Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue 4, Pages 1612-1623Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01423
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Funding
- Forma Therapeutics, Inc.
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Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe the structure-based design and optimization of quinoline lead compounds to identify FT-2102, a potent, orally bioavailable, brain penetrant, and selective mIDH1 inhibitor. FT-2102 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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