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, Helen R. Josephine, Marie Katz, Mark T. Kershaw, Lili Yao, Angela V. Toms, Kenneth J. Barr, Christopher J. Dinsmore, Duncan Walker, Susan Ashwell, Wei Lu
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.
Topics & Concepts
ADMEChemistryBioavailabilityMutantLead compoundPharmacologyIDH1In silicoBiochemistryIn vitroMedicineGeneGlioma Diagnosis and TreatmentCancer, Hypoxia, and MetabolismHistone Deacetylase Inhibitors Research