Treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia (CML) with resistance or intolerance to prior therapy including imatinib. Treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.

Dasatinib, an inhibitor of multiple tyrosine kinase, is an antineoplastic agent. At nanomolar concentrations, it inhibits the following kinases: BCR ABL, SRC family (SRC, LKC, YES, FYN), c-KIT, EPHA2, and platelet derived growth factor receptor (PDGFRβ).

Metabolism: Hepatic (extensive); metabolized by CYP3A4 (primarily), flavin-containing mono-oxygenase-3 (FOM-3) and uridine diphosphate-glucuronosyltransferase (UGT) to an active metabolite and other inactive metabolites. The overall mean terminal half-life of dasatinib is 3–5 hours.

Hypersensitivity to dasatinib or any other component of the formulation

D

Excretion in breast milk unknown/not recommended

Most common adverse reactions (320%) included fluid retention events, diarrhea, headache, skin rash, nausea, hemorrhage, fatigue, and dyspnea.; Hemotologic effects: neutropenia, anemia, thrombocytopenia.

Chronic phase CML: 100 mg once daily. Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL: 70 mg twice daily.
Administer once daily (morning or evening). May be taken without regard to food. Swallow whole; do not break, crush, or chew tablets. Take with a meal or with a large glass of water if GI upset occurs.
Avoid concomitant administration with strong CYP3A4 inhibitors (eg, clarithromycin, itraconazole, ketoconazole, nefazodone, protease inhibitors, telithromycin, voriconazole, grapefruit juice); if concomitant administration with a strong CYP3A4 inhibitor cannot be avoided, consider reducing the dasatinib dose with careful monitoring.
Avoid concomitant administration with strong CYP3A4 inducers (eg, carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin, St John’s wort); if concomitant administration with a strong CYP3A4 inducer cannot be avoided, consider increasing the dasatinib dose with careful monitoring.