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PMID
Authors N Brooks, R DeWalt, S Boulet, ZH Lu, L Kays, R cavitt, S Gomez, J Strelow, P Milligan, K Roth, R Bauer, S Antonysamy, P Hahn, Z Rankovic, D McCann, G Mo, R Tiu, T Burkholder, S Geeganage, R Gilmour
Title Identification and characterization of LY3410738, a novel covalent inhibitor of cancer-associated mutant Isocitrate Dehydrogenase 1 (IDH1)
Journal AACR Annual Meeting Online Proceedings
Vol
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Date
URL https://www.abstractsonline.com/pp8/#!/6812/presentation/9182
Abstract Text AACR Annual Meeting 2019, Abstract LB-274

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
LY3410738 LY3410738 1 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
LY3410738 LY-3410738|LY 3410738 IDH1 Inhibitor 8 LY3410738 is a covalent inhibitor of mutant IDH1, which may lead to anti-tumor activity in IDH1-mutant tumors (AACR Annual Meeting 2019, Abstract LB-274).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
IDH1 mutant acute myeloid leukemia predicted - sensitive LY3410738 Preclinical - Pdx & cell culture Actionable In a preclinical study, LY3410738 reversed mutant IDH1-induced differentiation block in patient-derived acute myeloid leukemia (AML) cells, inhibited 2-HG production, induced differentiation, and eliminated AML cells in patient-derived orthotopic animal models of IDH1-mutant AML (AACR 2019 Annual Meeting, Abstract LB-274). detail...