Therapy Detail

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Therapy Name	Flumatinib
Synonyms
Therapy Description	Flumatinib (HH-GV678) inhibits KIT, PDGFR, and BCR-ABL, potentially resulting in decreased tumor cell proliferation (PMID: 24205792, PMID: 31699612).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
Flumatinib		HH-GV678	BCR-ABL Inhibitor 32 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30	Flumatinib (HH-GV678) inhibits KIT, PDGFR, and BCR-ABL, potentially resulting in decreased tumor cell proliferation (PMID: 24205792, PMID: 31699612).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT A502_Y503dup (Y503_F504insAY) were sensitive to Flumatinib in culture, demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT D816H	Advanced Solid Tumor	predicted - sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT D816H were more sensitive to treatment with Flumatinib in culture compared to Gleevec (imatinib) (PMID: 24205792).	24205792
KIT D816V	Advanced Solid Tumor	resistant	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT D816V were resistant to treatment with Flumatinib in culture (PMID: 24205792).	24205792
KIT D816Y	Advanced Solid Tumor	resistant	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT D816Y were resistant to treatment with Flumatinib in culture (PMID: 24205792).	24205792
KIT I571_D579dup	Advanced Solid Tumor	predicted - resistant	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT I571_D579dup (KIT D579_H580insIDPTQLPYD) were moderately resistant to Flumatinib in culture (PMID: 24205792).	24205792
KIT N822K	Advanced Solid Tumor	predicted - sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT N822K were more sensitive to treatment with Flumatinib in culture compared to Gleevec (imatinib), demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT T417_D419delinsI	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT T417_D419delinsI were sensitive to treatment with Flumatinib, demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT V559_V560del	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT V559_V560del were sensitive to Flumatinib, demonstrating decreased cell proliferation in culture (PMID: 24205792).	24205792
KIT V559D	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT V559D were sensitive to Flumatinib, demonstrating decreased cell proliferation in culture and inhibition of Kit, Erk1/2, and Stat3 phosphorylation (PMID: 24205792).	24205792
KIT V559D KIT A829P	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells co-expressing KIT A829P and KIT V559D were sensitive to Flumatinib in culture, demonstrating decreased cell proliferation and inhibition of Kit, Erk1/2, and Stat3 phosphorylation (PMID: 24205792).	24205792
KIT V559D KIT D820G	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells co-expressing KIT D820G and KIT V559D were sensitive to Flumatinib in culture, demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT V559D KIT N822K	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells co-expressing KIT N822K and KIT V559D were sensitive to Flumatinib in culture, demonstrating decreased cell proliferation and inhibition of Kit, Erk 1/2, and Stat3 phosphorylation (PMID: 24205792).	24205792
KIT V560D KIT T670I	Advanced Solid Tumor	resistant	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells co-expressing KIT V560D and KIT T670I were resistant to Flumatinib in culture (PMID: 24205792).	24205792
KIT V560D KIT V654A	Advanced Solid Tumor	resistant	Flumatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells co-expressing KIT V560D and KIT V654A were resistant to Flumatinib in culture (PMID: 24205792).	24205792
KIT V559D KIT Y823D	Advanced Solid Tumor	sensitive	Flumatinib	Preclinical	Actionable	In a preclinical study, Flumatinib treatment in transformed cells co-expressing KIT Y823D and KIT V559D resulted in decreased cell proliferation and inhibition of Kit, Erk1/2, and Stat3 phosphorylation in culture, and led to improved survival in mouse models (PMID: 24205792).	24205792

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