Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor

Justin A. Caravella, Jian Lin, R. Bruce Diebold, Ann-Marie Campbell, Anna Ericsson, Gary Gustafson, Zhongguo Wang, Jennifer Castro, Andrea Clarke, Deepali Gotur,

Journal of Medicinal Chemistry · 2020 · 144 citations · 29 references

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Abstract

has excellent ADME/PK properties and reduces 2-hydroxyglutarate levels in an mIDH1 xenograft tumor model. This compound has been selected as a candidate for clinical development in hematologic malignancies, solid tumors, and gliomas with mIDH1.

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