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QuickView for Dasatinib (compound)


PubChem
Name: dasatinib
PubChem Compound ID: 11540687
Molecular formula: C22H28ClN7O3S
Molecular weight: 506.022 g/mol
DrugBank
Identification
Name: dasatinib
Name (isomeric): DB01254
Drug Type: small molecule
Synonyms:
BMS-354825
Brand: Sprycel
Category: Protein Kinase Inhibitors
CAS number: 302962-49-8
Pharmacology
Indication: For 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.
Pharmacology: Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor
Mechanism of Action:
Dasatinib, 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 sensi...
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Protein binding: 96%
Biotransformation: Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4
Route of elimination: Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces.
Half Life: The overall mean terminal half-life of dasatinib is 3-5 hours.
Toxicity: Acute overdose in animals was associated with cardiotoxicity.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
RanitidineRanitidine may decrease the serum level of dasatinib.
PhenytoinPhenytoin may decrease the serum level and efficacy of dasatinib.
TelithromycinTelithromycin may reduce clearance of Dasatinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dasatinib if Telithromycin is initiated, discontinued or dose changed.
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