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Identification
NameDasatinib
Accession NumberDB01254
TypeSmall Molecule
GroupsApproved, Investigational
Description

Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.

Structure
Thumb
Synonyms
Anh. dasatinib
Anhydrous dasatinib
BMS dasatinib
BMS-354825
Dasatinib
Dasatinib (anh.)
Dasatinibum
N-(2-CHLORO-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
External Identifiers
  • BMS-354825
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Spryceltablet70 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet20 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet70 mg/1oralPhysicians Total Care, Inc.2007-02-12Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet140 mg/1oralE.R. Squibb & Sons, L.L.C.2010-10-28Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet140 mgoralBristol Myers Squibb Canada2011-03-29Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet80 mg/1oralE.R. Squibb & Sons, L.L.C.2010-10-28Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet80 mgoralBristol Myers Squibb Canada2011-09-02Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet100 mg/1oralE.R. Squibb & Sons, L.L.C.2008-05-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet100 mgoralBristol Myers Squibb Canada2009-05-04Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet50 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet70 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet20 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet50 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIIRBZ1571X5H
CAS number302962-49-8
WeightAverage: 488.006
Monoisotopic: 487.155721508
Chemical FormulaC22H26ClN7O2S
InChI KeyInChIKey=ZBNZXTGUTAYRHI-UHFFFAOYSA-N
InChI
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
IUPAC Name
N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
SMILES
CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentN-arylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • N-arylamide
  • Aminotoluene
  • Dialkylarylamine
  • Thiazolecarboxylic acid or derivatives
  • Thiazolecarboxamide
  • N-alkylpiperazine
  • Toluene
  • Halobenzene
  • Chlorobenzene
  • Aminopyrimidine
  • 2,5-disubstituted 1,3-thiazole
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Thiazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • 1,2-aminoalcohol
  • Azacycle
  • Secondary amine
  • Carboxylic acid derivative
  • Alkanolamine
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy.
PharmacodynamicsDasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor
Mechanism of actionDasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
AbsorptionNot Available
Volume of distribution
  • 2505 L
Protein binding96%
Metabolism

Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4

Route of eliminationDasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces.
Half lifeThe overall mean terminal half-life of dasatinib is 3-5 hours.
ClearanceNot Available
ToxicityAcute overdose in animals was associated with cardiotoxicity.
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+0.9852
Blood Brain Barrier-0.507
Caco-2 permeable-0.5638
P-glycoprotein substrateSubstrate0.6562
P-glycoprotein inhibitor IInhibitor0.5371
P-glycoprotein inhibitor IIInhibitor0.5425
Renal organic cation transporterNon-inhibitor0.7288
CYP450 2C9 substrateNon-substrate0.7061
CYP450 2D6 substrateNon-substrate0.8152
CYP450 3A4 substrateSubstrate0.5704
CYP450 1A2 substrateNon-inhibitor0.5612
CYP450 2C9 inhibitorInhibitor0.8008
CYP450 2D6 inhibitorNon-inhibitor0.8358
CYP450 2C19 inhibitorInhibitor0.574
CYP450 3A4 inhibitorInhibitor0.7295
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8343
Ames testNon AMES toxic0.7185
CarcinogenicityNon-carcinogens0.7308
BiodegradationNot ready biodegradable0.9863
Rat acute toxicity2.4772 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8538
hERG inhibition (predictor II)Inhibitor0.718
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg/1
Tabletoral100 mg
Tabletoral140 mg/1
Tabletoral140 mg
Tabletoral20 mg
Tabletoral20 mg/1
Tabletoral50 mg
Tabletoral50 mg/1
Tabletoral70 mg/1
Tabletoral70 mg
Tabletoral80 mg
Tabletoral80 mg/1
Prices
Unit descriptionCostUnit
Sprycel 100 mg tablet278.24USD tablet
Sprycel 50 mg tablet139.12USD tablet
Sprycel 70 mg tablet139.12USD tablet
Sprycel 20 mg tablet69.56USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada23669322009-08-252020-04-12
United States71258752000-04-132020-04-13
United States74917252005-10-132025-10-13
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point280-286 °CNot Available
logP1.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0128 mg/mLALOGPS
logP2.77ALOGPS
logP3.82ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)8.49ChemAxon
pKa (Strongest Basic)7.22ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area106.51 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity133.08 m3·mol-1ChemAxon
Polarizability51.58 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 ReferenceUS6596746
General References
  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. Pubmed
  2. Talpaz M, Shah NP, Kantarjian H, Donato N, Nicoll J, Paquette R, Cortes J, O’Brien S, Nicaise C, Bleickardt E, Blackwood-Chirchir MA, Iyer V, Chen TT, Huang F, Decillis AP, Sawyers CL: Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med. 2006 Jun 15;354(24):2531-41. Pubmed
External Links
ATC CodesL01XE06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (237 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabDasatinib may increase the anticoagulant activities of Abciximab.
AcenocoumarolDasatinib may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenAcetaminophen may increase the hepatotoxic activities of Dasatinib.
Acetylsalicylic acidDasatinib may increase the anticoagulant activities of Acetylsalicylic acid.
ado-trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Dasatinib.
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Dasatinib.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Dasatinib.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Dasatinib.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Dasatinib.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Dasatinib.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Dasatinib.
ApixabanDasatinib may increase the anticoagulant activities of Apixaban.
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Dasatinib.
ArgatrobanDasatinib may increase the anticoagulant activities of Argatroban.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Dasatinib.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Dasatinib.
AtazanavirThe serum concentration of Dasatinib can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Dasatinib.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Dasatinib.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Dasatinib.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Dasatinib.
BexaroteneThe serum concentration of Dasatinib can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Dasatinib.
BivalirudinDasatinib may increase the anticoagulant activities of Bivalirudin.
BoceprevirThe serum concentration of Dasatinib can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Dasatinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Dasatinib.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Dasatinib.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Dasatinib.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Dasatinib.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Dasatinib.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Dasatinib.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Dasatinib.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Dasatinib.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Dasatinib.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CangrelorDasatinib may increase the anticoagulant activities of Cangrelor.
CarbamazepineThe serum concentration of Dasatinib can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Dasatinib can be increased when it is combined with Ceritinib.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Dasatinib.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Dasatinib.
CilostazolDasatinib may increase the anticoagulant activities of Cilostazol.
CimetidineCimetidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Dasatinib.
CitalopramDasatinib may increase the QTc-prolonging activities of Citalopram.
Citric AcidDasatinib may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Dasatinib can be increased when it is combined with Clarithromycin.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Dasatinib.
ClopidogrelDasatinib may increase the anticoagulant activities of Clopidogrel.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Dasatinib.
ClozapineThe risk or severity of adverse effects can be increased when Dasatinib is combined with Clozapine.
CobicistatThe serum concentration of Dasatinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Dasatinib.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Dasatinib.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Dasatinib.
ConivaptanThe serum concentration of Dasatinib can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Dasatinib.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Dasatinib.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Dasatinib.
Dabigatran etexilateDasatinib may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Dasatinib can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Dasatinib.
DalteparinDasatinib may increase the anticoagulant activities of Dalteparin.
DanaparoidDasatinib may increase the anticoagulant activities of Danaparoid.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Dasatinib.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Dasatinib.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Dasatinib.
DarunavirThe serum concentration of Dasatinib can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Dasatinib can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Dasatinib.
DesirudinDasatinib may increase the anticoagulant activities of Desirudin.
DesvenlafaxineDasatinib may increase the anticoagulant activities of Desvenlafaxine.
DexamethasoneThe serum concentration of Dasatinib can be decreased when it is combined with Dexamethasone.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Dasatinib.
DiclofenacDasatinib may increase the anticoagulant activities of Diclofenac.
DicoumarolDasatinib may increase the anticoagulant activities of Dicoumarol.
DiflunisalDasatinib may increase the anticoagulant activities of Diflunisal.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Dasatinib.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Dasatinib.
DipyridamoleDasatinib may increase the anticoagulant activities of Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Dasatinib.
DofetilideDasatinib may increase the QTc-prolonging activities of Dofetilide.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Dasatinib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Dasatinib.
DuloxetineDasatinib may increase the anticoagulant activities of Duloxetine.
Edetic AcidDasatinib may increase the anticoagulant activities of Edetic Acid.
EdoxabanDasatinib may increase the anticoagulant activities of Edoxaban.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Dasatinib.
EnoxaparinDasatinib may increase the anticoagulant activities of Enoxaparin.
EnzalutamideThe serum concentration of Dasatinib can be decreased when it is combined with Enzalutamide.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Dasatinib.
EptifibatideDasatinib may increase the anticoagulant activities of Eptifibatide.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Dasatinib.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Dasatinib.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Dasatinib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Dasatinib.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Dasatinib.
EsomeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Esomeprazole.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Dasatinib.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Dasatinib.
Ethyl biscoumacetateDasatinib may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacDasatinib may increase the anticoagulant activities of Etodolac.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Dasatinib.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Dasatinib.
FamotidineFamotidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Dasatinib.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Dasatinib.
FenoprofenDasatinib may increase the anticoagulant activities of Fenoprofen.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Dasatinib.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Dasatinib.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Dasatinib.
FloctafenineDasatinib may increase the anticoagulant activities of Floctafenine.
FluconazoleThe metabolism of Dasatinib can be decreased when combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Dasatinib.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Dasatinib.
FlurbiprofenDasatinib may increase the anticoagulant activities of Flurbiprofen.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Dasatinib.
FluvoxamineDasatinib may increase the anticoagulant activities of Fluvoxamine.
Fondaparinux sodiumDasatinib may increase the anticoagulant activities of Fondaparinux sodium.
FosaprepitantThe serum concentration of Dasatinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Dasatinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Dasatinib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Dasatinib.
GoserelinDasatinib may increase the QTc-prolonging activities of Goserelin.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Dasatinib.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Dasatinib.
HeparinDasatinib may increase the anticoagulant activities of Heparin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Dasatinib.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Dasatinib.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Dasatinib.
IbuprofenDasatinib may increase the anticoagulant activities of Ibuprofen.
IdelalisibThe serum concentration of Dasatinib can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Dasatinib can be increased when it is combined with Indinavir.
IndomethacinDasatinib may increase the anticoagulant activities of Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Dasatinib.
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Dasatinib.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Dasatinib.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Dasatinib.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Dasatinib.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Dasatinib.
ItraconazoleThe serum concentration of Dasatinib can be increased when it is combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Dasatinib.
IvacaftorThe serum concentration of Dasatinib can be increased when it is combined with Ivacaftor.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Dasatinib.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Dasatinib.
KetoconazoleThe serum concentration of Dasatinib can be increased when it is combined with Ketoconazole.
KetoprofenDasatinib may increase the anticoagulant activities of Ketoprofen.
KetorolacDasatinib may increase the anticoagulant activities of Ketorolac.
LansoprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Dasatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Dasatinib is combined with Leflunomide.
LeuprolideDasatinib may increase the QTc-prolonging activities of Leuprolide.
LevomilnacipranDasatinib may increase the anticoagulant activities of Levomilnacipran.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Dasatinib.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Dasatinib.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Dasatinib.
LuliconazoleThe serum concentration of Dasatinib can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Dasatinib.
MACITENTANThe serum concentration of MACITENTAN can be increased when it is combined with Dasatinib.
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Dasatinib.
Mefenamic acidDasatinib may increase the anticoagulant activities of Mefenamic acid.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Dasatinib.
MeloxicamDasatinib may increase the anticoagulant activities of Meloxicam.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Dasatinib.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Dasatinib.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Dasatinib.
MifepristoneThe serum concentration of Dasatinib can be increased when it is combined with Mifepristone.
MilnacipranDasatinib may increase the anticoagulant activities of Milnacipran.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Dasatinib.
MitotaneThe serum concentration of Dasatinib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Dasatinib.
NabumetoneDasatinib may increase the anticoagulant activities of Nabumetone.
NadroparinDasatinib may increase the anticoagulant activities of Nadroparin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Dasatinib.
NaproxenDasatinib may increase the anticoagulant activities of Naproxen.
NatalizumabThe risk or severity of adverse effects can be increased when Dasatinib is combined with Natalizumab.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Dasatinib.
NefazodoneThe serum concentration of Dasatinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Dasatinib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Dasatinib can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Dasatinib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Dasatinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Dasatinib.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Dasatinib.
NizatidineNizatidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Dasatinib.
OmeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Omeprazole.
OxaprozinDasatinib may increase the anticoagulant activities of Oxaprozin.
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Dasatinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Dasatinib.
PalbociclibThe serum concentration of Dasatinib can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Dasatinib.
PantoprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Pantoprazole.
ParoxetineDasatinib may increase the anticoagulant activities of Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Dasatinib.
PhenindioneDasatinib may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Dasatinib can be decreased when it is combined with Phenobarbital.
PhenprocoumonDasatinib may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Dasatinib can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dasatinib.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Dasatinib.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Dasatinib.
PiroxicamDasatinib may increase the anticoagulant activities of Piroxicam.
PosaconazoleThe serum concentration of Dasatinib can be increased when it is combined with Posaconazole.
PrasugrelDasatinib may increase the anticoagulant activities of Prasugrel.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Dasatinib.
PrimidoneThe serum concentration of Dasatinib can be decreased when it is combined with Primidone.
PropacetamolDasatinib may increase the hepatotoxic activities of Propacetamol.
RabeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Rabeprazole.
RanitidineRanitidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Dasatinib.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Dasatinib.
RifabutinThe serum concentration of Dasatinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Dasatinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Dasatinib can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Dasatinib can be increased when it is combined with Ritonavir.
RivaroxabanDasatinib may increase the anticoagulant activities of Rivaroxaban.
RoflumilastRoflumilast may increase the immunosuppressive activities of Dasatinib.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Dasatinib.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Dasatinib.
SaquinavirThe serum concentration of Dasatinib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Dasatinib.
SertralineDasatinib may increase the anticoagulant activities of Sertraline.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Dasatinib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Dasatinib.
SiltuximabThe serum concentration of Dasatinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Dasatinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Dasatinib.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Dasatinib.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Dasatinib.
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Dasatinib.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Dasatinib.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Dasatinib.
St. John's WortThe serum concentration of Dasatinib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Dasatinib can be increased when it is combined with Stiripentol.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Dasatinib.
SulindacDasatinib may increase the anticoagulant activities of Sulindac.
SulodexideDasatinib may increase the anticoagulant activities of Sulodexide.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Dasatinib.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Dasatinib.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Dasatinib.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Dasatinib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Dasatinib.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Dasatinib.
TelaprevirThe serum concentration of Dasatinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Dasatinib can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Dasatinib.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Dasatinib.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Dasatinib.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Dasatinib.
Tiaprofenic acidDasatinib may increase the anticoagulant activities of Tiaprofenic acid.
TicagrelorDasatinib may increase the anticoagulant activities of Ticagrelor.
TiclopidineDasatinib may increase the anticoagulant activities of Ticlopidine.
TinzaparinDasatinib may increase the anticoagulant activities of Tinzaparin.
TirofibanDasatinib may increase the anticoagulant activities of Tirofiban.
TocilizumabThe serum concentration of Dasatinib can be decreased when it is combined with Tocilizumab.
TofacitinibDasatinib may increase the immunosuppressive activities of Tofacitinib.
TolmetinDasatinib may increase the anticoagulant activities of Tolmetin.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Dasatinib.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Dasatinib.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Dasatinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Dasatinib.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Dasatinib.
TreprostinilDasatinib may increase the anticoagulant activities of Treprostinil.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Dasatinib.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Dasatinib.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Dasatinib.
VenlafaxineDasatinib may increase the anticoagulant activities of Venlafaxine.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Dasatinib.
VilazodoneDasatinib may increase the anticoagulant activities of Vilazodone.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Dasatinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Dasatinib.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Dasatinib.
VorapaxarDasatinib may increase the anticoagulant activities of Vorapaxar.
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Dasatinib.
VortioxetineDasatinib may increase the anticoagulant activities of Vortioxetine.
WarfarinDasatinib may increase the anticoagulant activities of Warfarin.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Dasatinib.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Dasatinib.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Dasatinib.
Food InteractionsNot Available

Targets

1. Tyrosine-protein kinase ABL1

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: multitarget

Components

Name UniProt ID Details
Tyrosine-protein kinase ABL1 P00519 Details

References:

  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  2. Piccaluga PP, Paolini S, Martinelli G: Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia. Cancer. 2007 Sep 15;110(6):1178-86. Pubmed
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Proto-oncogene tyrosine-protein kinase Src

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: multitarget

Components

Name UniProt ID Details
Proto-oncogene tyrosine-protein kinase Src P12931 Details

References:

  1. Kamath AV, Wang J, Lee FY, Marathe PH: Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol. 2007 Apr 11;. Pubmed
  2. Serrels A, Macpherson IR, Evans TR, Lee FY, Clark EA, Sansom OJ, Ashton GH, Frame MC, Brunton VG: Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib. Mol Cancer Ther. 2006 Dec;5(12):3014-22. Epub 2006 Dec 5. Pubmed
  3. Quintas-Cardama A, Kantarjian H, Cortes J: Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib. Future Oncol. 2006 Dec;2(6):655-65. Pubmed
  4. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res. 2006 Jan 1;66(1):473-81. Pubmed
  5. Nam S, Kim D, Cheng JQ, Zhang S, Lee JH, Buettner R, Mirosevich J, Lee FY, Jove R: Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res. 2005 Oct 15;65(20):9185-9. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

3. Ephrin type-A receptor 2

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Ephrin type-A receptor 2 P29317 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed

4. Tyrosine-protein kinase Lck

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: multitarget

Components

Name UniProt ID Details
Tyrosine-protein kinase Lck P06239 Details

References:

  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. Pubmed
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

5. Tyrosine-protein kinase Yes

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Tyrosine-protein kinase Yes P07947 Details

References:

  1. Trevino JG, Summy JM, Lesslie DP, Parikh NU, Hong DS, Lee FY, Donato NJ, Abbruzzese JL, Baker CH, Gallick GE: Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol. 2006 Mar;168(3):962-72. Pubmed
  2. Margutti S, Laufer SA: Are MAP Kinases Drug Targets? Yes, but Difficult Ones. ChemMedChem. 2007 Aug 13;2(8):1116-1140. Pubmed
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed

6. Mast/stem cell growth factor receptor Kit

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Mast/stem cell growth factor receptor Kit P10721 Details

References:

  1. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res. 2006 Jan 1;66(1):473-81. Pubmed
  2. Shah NP, Lee FY, Luo R, Jiang Y, Donker M, Akin C: Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91. Epub 2006 Jan 24. Pubmed
  3. Dizdar O, Dede DS, Bulut N, Altundag K: Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines. Breast Cancer Res Treat. 2007 Mar 10;. Pubmed

7. Platelet-derived growth factor receptor beta

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Platelet-derived growth factor receptor beta P09619 Details

References:

  1. Zhang Z, Meier KE: New assignments for multitasking signal transduction inhibitors. Mol Pharmacol. 2006 May;69(5):1510-2. Epub 2006 Feb 23. Pubmed
  2. Chen Z, Lee FY, Bhalla KN, Wu J: Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol. 2006 May;69(5):1527-33. Epub 2006 Jan 25. Pubmed
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed

8. Signal transducer and activator of transcription 5B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Signal transducer and activator of transcription 5B P51692 Details

References:

  1. Fiskus W, Pranpat M, Balasis M, Bali P, Estrella V, Kumaraswamy S, Rao R, Rocha K, Herger B, Lee F, Richon V, Bhalla K: Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells. Clin Cancer Res. 2006 Oct 1;12(19):5869-78. Pubmed
  2. Nam S, Williams A, Vultur A, List A, Bhalla K, Smith D, Lee FY, Jove R: Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells. Mol Cancer Ther. 2007 Apr;6(4):1400-5. Pubmed

9. Abelson tyrosine-protein kinase 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: multitarget

Components

Name UniProt ID Details
Abelson tyrosine-protein kinase 2 P42684 Details

References:

  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

10. Tyrosine-protein kinase Fyn

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: multitarget

Components

Name UniProt ID Details
Tyrosine-protein kinase Fyn P06241 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed# van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. Epub 2009 Sep 5. Pubmed
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

2. Cytochrome P450 1A1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. Epub 2009 Sep 5. Pubmed
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

3. Cytochrome P450 1A2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. Epub 2009 Sep 5. Pubmed
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

4. Cytochrome P450 1B1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1B1 Q16678 Details

References:

  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. Epub 2009 Sep 5. Pubmed
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

5. Cytochrome P450 3A5

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. Epub 2009 Sep 5. Pubmed
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

6. Dimethylaniline monooxygenase [N-oxide-forming] 3

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Dimethylaniline monooxygenase [N-oxide-forming] 3 P31513 Details

References:

  1. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. Epub 2008 Jun 12. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. 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. Epub 2010 Apr 27. Pubmed
  2. 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. Epub 2009 Sep 28. Pubmed
  3. 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. Epub 2008 Jul 31. Pubmed

2. ATP-binding cassette sub-family G member 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. 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. Epub 2010 Apr 27. Pubmed
  2. 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. Epub 2009 Sep 28. Pubmed

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Drug created on May 08, 2007 18:32 / Updated on July 14, 2014 13:31