Drug intelligence / Profile preview

olutasidenib + gemcitabine + cisplatin

Development stage
Unknown
Lead developer
Rigel Pharmaceuticals
Modality
Small Molecules
Administration
Oral (olutasidenib), Intravenous (gemcitabine), Intravenous (cisplatin)
01

Overview

**olutasidenib + gemcitabine + cisplatin** is a combination regimen consisting of olutasidenib (a potent, selective, oral small molecule inhibitor of mutant isocitrate dehydrogenase 1), gemcitabine (a nucleoside analog antimetabolite that interferes with DNA synthesis), and cisplatin (a platinum-based DNA-damaging agent)[3][1][2]. Olutasidenib targets mutant IDH1 (isocitrate dehydrogenase 1), blocking the production of the oncometabolite 2-hydroxyglutarate, and is developed primarily for cancers with IDH1 mutations such as acute myeloid leukemia[3][5]. Gemcitabine is mainly indicated for various solid tumors, including pancreatic, biliary tract, and urothelial cancers, and cisplatin is widely used as a chemotherapeutic agent for numerous malignancies[1][2]. This specific triple-drug combination would be hypothesized for use in IDH1-mutant solid tumors such as cholangiocarcinoma, although most clinical studies to date use ivosidenib (another mutant IDH1 inhibitor) rather than olutasidenib in combinations with cisplatin and gemcitabine[4].

Other names
olutasidenibgemcitabinecisplatin
02

Targets

DNA polymerase familyDNAIDH1 (Isocitrate dehydrogenase [NADP] cytoplasmic)

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