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Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.

Abstract：

:Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain of function in cancer cells, resulting in the production of d-2-hydroxyglutarate (2-HG), an oncometabolite. Elevated 2-HG levels are implicated in epigenetic alterations and impaired cellular differentiation. IDH1 mutations have been described in an array of hematologic malignancies and solid tumors. Here, we report the discovery of AG-120 (ivosidenib), an inhibitor of the IDH1 mutant enzyme that exhibits profound 2-HG lowering in tumor models and the ability to effect differentiation of primary patient AML samples ex vivo. Preliminary data from phase 1 clinical trials enrolling patients with cancers harboring an IDH1 mutation indicate that AG-120 has an acceptable safety profile and clinical activity.

journal_name

ACS Med Chem Lett

journal_title

ACS medicinal chemistry letters

authors

Popovici-Muller J,Lemieux RM,Artin E,Saunders JO,Salituro FG,Travins J,Cianchetta G,Cai Z,Zhou D,Cui D,Chen P,Straley K,Tobin E,Wang F,David MD,Penard-Lacronique V,Quivoron C,Saada V,de Botton S,Gross S,Dang L,Y

doi

10.1021/acsmedchemlett.7b00421

subject

Has Abstract

pub_date

2018-01-19 00:00:00

pages

300-305

issue

4

issn

1948-5875

journal_volume

9

pub_type

杂志文章

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