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ivosidenib + azacitidine + venetoclax
- Development stage
- Unknown
- Lead developer
- Servier
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous, Intravenous
01
Overview
This triplet combination therapy consists of ivosidenib, azacitidine, and venetoclax, and is primarily investigated for the treatment of acute myeloid leukemia (AML) harboring IDH1 mutations. Ivosidenib is a small molecule inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme, which prevents the accumulation of the oncometabolite 2-hydroxyglutarate (2-HG) and promotes the differentiation of malignant cells. Azacitidine is a hypomethylating agent that inhibits DNA methyltransferases, leading to the reversal of epigenetic silencing of tumor suppressor genes. Venetoclax is a selective inhibitor of the anti-apoptotic protein BCL-2, which restores the apoptotic signaling pathway in leukemia cells. Clinical studies suggest that this combination may overcome resistance mechanisms observed with single-agent IDH inhibitors and achieve high rates of deep molecular remission in patients with IDH1-mutated myeloid malignancies.
- Brand names
- TibsovoVenclextaVenclyxtoVidaza
- Other names
- IVA tripletivosidenib plus azacitidine plus venetoclax
02
Targets
IDH1 (Isocitrate dehydrogenase [NADP] cytoplasmic)DNMT (DNA methyltransferase)
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