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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) | ||||||||||||
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URL | https://www.abstractsonline.com/pp8/#!/6812/presentation/9182 | ||||||||||||
Abstract Text | AACR Annual Meeting 2019, Abstract LB-274 |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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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... |