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Molecular Profile | KIT exon11 |
Therapy | Ripretinib |
Indication/Tumor Type | gastrointestinal stromal tumor |
Response Type | sensitive |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT exon11 | gastrointestinal stromal tumor | sensitive | Ripretinib | Phase II | Actionable | In a Phase II trial, second-line Qinlock (ripretinib) treatment demonstrated a favorable safety profile and resulted in similar median progression-free survival (mPFS) compared to Sutent (sunitinib) (10.3 vs 8.3 mo, HR=0.99, p=0.92) in patients with gastrointestinal stromal tumors previously treated with Gleevec (imatinib), longer mPFS (not reached vs 4.9 months, HR=0.46, p=0.03) was observed in patients harboring KIT exon 11 mutations (PMID: 37980854). | 37980854 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Ripretinib | Phase I | Actionable | In a Phase I trial, Qinlock (ripretinib) was well tolerated, resulted in an objective response in 11.3% (16/142, 16 partial responses) and stable disease in 61.3% (87/142) of patients with advanced gastrointestinal stromal tumor harboring KIT (n=135) or PDGFRA mutations (n=7), with a median progression-free survival of 5.6 months, 72.5% (103/142) of the patients harbored KIT exon 11 mutations (PMID: 32804590; NCT02571036). | 32804590 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Ripretinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Qinlock (ripretinib) inhibited Kit phosphorylation and proliferation of gastrointestinal stromal tumor cells harboring a KIT exon 11 deletion mutation in culture, and resulted in tumor regression in cell line xenograft models (PMID: 31085175). | 31085175 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Ripretinib | Guideline | Actionable | Qinlock (ripretinib) is included in guidelines as fourth-line or subsequent therapy for locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 11 mutations (PMID: 34560242; ESMO.org). | 34560242 detail... |
PubMed Id | Reference Title | Details |
---|---|---|
ESMO Clinical Practice Guidelines | Full reference... | |
(31085175) | Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants. | Full reference... |
(32804590) | Switch Control Inhibition of KIT and PDGFRA in Patients With Advanced Gastrointestinal Stromal Tumor: A Phase I Study of Ripretinib. | Full reference... |
(34560242) | Gastrointestinal stromal tumours: ESMO-EURACAN-GENTURIS Clinical Practice Guidelines for diagnosis, treatment and follow-up. | Full reference... |
(37980854) | Efficacy and safety of ripretinib vs. sunitinib in patients with advanced gastrointestinal stromal tumor previously treated with imatinib: A phase 2, multicenter, randomized, open-label study in China. | Full reference... |