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Dasatinib, at nano molar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2 and PDGFRB. 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 inhibits 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 over expression.
Dasatinib is a kinase inhibitor indicated for the treatment of:
ï¬ Newly diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic
myeloid leukemia (CML) in chronic phase.
ï¬ Adults with chronic, accelerated or myeloid or lymphoid blast phase Ph+ CML with
resistance or intolerance to prior therapy including Imatinib.
ï¬ Adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+
ALL) with resistance or intolerance to prior therapy
DanibÂ® Tablet 100 mg: Each commercial box contains 30 tablets in Alu-Alu blister