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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
SynonymLanguageCode
Anh. dasatinibNot AvailableNot Available
Anhydrous dasatinibNot AvailableNot Available
BMS dasatinibNot AvailableNot Available
BMS-354825Not AvailableNot Available
DasatinibNot AvailableNot Available
Dasatinib (anh.)Not AvailableNot Available
DasatinibumNot AvailableNot Available
N-(2-CHLORO-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamideNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Spryceltablet70 mgoralE.R. Squibb & Sons, L.L.C.2006-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet20 mgoralE.R. Squibb & Sons, L.L.C.2006-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet50 mgoralE.R. Squibb & Sons, L.L.C.2006-06-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet100 mgoralE.R. Squibb & Sons, L.L.C.2008-05-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet80 mgoralE.R. Squibb & Sons, L.L.C.2010-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet140 mgoralE.R. Squibb & Sons, L.L.C.2010-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet70 mgoralPhysicians Total Care, Inc.2007-02-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Spryceltablet20 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet50 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet70 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet100 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet80 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Spryceltablet140 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
CAS number302962-49-8
WeightAverage: 488.006
Monoisotopic: 487.155721508
Chemical FormulaC22H26ClN7O2S
InChI KeyZBNZXTGUTAYRHI-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 substrateInhibitor0.8008
CYP450 2D6 substrateNon-inhibitor0.8358
CYP450 2C19 substrateInhibitor0.574
CYP450 3A4 substrateInhibitor0.7295
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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral140 mg
Tabletoral20 mg
Tabletoral50 mg
Tabletoral70 mg
Tabletoral80 mg
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 Reference
  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
AbciximabMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
AcenocoumarolDasatinib may enhance the anticoagulant effect of Anticoagulants.
AcetaminophenAcetaminophen may enhance the hepatotoxic effect of Dasatinib. Dasatinib may increase the serum concentration of Acetaminophen.
Acetylsalicylic acidMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
ado-trastuzumab emtansineMay increase the serum concentration of CYP3A4 Substrates.
AlfentanilMay increase the serum concentration of CYP3A4 Substrates.
AlfuzosinMay increase the serum concentration of CYP3A4 Substrates.
AlprazolamMay increase the serum concentration of CYP3A4 Substrates.
Aluminum hydroxideMay decrease the absorption of Dasatinib.
AminophyllineMay increase the serum concentration of CYP3A4 Substrates.
AmlodipineMay increase the serum concentration of CYP3A4 Substrates.
ApixabanMay enhance the anticoagulant effect of Anticoagulants.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
ArgatrobanMay enhance the anticoagulant effect of Anticoagulants.
AripiprazoleMay increase the serum concentration of CYP3A4 Substrates.
armodafinilMay increase the serum concentration of CYP3A4 Substrates.
AtazanavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
AtorvastatinMay increase the serum concentration of CYP3A4 Substrates.
AvanafilMay increase the serum concentration of CYP3A4 Substrates.
AxitinibMay increase the serum concentration of CYP3A4 Substrates.
BenzphetamineMay increase the serum concentration of CYP3A4 Substrates.
BisoprololMay increase the serum concentration of CYP3A4 Substrates.
BivalirudinMay enhance the anticoagulant effect of Anticoagulants.
BoceprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
BosutinibMay increase the serum concentration of CYP3A4 Substrates.
BromocriptineMay increase the serum concentration of CYP3A4 Substrates.
BuprenorphineMay increase the serum concentration of CYP3A4 Substrates.
BuspironeMay increase the serum concentration of CYP3A4 Substrates.
ButalbitalAcetaminophen may enhance the hepatotoxic effect of Dasatinib. Dasatinib may increase the serum concentration of Acetaminophen.
CabazitaxelMay increase the serum concentration of CYP3A4 Substrates.
CabozantinibMay increase the serum concentration of CYP3A4 Substrates.
CalcitriolMay increase the serum concentration of CYP3A4 Substrates.
Calcium carbonateMay decrease the absorption of Dasatinib.
CarbamazepineCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
ChlordiazepoxideMay increase the serum concentration of CYP3A4 Substrates.
ChloroquineMay increase the serum concentration of CYP3A4 Substrates.
CilostazolMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
CimetidineH2-Antagonists may decrease the absorption of Dasatinib.
CinacalcetMay increase the serum concentration of CYP3A4 Substrates.
Citric AcidDasatinib may enhance the anticoagulant effect of Anticoagulants.
ClarithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
ClidiniumMay increase the serum concentration of CYP3A4 Substrates.
ClonazepamMay increase the serum concentration of CYP3A4 Substrates.
ClopidogrelMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
ClozapineMyelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for agranulocytosis may be increased.
CocaineMay increase the serum concentration of CYP3A4 Substrates.
ColchicineMay increase the serum concentration of CYP3A4 Substrates.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
CrizotinibMay increase the serum concentration of CYP3A4 Substrates.
Cyproterone acetateMay increase the serum concentration of CYP3A4 Substrates.
Dabigatran etexilateMay enhance the anticoagulant effect of Anticoagulants.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DalteparinDasatinib may enhance the anticoagulant effect of Anticoagulants.
DanaparoidMay enhance the anticoagulant effect of Anticoagulants.
DantroleneMay increase the serum concentration of CYP3A4 Substrates.
DarifenacinMay increase the serum concentration of CYP3A4 Substrates.
DarunavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
DenosumabMay enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased.
DesvenlafaxineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
DiazepamMay increase the serum concentration of CYP3A4 Substrates.
DicoumarolDasatinib may enhance the anticoagulant effect of Anticoagulants.
DiflunisalMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
DihydrocodeineAcetaminophen may enhance the hepatotoxic effect of Dasatinib. Dasatinib may increase the serum concentration of Acetaminophen.
DihydroergotamineMay increase the serum concentration of CYP3A4 Substrates.
DiltiazemMay increase the serum concentration of CYP3A4 Substrates.
DipyridamoleMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
DocetaxelMay increase the serum concentration of CYP3A4 Substrates.
DoxazosinMay increase the serum concentration of CYP3A4 Substrates.
DuloxetineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
Edetic AcidDasatinib may enhance the anticoagulant effect of Anticoagulants.
EletriptanMay increase the serum concentration of CYP3A4 Substrates.
EnoxaparinMay enhance the anticoagulant effect of Anticoagulants.
EnzalutamideCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
EplerenoneMay increase the serum concentration of CYP3A4 Substrates.
EptifibatideMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
Ergoloid mesylateMay increase the serum concentration of CYP3A4 Substrates.
ErgonovineMay increase the serum concentration of CYP3A4 Substrates.
ErgotamineMay increase the serum concentration of CYP3A4 Substrates.
ErlotinibMay increase the serum concentration of CYP3A4 Substrates.
EsomeprazoleProton Pump Inhibitors may decrease the serum concentration of Dasatinib.
EszopicloneMay increase the serum concentration of CYP3A4 Substrates.
Ethinyl EstradiolMay increase the serum concentration of CYP3A4 Substrates.
EthosuximideMay increase the serum concentration of CYP3A4 Substrates.
Ethyl biscoumacetateDasatinib may enhance the anticoagulant effect of Anticoagulants.
EtodolacMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
EtoposideMay increase the serum concentration of CYP3A4 Substrates.
EverolimusMay increase the serum concentration of CYP3A4 Substrates.
FamotidineH2-Antagonists may decrease the absorption of Dasatinib.
FelbamateMay increase the serum concentration of CYP3A4 Substrates.
FelodipineMay increase the serum concentration of CYP3A4 Substrates.
FenoprofenMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
FentanylMay increase the serum concentration of CYP3A4 Substrates.
FesoterodineMay increase the serum concentration of CYP3A4 Substrates.
FloctafenineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
FlurazepamMay increase the serum concentration of CYP3A4 Substrates.
FlutamideMay increase the serum concentration of CYP3A4 Substrates.
Fluticasone furoateMay increase the serum concentration of CYP3A4 Substrates.
FluvoxamineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
Fondaparinux sodiumMay enhance the anticoagulant effect of Anticoagulants.
FosamprenavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
FosphenytoinCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
GefitinibMay increase the serum concentration of CYP3A4 Substrates.
GuanfacineMay increase the serum concentration of CYP3A4 Substrates.
HaloperidolMay increase the serum concentration of CYP3A4 Substrates.
HeparinMay enhance the anticoagulant effect of Anticoagulants.
HydrocodoneMay increase the serum concentration of CYP3A4 Substrates.
IbuprofenMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
IndinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
IndomethacinMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
IrinotecanMay increase the serum concentration of CYP3A4 Substrates.
IsavuconazoniumMay increase the serum concentration of CYP3A4 Substrates.
IsomethepteneAcetaminophen may enhance the hepatotoxic effect of Dasatinib. Dasatinib may increase the serum concentration of Acetaminophen.
Isosorbide DinitrateMay increase the serum concentration of CYP3A4 Substrates.
Isosorbide MononitrateMay increase the serum concentration of CYP3A4 Substrates.
IsradipineMay increase the serum concentration of CYP3A4 Substrates.
ItraconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
IxabepiloneMay increase the serum concentration of CYP3A4 Substrates.
KetamineMay increase the serum concentration of CYP3A4 Substrates.
KetoprofenMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
KetorolacMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
LansoprazoleProton Pump Inhibitors may decrease the serum concentration of Dasatinib.
LapatinibMay increase the serum concentration of CYP3A4 Substrates.
LeflunomideImmunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased.
LevomilnacipranMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
LomitapideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide.
LopinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
LovastatinMay increase the serum concentration of CYP3A4 Substrates.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
LurasidoneMay increase the serum concentration of CYP3A4 Substrates.
MACITENTANMay increase the serum concentration of CYP3A4 Substrates.
Magnesium oxideMay decrease the absorption of Dasatinib.
MaravirocMay increase the serum concentration of CYP3A4 Substrates.
Mefenamic acidMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
MefloquineMay increase the serum concentration of CYP3A4 Substrates.
MeloxicamMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
MethadoneMay increase the serum concentration of CYP3A4 Substrates.
MethylergometrineMay increase the serum concentration of CYP3A4 Substrates.
MidazolamMay increase the serum concentration of CYP3A4 Substrates.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MilnacipranMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
MirtazapineMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
ModafinilMay increase the serum concentration of CYP3A4 Substrates.
NabumetoneMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
NadroparinMay enhance the anticoagulant effect of Anticoagulants.
NaproxenMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
NatalizumabImmunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased.
NateglinideMay increase the serum concentration of CYP3A4 Substrates.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
NelfinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
NifedipineMay increase the serum concentration of CYP3A4 Substrates.
NimodipineMay increase the serum concentration of CYP3A4 Substrates.
NisoldipineMay increase the serum concentration of CYP3A4 Substrates.
NizatidineH2-Antagonists may decrease the absorption of Dasatinib.
OmeprazoleProton Pump Inhibitors may decrease the serum concentration of Dasatinib.
OxaprozinMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
OxycodoneMay increase the serum concentration of CYP3A4 Substrates.
PanobinostatMay increase the serum concentration of CYP3A4 Substrates.
PantoprazoleProton Pump Inhibitors may decrease the serum concentration of Dasatinib.
ParoxetineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
PazopanibMay increase the serum concentration of CYP3A4 Substrates.
PhenindioneDasatinib may enhance the anticoagulant effect of Anticoagulants.
PhenobarbitalCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
PhenprocoumonDasatinib may enhance the anticoagulant effect of Anticoagulants.
PhenytoinCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
PimecrolimusMay enhance the adverse/toxic effect of Immunosuppressants.
PimozideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
PipotiazineMay increase the serum concentration of CYP3A4 Substrates.
PiroxicamMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
PomalidomideMay increase the serum concentration of CYP3A4 Substrates.
PosaconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
PrasugrelMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
PraziquantelMay increase the serum concentration of CYP3A4 Substrates.
PrimidoneCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
RabeprazoleProton Pump Inhibitors may decrease the serum concentration of Dasatinib.
RanitidineH2-Antagonists may decrease the absorption of Dasatinib.
RanolazineMay increase the serum concentration of CYP3A4 Substrates.
RegorafenibMay increase the serum concentration of CYP3A4 Substrates.
RifampicinCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
RifapentineCYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib.
RitonavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
RivaroxabanMay enhance the anticoagulant effect of Anticoagulants.
RoflumilastMay enhance the immunosuppressive effect of Immunosuppressants.
RuxolitinibMay increase the serum concentration of CYP3A4 Substrates.
SalmeterolMay increase the serum concentration of CYP3A4 Substrates.
SaquinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
SaxagliptinMay increase the serum concentration of CYP3A4 Substrates.
SertralineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
SildenafilMay increase the serum concentration of CYP3A4 Substrates.
SilodosinMay increase the serum concentration of CYP3A4 Substrates.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of CYP3A4 Substrates.
SimvastatinMay increase the serum concentration of CYP3A4 Substrates.
Sipuleucel-TImmunosuppressants may diminish the therapeutic effect of Sipuleucel-T.
SirolimusMay increase the serum concentration of CYP3A4 Substrates.
Sodium bicarbonateAntacids may decrease the absorption of Dasatinib.
SolifenacinMay increase the serum concentration of CYP3A4 Substrates.
SpiramycinMay increase the serum concentration of CYP3A4 Substrates.
SufentanilMay increase the serum concentration of CYP3A4 Substrates.
SulfisoxazoleMay increase the serum concentration of CYP3A4 Substrates.
SulindacMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
SulodexideDasatinib may enhance the anticoagulant effect of Anticoagulants.
SunitinibMay increase the serum concentration of CYP3A4 Substrates.
SuvorexantMay increase the serum concentration of CYP3A4 Substrates.
TadalafilMay increase the serum concentration of CYP3A4 Substrates.
TamoxifenMay increase the serum concentration of CYP3A4 Substrates.
TamsulosinMay increase the serum concentration of CYP3A4 Substrates.
TelaprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
TelithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dasatinib.
TemsirolimusMay increase the serum concentration of CYP3A4 Substrates.
TeniposideMay increase the serum concentration of CYP3A4 Substrates.
TheophyllineMay increase the serum concentration of CYP3A4 Substrates.
TiagabineMay increase the serum concentration of CYP3A4 Substrates.
Tiaprofenic acidMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
TicagrelorMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
TiclopidineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
TinzaparinMay enhance the anticoagulant effect of Anticoagulants.
TirofibanMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TofacitinibImmunosuppressants may enhance the immunosuppressive effect of Tofacitinib.
TolmetinMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
TolterodineMay increase the serum concentration of CYP3A4 Substrates.
TolvaptanMay increase the serum concentration of CYP3A4 Substrates.
TrabectedinMay increase the serum concentration of CYP3A4 Substrates.
TramadolMay increase the serum concentration of CYP3A4 Substrates.
TrastuzumabMay enhance the neutropenic effect of Immunosuppressants.
TreprostinilDasatinib may enhance the anticoagulant effect of Anticoagulants.
TriazolamMay increase the serum concentration of CYP3A4 Substrates.
TrimipramineMay increase the serum concentration of CYP3A4 Substrates.
VardenafilMay increase the serum concentration of CYP3A4 Substrates.
VenlafaxineMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
VilazodoneMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
VinblastineMay increase the serum concentration of CYP3A4 Substrates.
VincristineMay increase the serum concentration of CYP3A4 Substrates.
VinorelbineMay increase the serum concentration of CYP3A4 Substrates.
VorapaxarMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
VoriconazoleVoriconazole may enhance the QTc-prolonging effect of Dasatinib. Voriconazole may increase the serum concentration of Dasatinib.
WarfarinDasatinib may enhance the anticoagulant effect of Anticoagulants.
ZolpidemMay increase the serum concentration of CYP3A4 Substrates.
ZonisamideMay increase the serum concentration of CYP3A4 Substrates.
ZopicloneMay increase the serum concentration of CYP3A4 Substrates.
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