asciminib + imatinib

Asciminib + imatinib is a combination of two small-molecule tyrosine kinase inhibitors for the treatment of chronic myeloid leukemia (CML), particularly in patients with resistance or suboptimal response to prior therapy. Asciminib is a first-in-class allosteric inhibitor that specifically targets the myristoyl pocket of ABL1 (STAMP inhibitor), locking the BCR-ABL1 fusion protein in an inactive conformation. Imatinib is an ATP-competitive inhibitor of BCR-ABL1. When combined, these drugs synergistically inhibit BCR-ABL1 through distinct mechanisms, enhancing efficacy and potentially overcoming resistance, as demonstrated in preclinical and clinical trials (notably ASC4MORE). This combination is being developed primarily for CML patients who have not achieved deep molecular response or have failed previous lines of kinase inhibitor therapy. Novartis is the primary developer and sponsor of the published trials[1][3][4][6][7][8].

Other names

asciminib plus imatinibASC + IMA