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Ref Type
Authors Cong Li, Lingming Liang, Liqin Liu, Zhen Xia, Zhihong Li, Xianghong Wang, Lawrence McGee, Angus Sinclair, Sasha Kamb, Dineli Wickramasinghe, Sachie Marubayashi, Juan C. Jaen, Jordan S. Fridman, and Kang Dai
Title Abstract 787: FLX925 (AMG 925) is a rationally designed FLT3, CDK4/6 inhibitor that retains potency against clinically relevant secondary resistance mutations in FLT3
Journal Cancer Research
Abstract Text Cancer Res August 1, 2015 75; 787


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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
FLX925 FLX925 1 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
FLX925 AMG925|AMG-925|AMG 925 CDK4/6 Inhibitor 12 FLT3 Inhibitor 61 FLX925 (AMG925) binds to and inhibits both FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinases 4 and 6 (CDK4/6), resulting in cell cycle arrest and inhibition of cell proliferation (Cancer Res 2015;75(15 Suppl):Abstract nr 787, PMID: 25326874).
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
FLT3 Y599_D600insSTDNEYFYVDFREYEY acute myeloid leukemia predicted - sensitive FLX925 Preclinical Actionable In a preclinical study, acute myeloid leukemia cells harboring a FLT3-ITD secondary resistance mutation demonstrated sensitivity to FLX925 (Cancer Res, August 1, 2015 75; 787). detail...