Molecular Profile Detail

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Profile Name	KIT A502_Y503dup
Gene Variant Detail	KIT A502_Y503dup (gain of function)
Relevant Treatment Approaches	KIT Inhibitor

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Showing 1 to 19 of 19 entries

Molecular Profile	Indication/Tumor Type	Response Type	Relevant Treatment Approaches	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
KIT A502_Y503dup	gastrointestinal stromal tumor	predicted - sensitive	KIT Inhibitor	Binimetinib + Imatinib	Case Reports/Case Series	Actionable	In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment resulted in a 90% pathological response and 27% RECIST response in the primary tumor and 100% pathological response in metastatic lesions of a patient with an esophageal gastrointestinal stromal tumor harboring KIT A502_Y503dup (PMID: 35041493; NCT01991379).	35041493
KIT A502_Y503dup	gastrointestinal stromal tumor	conflicting	KIT Inhibitor	Imatinib	Preclinical - Pdx	Actionable	In a preclinical study, a gastrointestinal stromal tumor patient-derived xenograft (PDX) model harboring KIT A502_Y503dup demonstrated resistance to treatment with Gleevec (imatinib), resulting in increased tumor volume (PMID: 27777285).	27777285
KIT A502_Y503dup	gastrointestinal stromal tumor	sensitive	KIT Inhibitor	Cabozantinib	Preclinical - Pdx	Actionable	In a preclinical study, Cometriq (Cabometyx, cabozantinib) resulted in decreased tumor volume and reduced mitotic activity in a gastrointestinal stromal tumor patient derived xenograft (PDX) model harboring KIT A502_Y503dup (PMID: 27777285).	27777285
KIT A502_Y503dup	gastrointestinal stromal tumor	predicted - sensitive	KIT Inhibitor	Regorafenib	Preclinical - Pdx	Actionable	In a preclinical study, Stivarga (regorafenib) did not significantly inhibit Kit, Erk, or Mtor signaling, but resulted in tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup and KIT D820E, which was established from a patient who did not respond to Gleevec (imatinib mesylate) and Sutent (sunitinib) (PMID: 29100343).	29100343
KIT A502_Y503dup	gastrointestinal stromal tumor	sensitive	KIT Inhibitor	Avapritinib	Preclinical - Pdx	Actionable	In a preclinical study, a patient derived xenograft (PDX) model with a gastrointestinal stromal tumor harboring KIT A502_Y503dup was sensitive to treatment with Ayvakit (avapritinib), demonstrating a 90% stabilized tumor volume at a dose of 30mg/kg and tumor regression at a dose of 60mg/kg, and inhibition of cell proliferation (PMID: 30274985).	30274985
KIT A502_Y503dup	gastrointestinal stromal tumor	predicted - sensitive	KIT Inhibitor	IDRX-42	Preclinical - Pdx	Actionable	In a preclinical study, IDRX-42 treatment inhibited mitosis and decreased tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup (Cancer Res 2022;82(12_Suppl):Abstract nr 2666).	detail...
KIT A502_Y503dup	gastrointestinal stromal tumor	conflicting	KIT Inhibitor	Imatinib	Preclinical - Pdx	Actionable	In a preclinical study, Gleevec (imatinib) treatment stabilized tumor growth in a gastrointestinal stromal tumor patient-derived xenograft (PDX) model harboring KIT A502_Y503dup (PMID: 35625872).	35625872
KIT A502_Y503dup	gastrointestinal stromal tumor	predicted - sensitive	KIT Inhibitor	Binimetinib + Dovitinib	Preclinical - Pdx	Actionable	In preclinical study, combination treatment with Mektovi (binimetinib) and Dovitinib (TKI258) resulted in tumor shrinkage in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup (PMID: 35625872).	35625872
KIT A502_Y503dup	gastrointestinal stromal tumor	predicted - sensitive	KIT Inhibitor	Dovitinib	Preclinical - Pdx	Actionable	In preclinical study, Dovitinib (TKI258) treatment resulted in tumor shrinkage in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup (PMID: 35625872).	35625872
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	Imatinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT A502_Y503dup (Y503_F504insAY) were sensitive to Gleevec (imatinib) in culture, demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	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 A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	Sunitinib	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT A502_Y503dup (Y503_F504insAY) were sensitive to Sutent (sunitinib) in culture, demonstrating decreased cell proliferation (PMID: 24205792).	24205792
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	AZD3229	Preclinical - Cell culture	Actionable	In a preclinical study, transformed cells expressing KIT A502_Y503dup demonstrated sensitivity to AZD3229 in culture, resulting in reduced cell viability and inhibition of KIT signaling (PMID: 32350132).	32350132
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	Regorafenib	Preclinical - Cell culture	Actionable	In a preclinical study, Stivarga (regorafenib) treatment resulted in decreased viability of transformed cells expressing KIT A502_Y503dup in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132).	32350132
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	Avapritinib	Preclinical - Cell culture	Actionable	In a preclinical study, Ayvakit (avapritinib) treatment resulted in decreased cell viability and reduced KIT signaling in transformed cells expressing KIT A502_Y503dup in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132).	32350132
KIT A502_Y503dup	Advanced Solid Tumor	sensitive	KIT Inhibitor	Ripretinib	Preclinical - Cell culture	Actionable	In a preclinical study, Qinlock (ripretinib) treatment resulted in decreased cell viability and reduced KIT signaling in transformed cells expressing KIT A502_Y503dup in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132).	32350132
KIT A502_Y503dup	gastrointestinal stromal tumor	resistant	KIT Inhibitor	Ripretinib	Preclinical - Cell culture	Actionable	In a preclinical study, a gastrointestinal stromal tumor cell line expressing KIT A502_Y503dup demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285).	38408285
KIT A502_Y503dup	gastrointestinal stromal tumor	sensitive	KIT Inhibitor	Sunitinib	Preclinical - Cell culture	Actionable	In a preclinical study, Sutent (sunitinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT A502_Y503dup in culture (PMID: 38408285).	38408285
KIT A502_Y503dup	gastrointestinal stromal tumor	sensitive		Nintedanib	Preclinical - Cell culture	Actionable	In a preclinical study, Ofev (nintedanib) inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT A502_Y503dup in culture (PMID: 38408285).	38408285

Showing 1 to 19 of 19 entries

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