Products
Mirsonib
Pharmacotherapeutic group
antitumor agents; protein kinase inhibitors; BCR-ABL tyrosine kinase inhibitorsInternational name
DasatinibDosage form
film-coated tabletsDasatinib inhibits BCR-ABL and SRC family tyrosine kinases, as well as many other oncogenic kinases, including c-KIT, ephrin receptor kinase (ERK) and PDGFβ receptor. It binds to active and inactive forms of the BCR-ABL enzyme and inhibits it at subnanomolar concentrations (0.6-0.8 nmol/mL). Under in vitro conditions, dasatinib exhibits activity in cellular models of leukemia, both against sensitive and resistant cells to imatinib. It overcomes resistance to imatinib associated with BCR-ABL overexpression, BCR-ABL kinase domain mutations, activation of alternative mechanisms inducing SRC family kinases (LYN, ISK), as well as overexpression of multidrug resistance gene.