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olutasidenib + azacitidine
- Development stage
- Unknown
- Lead developer
- Rigel Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
olutasidenib + azacitidine is a combination therapy consisting of olutasidenib, a potent, selective, oral small-molecule inhibitor specifically targeting mutant isocitrate dehydrogenase 1 (mIDH1), and azacitidine, a hypomethylating agent. Olutasidenib inhibits aberrant IDH1 enzyme activity, reducing 2-hydroxyglutarate levels and leading to reversion of the block in cellular differentiation. Azacitidine, a cytidine analog, is incorporated into DNA and RNA, resulting in DNA hypomethylation and cytotoxicity in abnormal hematopoietic cells. This combination is under investigation for the treatment of relapsed or refractory IDH1-mutated acute myeloid leukemia (AML), higher-risk myelodysplastic syndromes (MDS), chronic myelomonocytic leukemia (CMML), and advanced myeloproliferative neoplasms (MPN). Both agents are administered with olutasidenib orally and azacitidine intravenously or subcutaneously[1][2][3][4][5].
- Other names
- olutasidenib plus azacitidineolutasidenib/azacitidine
02
Targets
DNMT (DNA methyltransferase)IDH1 (Isocitrate dehydrogenase [NADP] cytoplasmic)
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