Molecular Profile Detail

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Profile Name KIT D816Y
Gene Variant Detail

KIT D816Y (gain of function)

Relevant Treatment Approaches KIT Inhibitor Avapritinib

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
KIT D816Y Advanced Solid Tumor resistant KIT Inhibitor Imatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816Y were resistant to Gleevec (imatinib mesylate) in culture (PMID: 16397263). 16397263
KIT D816Y Advanced Solid Tumor resistant KIT Inhibitor Imatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816Y were resistant to treatment with Gleevec (imatinib) in culture (PMID: 24205792). 24205792
KIT D816Y mast cell neoplasm predicted - sensitive KIT Inhibitor Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of a mouse mastocytosis cell line expressing KIT K816Y in culture (Cancer Res 2015;75(15 Suppl):Abstract nr 2690). detail...
KIT D816Y mast cell neoplasm predicted - sensitive KIT Inhibitor Ripretinib Preclinical Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) in culture, and resulted in tumor growth inhibition in allograft models (PMID: 31085175). 31085175
KIT D816Y mast cell neoplasm predicted - resistant KIT Inhibitor Imatinib Preclinical - Cell culture Actionable In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) were resistant to Gleevec (imatinib) in culture (PMID: 31085175). 31085175
KIT D816Y mast cell neoplasm decreased response KIT Inhibitor Sunitinib Preclinical - Cell culture Actionable In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) demonstrated reduced response to growth inhibition by Sutent (sunitinib) compared to GIST cells harboring KIT exon 11 deletion in culture (PMID: 31085175). 31085175
KIT D816Y mast cell neoplasm predicted - sensitive Avapritinib KIT Inhibitor Avapritinib Preclinical Actionable In a preclinical study, Ayvakit (avapritinib) inhibited Kit phosphorylation and proliferation of murine mastocytoma cells harboring KIT D814Y (corresponding to human D816Y) in culture, and resulted in tumor regression in allograft animal models (PMID: 29093181). 29093181
KIT D816Y Advanced Solid Tumor resistant KIT Inhibitor Sunitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816Y were resistant to treatment with Sutent (sunitinib) in culture (PMID: 24205792). 24205792
KIT D816Y mast cell neoplasm predicted - sensitive KIT Inhibitor Midostaurin Preclinical - Cell culture Actionable In a preclinical study, Rydapt (midostaurin) inhibited proliferation of mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) in culture (PMID: 31085175). 31085175
KIT D816Y mast cell neoplasm predicted - resistant KIT Inhibitor Regorafenib Preclinical - Cell culture Actionable In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). 31085175
KIT D816Y Advanced Solid Tumor resistant KIT Inhibitor 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
Clinical Trial Phase Therapies Title Recruitment Status