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Identification
NameBosutinib
Accession NumberDB06616
TypeSmall Molecule
GroupsApproved
DescriptionBosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012.
Structure
Thumb
Synonyms
4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile
Bosulif®
Bosutinib
Bosutinib Monohydrate
SKI 606
SKI-606
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bosuliftablet, film coated100 mg/1oralPfizer Laboratories Div Pfizer Inc2012-09-04Not applicableUs
Bosuliftablet500 mgoralPfizer Canada Inc2014-03-24Not applicableCanada
Bosuliftablet, film coated500 mg/1oralPfizer Laboratories Div Pfizer Inc2012-09-04Not applicableUs
Bosuliftablet, film coated100 mg/1oralU.S. Pharmaceuticals2012-09-04Not applicableUs
Bosuliftablet100 mgoralPfizer Canada Inc2014-04-24Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5018V4AEZ0
CAS number380843-75-4
WeightAverage: 530.446
Monoisotopic: 529.164745233
Chemical FormulaC26H29Cl2N5O3
InChI KeyInChIKey=UBPYILGKFZZVDX-UHFFFAOYSA-N
InChI
InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)
IUPAC Name
4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
SMILES
COC1=CC(NC2=C(C=NC3=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23)C#N)=C(Cl)C=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as aminoquinolines and derivatives. These are organic compounds containing an amino group attached to a quinoline ring system.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassAminoquinolines and derivatives
Direct ParentAminoquinolines and derivatives
Alternative Parents
Substituents
  • Hydroxyquinoline
  • Aminoquinoline
  • Methoxyaniline
  • Methoxybenzene
  • Substituted aniline
  • Phenol ether
  • 1,3-dichlorobenzene
  • Anisole
  • N-alkylpiperazine
  • N-methylpiperazine
  • Halobenzene
  • Chlorobenzene
  • Aniline
  • Aminopyridine
  • Alkyl aryl ether
  • Benzenoid
  • Pyridine
  • Piperazine
  • 1,4-diazinane
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Nitrile
  • Carbonitrile
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy in adult patients.
PharmacodynamicsNot Available
Mechanism of actionBosutinib is a tyrosine kinase inhibitor. Although it is able to inhibit several tyrosine kinases such as Src, Lyn, and Hck, which are members of the Src-family of kinases, its primary target is the Bcr-Abl kinase. The Bcr-Abl gene is a chimeric oncogene created from the fusion of the breakpoint-cluster (Bcr) gene and Abelson (Abl) tyrosine gene. This chromosomal abnormality results in the formation of what is commonly known as the Philadelphia chromosome or Philadelphia translocation. The Bcr-Abl gene expresses a particular kinase that promotes the progression of CML. A decrease in the growth and size of the CML tumour has been observed following administration of bosutinib. Bosutinib did not inhibit the T315I and V299L mutant cells.
Related Articles
AbsorptionFood increase the exposure of bosutinib. Tmax, single dose, cancer patients, fed-state = 4-6 hours; After 15 daily doses of bosutinib 500 mg with food in CML patients, the pharmacokinetic parameters are as follows: Cmax = 200 ng/mL; AUC = 3650 ng∙h/mL
Volume of distribution

Apparent volume of distribution = 6080 ± 1230 L.

Protein binding94% bound to human plasma proteins in vitro. 96% bound to human plasma proteins in healthy subjects ex vivo. Extent of protein binding is not concentration-dependent.
Metabolism

Bosutinib is primarily metabolized by CYP3A4. The major circulating metabolites identified in plasma are oxydechlorinated (M2) bosutinib (19% of parent exposure) and N-desmethylated (M5) bosutinib (25% of parent exposure), with bosutinib N-oxide (M6) as a minor circulating metabolite. All the metabolites were deemed inactive.

Route of eliminationWhen given a single oral dose, 91.3% of the dose was recovered in feces and 3% of the dose recovered in urine.
Half lifeTerminal phase elimination half-life, single oral dose, fed-state = 22.5 hours
Clearance

Mean clearance (CL/F), single oral dose, fed-state = 189 L/h

ToxicityMost common adverse reactions (incidence greater than 20%) are diarrhea, nausea, thrombocytopenia, vomiting, abdominal pain, rash, anemia, pyrexia, and fatigue. Because bosutinib is not an inhibitor of c-KIT or PDGF receptor, it has less hematologic toxicities.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9823
Blood Brain Barrier+0.9272
Caco-2 permeable+0.6542
P-glycoprotein substrateSubstrate0.7601
P-glycoprotein inhibitor IInhibitor0.8409
P-glycoprotein inhibitor IIInhibitor0.9108
Renal organic cation transporterInhibitor0.5663
CYP450 2C9 substrateNon-substrate0.854
CYP450 2D6 substrateNon-substrate0.6953
CYP450 3A4 substrateSubstrate0.6987
CYP450 1A2 substrateInhibitor0.5606
CYP450 2C9 inhibitorNon-inhibitor0.7372
CYP450 2D6 inhibitorNon-inhibitor0.5136
CYP450 2C19 inhibitorNon-inhibitor0.5725
CYP450 3A4 inhibitorInhibitor0.5
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7021
Ames testAMES toxic0.5922
CarcinogenicityNon-carcinogens0.8869
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.4201 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6147
hERG inhibition (predictor II)Inhibitor0.7754
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral500 mg
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral500 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6002008 No1998-03-272018-03-27Us
US7417148 No2006-01-232026-01-23Us
US7767678 No2006-11-232026-11-23Us
US7919625 No2005-12-112025-12-11Us
USRE42376 No1999-09-242019-09-24Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0095 mg/mLALOGPS
logP4.87ALOGPS
logP4.09ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)15.48ChemAxon
pKa (Strongest Basic)8.43ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area82.88 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity142.12 m3·mol-1ChemAxon
Polarizability56.14 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Amsberg GK, Schafhausen P: Bosutinib in the management of chronic myelogenous leukemia. Biologics. 2013;7:115-22. doi: 10.2147/BTT.S30182. Epub 2013 May 6. [PubMed:23674887 ]
  2. Keller-V Amsberg G, Brummendorf TH: Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia. Expert Rev Anticancer Ther. 2012 Sep;12(9):1121-7. doi: 10.1586/era.12.84. [PubMed:23098112 ]
  3. Link [Link]
External Links
ATC CodesL01XE14
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (326 KB)
MSDSDownload (97.1 KB)
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Bosutinib.
AcetaminophenThe serum concentration of Bosutinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Bosutinib.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Bosutinib.
AfatinibThe serum concentration of Bosutinib can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Bosutinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Bosutinib can be decreased when it is combined with Aldosterone.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Bosutinib.
AlectinibThe serum concentration of Bosutinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Bosutinib can be increased when it is combined with Alfentanil.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Bosutinib.
Aluminum hydroxideThe serum concentration of Bosutinib can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Bosutinib can be decreased when it is combined with Aluminum phosphate.
AmantadineThe serum concentration of Bosutinib can be increased when it is combined with Amantadine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Bosutinib.
Aminohippuric acidThe serum concentration of Bosutinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Bosutinib can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Bosutinib can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Bosutinib can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Bosutinib can be increased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Bosutinib can be increased when it is combined with Amsacrine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Bosutinib.
AprepitantThe serum concentration of Bosutinib can be increased when it is combined with Aprepitant.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Bosutinib.
AsenapineThe serum concentration of Bosutinib can be decreased when it is combined with Asenapine.
AstemizoleThe serum concentration of Bosutinib can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Bosutinib can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Bosutinib can be increased when it is combined with Atenolol.
AtomoxetineThe serum concentration of Bosutinib can be increased when it is combined with Atomoxetine.
AtorvastatinThe serum concentration of Bosutinib can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Bosutinib.
AzelastineThe serum concentration of Bosutinib can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Bosutinib can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Bosutinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Bosutinib can be increased when it is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Bosutinib.
BevacizumabBevacizumab may increase the cardiotoxic activities of Bosutinib.
BexaroteneThe serum concentration of Bosutinib can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Bosutinib can be increased when it is combined with Biperiden.
Bismuth SubcitrateThe serum concentration of Bosutinib can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Bosutinib can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bosutinib can be increased when it is combined with Bortezomib.
BosentanThe serum concentration of Bosutinib can be decreased when it is combined with Bosentan.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Bosutinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Bosutinib can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Bosutinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Bosutinib can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Bosutinib can be increased when it is combined with Caffeine.
Calcium carbonateThe serum concentration of Bosutinib can be decreased when it is combined with Calcium carbonate.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Bosutinib.
CanagliflozinThe serum concentration of Bosutinib can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Bosutinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Bosutinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Bosutinib can be increased when it is combined with Carbamazepine.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Bosutinib.
CarvedilolThe serum concentration of Bosutinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Bosutinib can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of Bosutinib can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Bosutinib.
ChloroquineThe serum concentration of Bosutinib can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Bosutinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Bosutinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Bosutinib can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Bosutinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Bosutinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Bosutinib can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Bosutinib can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Bosutinib can be increased when it is combined with Ciprofloxacin.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Bosutinib.
CitalopramThe serum concentration of Bosutinib can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Bosutinib can be increased when it is combined with Clarithromycin.
ClemastineThe serum concentration of Bosutinib can be increased when it is combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Bosutinib.
ClofazimineThe serum concentration of Bosutinib can be increased when it is combined with Clofazimine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Bosutinib.
ClomipramineThe serum concentration of Bosutinib can be increased when it is combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Bosutinib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Bosutinib.
ClotrimazoleThe serum concentration of Bosutinib can be increased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Bosutinib is combined with Clozapine.
CobicistatThe serum concentration of Bosutinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Bosutinib.
ColchicineThe serum concentration of Bosutinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Bosutinib can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Bosutinib can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Bosutinib.
CrizotinibThe serum concentration of Bosutinib can be increased when it is combined with Crizotinib.
CyclophosphamideThe serum concentration of Bosutinib can be increased when it is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Bosutinib can be increased when it is combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Bosutinib.
DabrafenibThe serum concentration of Bosutinib can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Bosutinib.
DaclatasvirThe serum concentration of Bosutinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Bosutinib can be increased when it is combined with Dactinomycin.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Bosutinib.
DarunavirThe serum concentration of Bosutinib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Bosutinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Bosutinib can be increased when it is combined with Daunorubicin.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Bosutinib.
DeferasiroxThe serum concentration of Bosutinib can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Bosutinib can be increased when it is combined with Delavirdine.
DesipramineThe serum concentration of Bosutinib can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Bosutinib.
DesloratadineThe serum concentration of Bosutinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Bosutinib can be increased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Bosutinib can be increased when it is combined with Dextromethorphan.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Bosutinib.
DiclofenacThe serum concentration of Bosutinib can be increased when it is combined with Diclofenac.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Bosutinib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Bosutinib.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Bosutinib.
DigoxinThe serum concentration of Bosutinib can be increased when it is combined with Digoxin.
DihydroergotamineThe serum concentration of Bosutinib can be increased when it is combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Bosutinib.
DiltiazemThe serum concentration of Bosutinib can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Bosutinib can be increased when it is combined with Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Bosutinib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Bosutinib.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Bosutinib.
DoxazosinThe serum concentration of Bosutinib can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Bosutinib can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Bosutinib can be increased when it is combined with Doxorubicin.
DoxycyclineThe serum concentration of Bosutinib can be increased when it is combined with Doxycycline.
DronabinolThe serum concentration of Bosutinib can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Bosutinib can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Bosutinib.
EfavirenzThe serum concentration of Bosutinib can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Bosutinib can be increased when it is combined with Elbasvir.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Bosutinib.
EnalaprilThe serum concentration of Bosutinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Bosutinib can be increased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Bosutinib can be decreased when it is combined with Epinastine.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Bosutinib.
ErgonovineThe serum concentration of Bosutinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Bosutinib can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Bosutinib.
ErythromycinThe serum concentration of Bosutinib can be increased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Bosutinib can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Bosutinib can be decreased when it is combined with Esomeprazole.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Bosutinib.
EstramustineThe serum concentration of Bosutinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Bosutinib can be decreased when it is combined with Estriol.
EstriolThe serum concentration of Estriol can be increased when it is combined with Bosutinib.
EstroneThe serum concentration of Bosutinib can be decreased when it is combined with Estrone.
EstroneThe serum concentration of Estrone can be increased when it is combined with Bosutinib.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Bosutinib.
EtoposideThe serum concentration of Bosutinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Bosutinib can be increased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Bosutinib.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Bosutinib.
FamotidineThe serum concentration of Bosutinib can be decreased when it is combined with Famotidine.
FelodipineThe serum concentration of Bosutinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Bosutinib can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Bosutinib.
FexofenadineThe serum concentration of Bosutinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Bosutinib can be increased when it is combined with Fidaxomicin.
FluconazoleThe serum concentration of Bosutinib can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Bosutinib can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Bosutinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Bosutinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Bosutinib can be increased when it is combined with Flurazepam.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Bosutinib.
FluvoxamineThe serum concentration of Bosutinib can be increased when it is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Bosutinib can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Bosutinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Bosutinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Bosutinib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Bosutinib can be increased when it is combined with Gefitinib.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Bosutinib.
GenisteinThe serum concentration of Bosutinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Bosutinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Bosutinib can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Bosutinib can be increased when it is combined with Gramicidin D.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Bosutinib.
GrepafloxacinThe serum concentration of Bosutinib can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Bosutinib can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Bosutinib can be increased when it is combined with Hydrocortisone.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Bosutinib.
IdelalisibThe serum concentration of Bosutinib can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Bosutinib can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Bosutinib can be increased when it is combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Bosutinib.
IndinavirThe serum concentration of Bosutinib can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Bosutinib can be increased when it is combined with Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Bosutinib.
IsavuconazoniumThe serum concentration of Bosutinib can be increased when it is combined with Isavuconazonium.
IsradipineThe serum concentration of Bosutinib can be increased when it is combined with Isradipine.
ItraconazoleThe serum concentration of Bosutinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Bosutinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Bosutinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Bosutinib can be increased when it is combined with Ketamine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Bosutinib.
KetoconazoleThe serum concentration of Bosutinib can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Bosutinib.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Bosutinib.
LansoprazoleThe serum concentration of Bosutinib can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Bosutinib can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Bosutinib.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Bosutinib.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Bosutinib.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Bosutinib.
LevofloxacinThe serum concentration of Bosutinib can be increased when it is combined with Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Bosutinib.
LevothyroxineThe serum concentration of Bosutinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Bosutinib can be increased when it is combined with Lidocaine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Bosutinib.
LiothyronineThe serum concentration of Bosutinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Bosutinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Bosutinib can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Bosutinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Bosutinib can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Bosutinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Bosutinib can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Bosutinib can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Bosutinib can be increased when it is combined with Lovastatin.
LuliconazoleThe serum concentration of Bosutinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Bosutinib can be decreased when it is combined with Lumacaftor.
MagaldrateThe serum concentration of Bosutinib can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Bosutinib can be decreased when it is combined with Magnesium carbonate.
Magnesium hydroxideThe serum concentration of Bosutinib can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Bosutinib can be decreased when it is combined with Magnesium oxide.
Magnesium TrisilicateThe serum concentration of Bosutinib can be decreased when it is combined with Magnesium Trisilicate.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Bosutinib.
MaprotilineThe serum concentration of Bosutinib can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Bosutinib can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Bosutinib can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Bosutinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Bosutinib can be increased when it is combined with Meprobamate.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Bosutinib.
MethadoneThe serum concentration of Bosutinib can be increased when it is combined with Methadone.
MethanthelineThe serum concentration of Bosutinib can be decreased when it is combined with Methantheline.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Bosutinib.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Bosutinib.
MetiamideThe serum concentration of Bosutinib can be decreased when it is combined with Metiamide.
MetoprololThe serum concentration of Bosutinib can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Bosutinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Bosutinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Bosutinib can be increased when it is combined with Midazolam.
MifepristoneThe serum concentration of Bosutinib can be increased when it is combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Bosutinib.
MitomycinThe serum concentration of Bosutinib can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Bosutinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Bosutinib can be increased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Bosutinib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Bosutinib can be increased when it is combined with Morphine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Bosutinib.
NadololThe serum concentration of Nadolol can be increased when it is combined with Bosutinib.
NafcillinThe serum concentration of Bosutinib can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Bosutinib.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Bosutinib.
NaltrexoneThe serum concentration of Bosutinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Bosutinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Bosutinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Bosutinib can be increased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Bosutinib can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Bosutinib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Bosutinib can be increased when it is combined with Nevirapine.
NicardipineThe serum concentration of Bosutinib can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Bosutinib can be increased when it is combined with Nifedipine.
NilotinibThe serum concentration of Bosutinib can be increased when it is combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Bosutinib.
NisoldipineThe serum concentration of Bosutinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Bosutinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Bosutinib can be increased when it is combined with Nitrendipine.
NizatidineThe serum concentration of Bosutinib can be decreased when it is combined with Nizatidine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Bosutinib.
NorethisteroneThe serum concentration of Bosutinib can be decreased when it is combined with Norethisterone.
OlanzapineThe serum concentration of Bosutinib can be decreased when it is combined with Olanzapine.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Bosutinib.
OlaparibThe serum concentration of Bosutinib can be increased when it is combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Bosutinib.
OmeprazoleThe serum concentration of Bosutinib can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Bosutinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Bosutinib.
P-NitrophenolThe serum concentration of Bosutinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Bosutinib can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Bosutinib can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Bosutinib can be increased when it is combined with Palmitic Acid.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Bosutinib.
PantoprazoleThe serum concentration of Bosutinib can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Bosutinib can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Bosutinib.
PentobarbitalThe serum concentration of Bosutinib can be decreased when it is combined with Pentobarbital.
PerindoprilThe serum concentration of Bosutinib can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Bosutinib can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Bosutinib.
PhenytoinThe serum concentration of Bosutinib can be decreased when it is combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Bosutinib.
PimozideThe serum concentration of Bosutinib can be increased when it is combined with Pimozide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Bosutinib.
Platelet Activating FactorThe serum concentration of Bosutinib can be decreased when it is combined with Platelet Activating Factor.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Bosutinib.
PonatinibThe serum concentration of Bosutinib can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Bosutinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Bosutinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Bosutinib can be increased when it is combined with Prazosin.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Bosutinib.
PrednisoneThe serum concentration of Bosutinib can be increased when it is combined with Prednisone.
PrimidoneThe serum concentration of Bosutinib can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Bosutinib can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Bosutinib can be increased when it is combined with Progesterone.
PromethazineThe serum concentration of Bosutinib can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Bosutinib can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Bosutinib can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Bosutinib can be increased when it is combined with Protriptyline.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Bosutinib.
QuercetinThe serum concentration of Bosutinib can be increased when it is combined with Quercetin.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Bosutinib.
QuinacrineThe serum concentration of Bosutinib can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Bosutinib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Bosutinib can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Bosutinib can be decreased when it is combined with Rabeprazole.
RanitidineThe serum concentration of Bosutinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Bosutinib.
ReboxetineThe serum concentration of Bosutinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Bosutinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Bosutinib can be increased when it is combined with Reserpine.
RifabutinThe serum concentration of Bosutinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Bosutinib can be increased when it is combined with Rifampicin.
RifapentineThe serum concentration of Bosutinib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Bosutinib.
RilpivirineThe serum concentration of Bosutinib can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Bosutinib.
RitonavirThe serum concentration of Bosutinib can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Bosutinib.
RolapitantThe serum concentration of Bosutinib can be increased when it is combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Bosutinib.
Roxatidine acetateThe serum concentration of Bosutinib can be decreased when it is combined with Roxatidine acetate.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Bosutinib.
SaquinavirThe serum concentration of Bosutinib can be increased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Bosutinib can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Bosutinib can be increased when it is combined with Selegiline.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Bosutinib.
SertralineThe serum concentration of Bosutinib can be increased when it is combined with Sertraline.
SildenafilThe serum concentration of Bosutinib can be increased when it is combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Bosutinib.
SiltuximabThe serum concentration of Bosutinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Bosutinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Bosutinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Bosutinib can be increased when it is combined with Sirolimus.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Bosutinib.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Bosutinib.
SorafenibThe serum concentration of Bosutinib can be increased when it is combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Bosutinib.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Bosutinib.
SpironolactoneThe serum concentration of Bosutinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Bosutinib can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Bosutinib can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Bosutinib can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Bosutinib can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Bosutinib can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe serum concentration of Bosutinib can be increased when it is combined with Sulfisoxazole.
SumatriptanThe serum concentration of Bosutinib can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Bosutinib can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Bosutinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Bosutinib can be increased when it is combined with Tacrolimus.
TAK-390MRThe serum concentration of Bosutinib can be decreased when it is combined with TAK-390MR.
TamoxifenThe serum concentration of Bosutinib can be increased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Bosutinib can be increased when it is combined with Taurocholic Acid.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Bosutinib.
TelaprevirThe serum concentration of Bosutinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Bosutinib can be increased when it is combined with Telithromycin.
TelmisartanThe serum concentration of Bosutinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Bosutinib can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Bosutinib can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Bosutinib can be increased when it is combined with Terfenadine.
TesmilifeneThe serum concentration of Bosutinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Bosutinib can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Bosutinib can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Bosutinib can be increased when it is combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Bosutinib.
TocilizumabThe serum concentration of Bosutinib can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Bosutinib can be increased when it is combined with Tolvaptan.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Bosutinib.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Bosutinib.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Bosutinib.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Bosutinib.
TrazodoneThe serum concentration of Bosutinib can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Bosutinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Bosutinib can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Bosutinib can be increased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Bosutinib can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Bosutinib can be increased when it is combined with Troleandomycin.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Bosutinib.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Bosutinib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Bosutinib.
VenlafaxineThe serum concentration of Bosutinib can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Bosutinib can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Bosutinib can be increased when it is combined with Vinblastine.
VincristineThe serum concentration of Bosutinib can be increased when it is combined with Vincristine.
VinorelbineThe serum concentration of Bosutinib can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Bosutinib.
VoriconazoleThe serum concentration of Bosutinib can be increased when it is combined with Voriconazole.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Bosutinib.
ZimelidineThe serum concentration of Bosutinib can be increased when it is combined with Zimelidine.
ZiprasidoneThe serum concentration of Bosutinib can be increased when it is combined with Ziprasidone.
Food Interactions
  • When given with a high fat meal, the Cmax and AUC of bosutinib increased 1.8- and 1.7-fold, respectively.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Rho guanyl-nucleotide exchange factor activity
Specific Function:
GTPase-activating protein for RAC1 and CDC42. Promotes the exchange of RAC or CDC42-bound GDP by GTP, thereby activating them. Displays serine/threonine kinase activity.
Gene Name:
BCR
Uniprot ID:
P11274
Molecular Weight:
142818.07 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor signaling protein tyrosine kinase activity
Specific Function:
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, responses to growth factors and cytokines, integrin signaling, but also responses to DNA damage and genotoxic agents. Functions primarily as negative regulator, but can also function as activator, depending ...
Gene Name:
LYN
Uniprot ID:
P07948
Molecular Weight:
58573.595 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase found in hematopoietic cells that transmits signals from cell surface receptors and plays an important role in the regulation of innate immune responses, including neutrophil, monocyte, macrophage and mast cell functions, phagocytosis, cell survival and proliferation, cell adhesion and migration. Acts downstream of receptors that bind the Fc region of immuno...
Gene Name:
HCK
Uniprot ID:
P08631
Molecular Weight:
59599.355 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sh3/sh2 adaptor activity
Specific Function:
Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion receptors, receptor protein tyrosine kinases, G protein-coupled receptors as well as cytokine receptors. Participates in signaling pathways that control a diverse spectrum of biological activities including...
Gene Name:
SRC
Uniprot ID:
P12931
Molecular Weight:
59834.295 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synt...
Gene Name:
CDK2
Uniprot ID:
P24941
Molecular Weight:
33929.215 Da
References
  1. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [PubMed:19039322 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Receptor signaling protein tyrosine phosphatase activity
Specific Function:
Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2...
Gene Name:
MAP2K1
Uniprot ID:
Q02750
Molecular Weight:
43438.65 Da
References
  1. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [PubMed:19039322 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Scaffold protein binding
Specific Function:
Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity).
Gene Name:
MAP2K2
Uniprot ID:
P36507
Molecular Weight:
44423.735 Da
References
  1. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Muller A, Baumgartner C, Valent P, Augustin M, Till JH, Superti-Furga G: Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. doi: 10.1038/leu.2008.334. Epub 2008 Nov 27. [PubMed:19039322 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Component of a protein kinase signal transduction cascade. Regulates the JNK and ERK5 pathways by phosphorylating and activating MAP2K5 and MAP2K7 (By similarity). Plays a role in caveolae kiss-and-run dynamics.
Gene Name:
MAP3K2
Uniprot ID:
Q9Y2U5
Molecular Weight:
69740.21 Da
References
  1. Ahmad S, Hughes MA, Johnson GL, Scott JE: Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors. J Biomol Screen. 2013 Apr;18(4):388-99. doi: 10.1177/1087057112466430. Epub 2012 Nov 7. [PubMed:23134735 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Protein homodimerization activity
Specific Function:
Calcium/calmodulin-dependent protein kinase that functions autonomously after Ca(2+)/calmodulin-binding and autophosphorylation, and is involved in sarcoplsamic reticulum Ca(2+) transport in skeletal muscle and may function in dendritic spine and synapse formation and neuronal plasticity. In slow-twitch muscles, is involved in regulation of sarcoplasmic reticulum (SR) Ca(2+) transport and in fa...
Gene Name:
CAMK2G
Uniprot ID:
Q13555
Molecular Weight:
62608.655 Da
References
  1. Amsberg GK, Koschmieder S: Profile of bosutinib and its clinical potential in the treatment of chronic myeloid leukemia. Onco Targets Ther. 2013;6:99-106. doi: 10.2147/OTT.S19901. Epub 2013 Mar 4. [PubMed:23493838 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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

Transporters

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
Comments
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Drug created on March 19, 2008 10:41 / Updated on September 26, 2016 02:14