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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 | ||||||||||||
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URL | http://cancerres.aacrjournals.org/content/75/15_Supplement/787.short | ||||||||||||
Abstract Text | Cancer Res August 1, 2015 75; 787 |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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FLX925 | AMG925|AMG-925|AMG 925 | CDK4/6 Inhibitor 14 FLT3 Inhibitor 69 | 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 |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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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... |