease / Philadelphia Chromosome Positive / T Acute Lymphoblastic Leukemia / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Lymphoma, Lymphoblastic1
3RecruitingTreatmentChronic Myeloid Leukemia (CML)2
3RecruitingTreatmentGraft Versus Host Disease (GVHD) / Graft-versus-host Disease (GVHD)1
3RecruitingTreatmentLeukemias / Mucositis / Oral Complications1
3RecruitingTreatmentPhiladelphia Chromosome Positive Adult Acute Lymphoblastic Leukemia1
3RecruitingTreatmentSarcomas1
3SuspendedTreatmentChronic Myeloid Leukemia (CML)1
3TerminatedTreatmentChronic Myeloid Leukemia (CML)1
3TerminatedTreatmentGastrointestinal Stromal Tumors5
3TerminatedTreatmentLeukemia, Myeloid, Chronic Phase1
3TerminatedTreatmentLeukemia, Myeloid, Chronic-Phase1
3TerminatedTreatmentLeukemias1
3TerminatedTreatmentMyelogenous Leukemia1
3TerminatedTreatmentPulmonary Arterial Hypertension (PAH)2
3Unknown StatusTreatmentChronic Myeloid Leukemia (CML)2
3Unknown StatusTreatmentGastrointestinal Stromal Tumors1
3Unknown StatusTreatmentLeukemia, Myeloid, Philadelphia-Positive1
4Active Not RecruitingOtherChronic Myeloid Leukemia (CML)1
4CompletedNot AvailableChronic Myeloid Leukemia (CML)1
4CompletedTreatmentCancer, Breast1
4CompletedTreatmentChronic Myeloid Leukemia (CML)1
4CompletedTreatmentGastrointestinal Stromal Tumors1
4CompletedTreatmentProgressive Gastrointestinal Stromal Tumor1
4CompletedTreatmentSystemic Mastocytosis1
4CompletedTreatmentChronic Chronic myelogenous leukemia2
4No Longer AvailableNot AvailableGastrointestinal Stromal Tumors1
4Not Yet RecruitingTreatmentChronic Myeloid Leukemia (CML)1
4RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
4RecruitingTreatmentAcute Lymphoblastic Leukemia Ph Positive1
4RecruitingTreatmentChronyc Myeloid Leukemia1
4RecruitingTreatmentGIST and CML1
Not AvailableAvailableNot AvailableChronic Myeloid Leukemia (CML)1
Not AvailableCompletedNot AvailableAll Indications for Glivec/Gleevec and Tasigna1
Not AvailableCompletedNot AvailableChronic Myeloid Leukemia (CML) / Newly Diagnosed1
Not AvailableCompletedNot AvailableChronic Myeloid Leukemia, Chronic Phase1
Not AvailableCompletedNot AvailableLeukemia, Myeloid, Chronic-Phase (CML-CP)1
Not AvailableCompletedTreatmentChronic Myeloid Leukemia (CML)1
Not AvailableCompletedTreatmentChronic Myeloid Leukemia (CML) / Chronic Myelomonocytic Leukemia / Hypereosinophilic Syndromes / Polycythemia Vera (PV) / Urticaria Pigmentosa1
Not AvailableCompletedTreatmentChronic Myeloid Leukemia (CML) / Gastrointestinal Stromal Tumors1
Not AvailableCompletedTreatmentL1 Childhood Acute Lymphoblastic Leukemia / L2 Childhood Acute Lymphoblastic Leukemia / Non-T, Non-B Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / T-cell Childhood Acute Lymphoblastic Leukemia1
Not AvailableCompletedTreatmentLeukemias1
Not AvailableNot Yet RecruitingNot AvailablePhiladelphia Chromosome-positive Chronic Myeloid Leukemia in Chronic Phase1
Not AvailableRecruitingNot AvailableAcute Lymphoblastic Leukaemias (ALL)1
Not AvailableRecruitingNot AvailableChronic Myeloid Leukemia (CML)1
Not AvailableRecruitingNot AvailableGIST1
Not AvailableRecruitingNot AvailableMethod of Differentiating Benignancy and Malignancy, Grading and Staging for GIST1
Not AvailableRecruitingTreatmentGastrointestinal Cancers1
Not AvailableRecruitingTreatmentChronic Chronic myelogenous leukemia1
Not AvailableTerminatedNot AvailableChronic Chronic myelogenous leukemia1
Not AvailableUnknown StatusNot AvailableChronic Myeloid Leukemia (CML)1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
Packagers
  • Murfreesboro Pharmaceutical Nursing Supply
  • Novartis AG
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
CapsuleOral100 mg
TabletOral100 mg
TabletOral100 mg/1
TabletOral400 mg
TabletOral400 mg/1
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)
CA2093203No2002-11-262013-04-01Canada
USRE43932Yes2013-01-152019-07-16Us
US7544799Yes2009-06-092019-07-16Us
US6894051Yes2005-05-172019-11-23Us
US6958335Yes2005-10-252022-06-19Us
US5521184Yes1996-05-282015-07-04Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)226 °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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0006-0000900000-3974d719909aa7a75039
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0006-0000900000-dd386ae17930da36c11f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0f6x-0159500000-576f293e026deaa1ec7f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0ik9-0495000000-06102c4afd3c2e88cf87
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-03ka-0971000000-b487f693e17cba198e37
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-05fs-0930000000-9319811c561fd5cc8f2f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0159-4910000000-25480eb9451aee843c26
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9000000000-0638bee21655c0e0ca00
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-9000000000-76f9b62b017fe8241e67
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0000900000-9825e12c65f9bf36d72f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-1029200000-acd76280414e767f0280
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-2269000000-f55e5c707c9de5ba2d0f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00ba-3494000000-19e7d8361f050ec8b637
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00ba-3693000000-c1e011113081e3341bba
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0596-5981000000-a0f689cd067d45644bcd
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f9f-5930000000-71f05e812cf29e11cc69
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00ku-5910000000-3f91ea6a6f7402767a78
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-029i-7900000000-507c771376ea4b799b6d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0191000000-fb24a3158c9475186c82
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0036900000-e06abe669a9b1b57e2c3
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-3379600000-f122458b106bcf2c8b8e

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Anilides
Direct Parent
Benzanilides
Alternative Parents
Pyridinylpyrimidines / Benzamides / Diaminotoluenes / Aniline and substituted anilines / Benzoyl derivatives / Benzylamines / Phenylmethylamines / N-methylpiperazines / Aminopyrimidines and derivatives / Aralkylamines
show 11 more
Substituents
Benzanilide / Pyridinylpyrimidine / Benzamide / Benzoic acid or derivatives / Diaminotoluene / Phenylmethylamine / Benzoyl / Benzylamine / Aniline or substituted anilines / Aminopyrimidine
show 27 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
pyrimidines, benzamides, pyridines, aromatic amine, N-methylpiperazine (CHEBI:45783)

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
Uniprot Name
BCR/ABL fusion protein isoform X9
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
Antagonist
Multitarget
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 main...
Gene Name
KIT
Uniprot ID
P10721
Uniprot Name
Mast/stem cell growth factor receptor Kit
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
Uniprot Name
RET proto-oncogene
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 sympatheti...
Gene Name
NTRK1
Uniprot ID
P04629
Uniprot Name
High affinity nerve growth factor receptor
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 ...
Gene Name
CSF1R
Uniprot ID
P07333
Uniprot Name
Macrophage colony-stimulating factor 1 receptor
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 chem...
Gene Name
PDGFRA
Uniprot ID
P16234
Uniprot Name
Platelet-derived growth factor receptor alpha
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, dif...
Gene Name
DDR1
Uniprot ID
Q08345
Uniprot Name
Epithelial discoidin domain-containing receptor 1
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 a...
Gene Name
ABL1
Uniprot ID
P00519
Uniprot Name
Tyrosine-protein kinase ABL1
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...
Gene Name
PDGFRB
Uniprot ID
P09619
Uniprot Name
Platelet-derived growth factor receptor beta
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

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Substrate
Inhibitor
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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
Substrate
Inhibitor
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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. van Erp N, Gelderblom H, van Glabbeke M, Van Oosterom A, Verweij J, Guchelaar HJ, Debiec-Rychter M, Peng B, Blay JY, Judson I: Effect of cigarette smoking on imatinib in patients in the soft tissue and bone sarcoma group of the EORTC. Clin Cancer Res. 2008 Dec 15;14(24):8308-13. doi: 10.1158/1078-0432.CCR-08-1303. [PubMed:19088049]
  3. Liu XY, Xu T, Li WS, Luo J, Geng PW, Wang L, Xia MM, Chen MC, Yu L, Hu GX: The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184. doi: 10.1155/2013/789184. Epub 2013 Nov 28. [PubMed:24369535]
  4. Imatinib FDA label [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Recoche I, Rousseau V, Bourrel R, Lapeyre-Mestre M, Chebane L, Despas F, Montastruc JL, Bondon-Guitton E: Drug-drug interactions with imatinib: An observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076. doi: 10.1097/MD.0000000000005076. [PubMed:27749579]
  2. Imatinib FDA label [File]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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 gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
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

Details
1. Serum albumin
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
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...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. 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]
  2. 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]
  3. Watkins DB, Hughes TP, White DL: OCT1 and imatinib transport in CML: is it clinically relevant? Leukemia. 2015 Oct;29(10):1960-9. doi: 10.1038/leu.2015.170. Epub 2015 Jul 9. [PubMed:26122430]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
Uniprot Name
Multidrug resistance protein 1
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, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
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
Substrate
Inhibitor
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
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
Uniprot Name
ATP-binding cassette sub-family A member 3
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]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on December 16, 2018 23:29