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lisaftoclax + olverembatinib + azacitidine is an investigational combination regimen consisting of lisaftoclax (APG-2575), a selective BCL-2 inhibitor; olverembatinib (HQP1351), a third-generation BCR-ABL tyrosine kinase inhibitor (which also acts as a multikinase inhibitor targeting FLT3, KIT, and other kinases); and azacitidine, a hypomethylating agent. Developed by Ascentage Pharma, this triplet regimen is being evaluated in clinical trials for the treatment of hematologic malignancies, particularly relapsed or refractory acute myeloid leukemia (R/R AML) in patients who have failed prior treatment with venetoclax or other BCL-2 inhibitors. Mechanistically, the combination of BCL-2 inhibition, multikinase/FLT3 inhibition, and DNA hypomethylation synergistically promotes apoptosis and overcomes resistance pathways in leukemia cells.
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