Drug intelligence / Profile preview

lisaftoclax + olverembatinib + azacitidine

Development stage
Approved
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Intravenous, Oral, Subcutaneous
01

Overview

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.

Other names
APG-2575 + HQP1351 + AZAAPG-2575 + HQP1351 + azacitidineAPG-2575 + HQP1351 + azacytidineAPG-2575 + HQP1351 + 阿扎胞苷lisaftoclax + olverembatinib + AZAlisaftoclax + olverembatinib + azacitidinelisaftoclax + olverembatinib + azacytidine利沙托克拉 + 奥雷巴替尼 + 阿扎胞苷利生妥 + 耐立克 + azacitidine利生妥 + 耐立克 + 阿扎胞苷
02

Targets

BCL-2 (BCL-2 family)DNMT1 (DNA (cytosine-5)-methyltransferase 1)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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