asciminib + dasatinib

Asciminib + dasatinib is an investigational oral combination of two small-molecule tyrosine kinase inhibitors developed for the dual inhibition of the BCR-ABL1 oncoprotein in Philadelphia chromosome–positive leukemias, particularly acute lymphoblastic leukemia (Ph+ ALL) and chronic myeloid leukemia in lymphoid blast crisis (CML-LBC). Asciminib is a first-in-class allosteric inhibitor that targets the myristoyl pocket of ABL1, locking the BCR-ABL1 fusion kinase into an inactive conformation and thus preventing leukemogenic signaling. Dasatinib is an ATP-competitive inhibitor of BCR-ABL1 and several other kinases. The combination is intended to provide deeper molecular responses and prevent the emergence of resistant disease by targeting both the allosteric and ATP-binding sites of BCR-ABL1. The combination, with or without the addition of prednisone, has demonstrated promising safety and efficacy signals in early-phase clinical trials, with high rates of hematologic and cytogenetic remission in Ph+ ALL[1][3][5][7][9].

Other names

asciminib + dasatinib