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Profile Name | KIT exon11 |
Gene Variant Detail | |
Relevant Treatment Approaches |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT exon11 KIT A829P | gastrointestinal stromal tumor | sensitive | Imatinib + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Gleevec (imatinib) and MK2206 demonstrated synergy in inhibiting growth of a Gleevec (imatinib)-resistant gastrointestinal stromal tumor cell line harboring a KIT exon 11 mutation and KIT A829P in culture (PMID: 27370604). | 27370604 |
KIT exon11 KIT V654A | gastrointestinal stromal tumor | sensitive | Imatinib + MK2206 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Gleevec (imatinib) and MK2206 demonstrated synergy in inhibiting growth of a Gleevec (imatinib)-resistant gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion mutation and KIT V654A in culture (PMID: 27370604). | 27370604 |
KIT exon11 KIT T670I | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib mesylate) did not inhibit Kit, Erk signaling and resulted in limited (53.9%) tumor inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT exon 11 mutation (K550_splice) and KIT T670I, which was established from a patient who did not respond to Gleevec (imatinib mesylate) (PMID: 29100343). | 29100343 |
KIT exon11 KIT T670I | gastrointestinal stromal tumor | predicted - sensitive | Sunitinib | Preclinical - Pdx | Actionable | In a preclinical study, Sutent (sunitinib) inhibited Kit signaling, resulted in 86.7% tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT exon 11 mutation (K550_splice) and KIT T670I, which was established from a patient who did not respond to Gleevec (imatinib mesylate) (PMID: 29100343). | 29100343 |
KIT exon11 KIT T670I | gastrointestinal stromal tumor | predicted - sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Kit signaling, resulted in tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT exon 11 mutation (K550_splice) and KIT T670I, which was established from a patient who did not respond to Gleevec (imatinib mesylate) (PMID: 29100343). | 29100343 |
KIT exon11 KIT exon17 | gastrointestinal stromal tumor | predicted - sensitive | PLX9486 | Phase I | Actionable | In a Phase I trial, PLX9486 treatment resulted in partial response with 33% decrease of tumor size after 4 cycles of therapy in a patient with gastrointestinal stromal tumor harboring a primary KIT exon 11 mutation and a secondary KIT exon 17 mutation, who progressed on prior Gleevec (imatinib mesylate) and Sutent (sunitinib) therapies (CTOS Annual Meeting, Nov 2017, abstract # 2771952). | detail... |
KIT exon11 KIT V654A | gastrointestinal stromal tumor | sensitive | Copanlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Aliqopa (copanlisib) inhibited cell growth and PI3K signaling in a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and KIT V654A in culture (PMID: 32371592). | 32371592 |
KIT exon11 KIT V654A | gastrointestinal stromal tumor | predicted - sensitive | Copanlisib + Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Aliqopa (copanlisib) and Gleevec (imatinib) demonstrated enhanced cell growth inhibition but did not result in increased apoptosis of gastrointestinal stromal tumor cells harboring a KIT exon 11 deletion and KIT V654A compared to either agent alone in culture (PMID: 32371592). | 32371592 |
KIT exon11 KIT exon13 | gastrointestinal stromal tumor | predicted - sensitive | DCC-3009 | Preclinical | Actionable | In a preclinical study, DCC-3009 induced tumor regression in a xenograft model of gastrointestinal stromal tumor harboring KIT exon 11 and exon 13 mutations (Cancer Res (2023) 83 (7_Supplement): 4033). | detail... |
KIT exon11 KIT exon17 | gastrointestinal stromal tumor | predicted - sensitive | DCC-3009 | Preclinical | Actionable | In a preclinical study, DCC-3009 induced tumor regression in a xenograft model of gastrointestinal stromal tumor harboring KIT exon 11 and exon 17 mutations (Cancer Res (2023) 83 (7_Supplement): 4033). | detail... |