ADMET-Absorption, Distribution, Metabolism, Excretion, and Toxicity

StatusFDA approved
AdministrationN/A
PharmacologyA cancer drug produced by Bristol-Myers Squibb and sold under the trade name Sprycel.

MetabollsmDasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. CYP3A4 was the primary enzyme responsible for the formation of the active metabolite. Flavin-containing monooxygenase 3 (FMO-3) and uridine diphosphate-glucuronosyltransferase (UGT) enzymes are also involved in the formation of dasatinib metabolites. In human liver microsomes, dasatinib was a weak time-dependent inhibitor of CYP3A4. The exposure of the active metabolite, which is equipotent to dasatinib, represents approximately 5% of the dasatinib AUC. This indicates that the active metabolite of dasatinib is unlikely to play a major role in the observed pharmacology of the drug. Dasatinib also had several other inactive oxidative metabolites.
Half life1.3~5 h

ToxicityThe most frequently reported adverse events included fluid retention events such as pleural effusion, gastrointestinal events including diarrhea, nausea, abdominal pain and vomiting, bleeding events. The most frequently reported serious adverse events included pyrexia, pleural effusion, febrile neutropenia, gastrointestinal bleeding, pneumonia, thrombocytopenia, dyspnea, anemia, cardiac failure, and diarrhea.
LD50 (rat)N/A
LD50 (mouse)N/A