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Drug intelligence / Profile preview
olverembatinib + venetoclax + azacitidine
- Development stage
- Phase 2
- Lead developer
- Ascentage Pharma
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous, Intravenous
01
Overview
Olverembatinib + venetoclax + azacitidine is a combination therapy currently in Phase II clinical development for the treatment of blast phase chronic myeloid leukemia (CML). This regimen integrates three distinct therapeutic mechanisms: olverembatinib (HQP1351), a third-generation tyrosine kinase inhibitor (TKI) that targets the BCR-ABL1 fusion protein, including the gatekeeper T315I mutation; venetoclax, a selective B-cell lymphoma 2 (BCL-2) inhibitor that promotes apoptosis; and azacitidine, a hypomethylating agent that inhibits DNA methyltransferases. The combination is designed to address the multi-faceted resistance mechanisms observed in advanced CML, such as kinase mutations, anti-apoptotic signaling, and epigenetic dysregulation. By targeting both the underlying oncogenic driver and survival pathways in leukemia stem cells, this combination aims to achieve deeper molecular responses and improve outcomes in patients with blast crisis CML, a population with historically poor prognosis.
- Other names
- Olverembatinib + Venetoclax + AzacitidineHQP1351 + ABT-199 + Azacitidine
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DNMT (DNA methyltransferase)
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