Which generation of targeted drug is Dasatinib?

Dasatinib is a second-generation targeted drug used to treat Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML) in adults and children. It is also used to treat adults with Ph+ CML and Philadelphia chromosome-positive acute lymphoblastic leukemia(Ph+ ALL) after other drugs have failed.

Dasatinib is a second-generation BCR-ABL inhibitor with superior efficacy in vitro against engineered cell lines expressing non-mutated BCR-ABL Tinib is 325 times more effective and has inhibitory activity against most imatinib-resistant BCR-ABL mutants. DasatinibTablets are white to off-white biconvex film-coated tablets containing dasatinib and the following inactive ingredients:Lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hydroxypropylcellulose, and magnesium stearate. The tablet coating consists of hypromellose, titanium dioxide, and polyethylene glycol.

A high-fat meal increased the mean AUCof a single 100 mgdasatinib dose by 14%. The total calories of the high-fat food is 985kcal. The calories from fat, carbohydrates, and protein in the high-fat meal were 52%, 34%, and 14%, respectively. The mean terminal half-life of dasatinib ranges from 3 hours to 5 hours. The average apparent oral clearance was 363.8 liters/hour (CV% 81.3%). Dasatinib is mainly metabolized by CYP3A4 in the human body. CYP3A4 is the main enzyme responsible for the formation of active metabolites. Flavin monooxygenase3 (FMO-3)and uridine diphosphate glucuronosyltransferase(UGT)Also involved in the formation of dasatinib metabolites. Exposure to an active metabolite equivalent to dasatinib is approximately 5% of the AUC of dasatinib. It is unlikely that the active metabolite of dasatinib plays a major role in the observed pharmacology of this drug,Dasatinib also has several other inactive oxidative metabolites. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to learn more about high-quality overseas drugs for you.

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