Synonyms: AG-120 | AG120 | Tibsovo®
ivosidenib is an approved drug (FDA (2018), EMA (2023))
Compound class:
Synthetic organic
Comment: Ivosidenib (AG-120) is an orally active, selective inhibitor of isocitrate dehydrogenase 1 (IDH1) [5], in particular with activity against IDH1 R132H or R132C mutants. It is one of the compounds claimed in Agios' patent WO2013107291, where it is Compound 176 [4]. It is structurally related to AGI-5198 also from Agios.
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References |
1. Birendra KC, DiNardo CD. (2016)
Evidence for Clinical Differentiation and Differentiation Syndrome in Patients With Acute Myeloid Leukemia and IDH1 Mutations Treated With the Targeted Mutant IDH1 Inhibitor, AG-120. Clin Lymphoma Myeloma Leuk, 16 (8): 460-5. [PMID:27245312] |
2. Dang L, White DW, Gross S, Bennett BD, Bittinger MA, Driggers EM, Fantin VR, Jang HG, Jin S, Keenan MC et al.. (2009)
Cancer-associated IDH1 mutations produce 2-hydroxyglutarate. Nature, 462 (7274): 739-44. [PMID:19935646] |
3. DiNardo CD, Stein EM, de Botton S, Roboz GJ, Altman JK, Mims AS, Swords R, Collins RH, Mannis GN, Pollyea DA et al.. (2018)
Durable Remissions with Ivosidenib in IDH1-Mutated Relapsed or Refractory AML. N Engl J Med, 378 (25): 2386-2398. [PMID:29860938] |
4. Lemieux RM, Popovici-Muller J, Travins J, Cai Z, Cui D, Zhou D. (2013)
Therapeutically active compounds and their methods of use. Patent number: WO2013107291. Assignee: Agios Pharmaceuticals, Inc.. Priority date: 19/01/2012. Publication date: 25/07/2013. |
5. Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D et al.. (2018)
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers. ACS Med Chem Lett, 9 (4): 300-305. [PMID:29670690] |