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tamibarotene + venetoclax + azacitidine
- Development stage
- Unknown
- Lead developer
- Syros Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
Tamibarotene + venetoclax + azacitidine is an investigational **oral combination therapy** for adults with newly diagnosed acute myeloid leukemia (AML) with *retinoic acid receptor alpha* (RARA) overexpression who are unfit for intensive induction chemotherapy. Tamibarotene is a first-in-class, selective retinoic acid receptor alpha (RARα) agonist. Venetoclax is a BCL-2 inhibitor, and azacitidine is a nucleoside metabolic inhibitor and DNA methyltransferase inhibitor. The combination aims to target leukemic differentiation (via tamibarotene), evade apoptosis inhibition (via venetoclax), and induce hypomethylation and cytotoxicity (via azacitidine). This triplet received FDA Fast Track Designation and is currently in phase 2 trials (SELECT-AML-1) for AML with RARA overexpression.
- Brand names
- VidazaVenclextaAmnolake
- Other names
- SY-1425 + Azacitidine + VenetoclaxTamibarotene + Azacitidine + Venetoclax
02
Targets
DNMT3A (DNA methyltransferase 3 alpha)RARA (Retinoic acid receptor alpha)DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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