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venetoclax + azacitidine + cytarabine
- Development stage
- Unknown
- Lead developer
- AbbVie and Genentech
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
Venetoclax + azacitidine + cytarabine is an investigational combination regimen, sometimes referred to as the VAA regimen, used primarily in the treatment of relapsed or refractory acute myeloid leukemia (AML). Venetoclax is a selective BCL-2 inhibitor that promotes apoptosis in malignant hematologic cells. Azacitidine is a hypomethylating agent that incorporates into DNA and RNA, leading to DNA hypomethylation and direct cytotoxicity. Cytarabine is an antimetabolite chemotherapeutic agent that inhibits DNA synthesis. The combination leverages synergistic effects between these agents to induce cell death in AML blasts, with clinical studies showing high rates of composite complete remission (CRc) and manageable safety profiles in relapsed/refractory AML patients[1][2]. This specific triple-drug combination has been studied mainly for R/R AML but each component has broader use individually or as doublets.
- Other names
- VAA regimen
02
Targets
DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNA polymerase family
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