Therapy Detail

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Therapy Name Ripretinib
Synonyms
Therapy Description

Qinlock (ripretinib) is a dual inhibitor of KIT and PDGFRa, resulting in growth inhibition and anti-tumor effects (PMID: 29439183, PMID: 31085175, PMID: 31201392). Qinlock (ripretinib) is FDA approved for use in patients with advanced gastrointestinal stromal tumor who received 3 or more prior kinase inhibitor therapies (FDA.gov)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Ripretinib Qinlock DCC-2618|DCC2618 KIT Inhibitor 57 PDGFR-alpha Inhibitor 9 Qinlock (ripretinib) is a dual inhibitor of KIT and PDGFRa, resulting in growth inhibition and anti-tumor effects (PMID: 29439183, PMID: 31085175, PMID: 31201392). Qinlock (ripretinib) is FDA approved for use in patients with advanced gastrointestinal stromal tumor who received 3 or more prior kinase inhibitor therapies (FDA.gov)

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KIT W557_K558del KIT V654G KIT D816H gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT W557_K558del and D816H progressed on sixth-line treatment with Qinlock (ripretinib) after 11.5 months and was found to have acquired KIT V654G in the metastatic lesion (PMID: 38408285). 38408285
KIT V560D Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT act mut skin melanoma sensitive Ripretinib Guideline Actionable Qinlock (ripretinib) is included in guidelines as second-line therapy for metastatic or unresectable cutaneous melanoma patients with KIT activating mutations (NCCN.org). detail...
KIT exon 11 del KIT A829P gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT A829P in culture (PMID: 38408285). 38408285
KIT mutant gastrointestinal stromal tumor predicted - sensitive Ripretinib Phase I Actionable In a Phase I trial, Qinlock (ripretinib) demonstrated preliminary safety and efficacy in patients with advanced solid tumors, including KIT-mutant gastrointestinal stromal tumor (GIST), with 1 patient harboring KIT exon 11 and 17 mutations demonstrating a partial response, and 7/7 KIT-mutant GIST patients demonstrating a partial metabolic response (EORTC-NCI-AACR 2016, Abs 7LBA). detail...
KIT mutant gastrointestinal stromal tumor predicted - 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 (exon 11, n=103; exon 9, n=26; other, n=6) or PDGFRA mutations (n=7), with a median progression-free survival of 5.6 months (PMID: 32804590; NCT02571036). 32804590
KIT A502_Y503dup KIT D816H Advanced Solid Tumor decreased response Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT D816H demonstrated a decreased response to treatment with Qinlock (ripretinib) compared to cells expressing KIT A502_Y503dup alone in culture (PMID: 32350132). 32350132
KIT V559D KIT V654A Advanced Solid Tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V559D and V654A were resistant to Qinlock (ripretinib) treatment in culture (PMID: 35194937). 35194937
KIT L576P melanoma predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, Qinlock (ripretinib) treatment resulted in a partial response in 3 of 4 patients with metastatic melanoma harboring KIT L576P (PMID: 35753087; NCT02571036). 35753087
KIT mutant melanoma predicted - sensitive Ripretinib Phase I Actionable In a Phase I trial, Qinlock (ripretinib) treatment demonstrated manageable safety and preliminary efficacy in patients with KIT-mutated melanoma, and led to an objective response rate of 23% (6/26, 1 complete and 5 partial responses), a median progression-free survival of 7.3 months, and a median duration of response of 9.1 months (PMID: 35753087; NCT02571036). 35753087
KIT D816Y mast cell neoplasm predicted - sensitive 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 A502_Y503dup KIT V654A Advanced Solid Tumor decreased response Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT V654A demonstrated a decreased response to treatment with Qinlock (ripretinib) compared to cells expressing KIT A502_Y503dup alone in culture (PMID: 32350132). 32350132
KIT exon 11 del KIT V654A KIT A829P gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT V654A and A829P demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT W557_K558del KIT T670I Advanced Solid Tumor decreased response Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Qinlock (ripretinib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). 32350132
KIT A502_Y503dup Advanced Solid Tumor sensitive 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 D820Y melanoma predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, Qinlock (ripretinib) treatment resulted in a complete response in a patient with metastatic melanoma harboring KIT D820Y (PMID: 35753087; NCT02571036). 35753087
KIT N560_Y574del KIT V654A gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT N560_Y574del and N822Y progressed on second-line treatment with Qinlock (ripretinib) after 1.5 months and was found to have lost KIT N822Y but acquired KIT V654A in the metastatic lesion (PMID: 38408285). 38408285
KIT exon 11 del 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 KIT exon 11 deletion, resulted in tumor regression in cell line xenograft models (PMID: 31085175). 31085175
KIT exon 11 del gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion in culture (PMID: 38408285). 38408285
KIT V560D KIT D816H Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D and KIT D816H demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT exon 11 del KIT V654A KIT D820A gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT V654A and D820A demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT Q556_V559delinsH KIT Y823D gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT Q556_V559delinsH and Y823D progressed on fourth-line treatment with Qinlock (ripretinib) after 22.1 months and was found to have acquired KIT Y646C in the metastatic lesion (PMID: 38408285). 38408285
KIT exon 11 del KIT T670I gastrointestinal stromal tumor predicted - resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT T670I demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT exon 11 del KIT T670I gastrointestinal stromal tumor predicted - resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT T670I demonstrated reduced response to growth inhibition by Qinlock (ripretinib) compared to cells harboring KIT exon 11 deletion alone in culture (PMID: 31085175). 31085175
KIT V560_Y578del KIT V654A gastrointestinal stromal tumor predicted - resistant Ripretinib Preclinical - Cell line xenograft Actionable In a preclinical study, Qinlock (ripretinib) resulted in slight decreases in cell viability and KIT signaling in a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del and KIT V654A in culture, but failed to suppress tumor growth in cell line xenograft models (PMID: 32350132). 32350132
KIT N655K Advanced Solid Tumor predicted - sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT N655K demonstrated some sensitivity to Qinlock (ripretinib) treatment in culture, but were less sensitive than cells expressing KIT W557_K558del (PMID: 33212994). 33212994
KIT W557_K558del KIT V654A KIT I748D gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT W557_K558del and T670E progressed on fifth-line treatment with Qinlock (ripretinib) after 12 months and was found to have lost T670E but acquired KIT V654A and I748D in the metastatic lesion (PMID: 38408285). 38408285
KIT exon 11 del KIT V654A KIT N822K gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT V654A and N822K demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT V560G KIT D816V mast cell neoplasm sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of mast cells harboring KIT D816V and KIT V560G in culture, and inhibited tumor growth in cell line xenograft models (PMID: 31085175). 31085175
KIT exon9 gastrointestinal stromal tumor predicted - 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 9 mutations (PMID: 34560242; ESMO.org). 34560242 detail...
KIT exon9 gastrointestinal stromal tumor predicted - 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, 18.3% (26/142) of the patients harbored KIT exon 9 mutations (PMID: 32804590; NCT02571036). 32804590
KIT V560_Y578del gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited cell growth and KIT signaling in a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del in culture, but was less potent compared to AZD3229 (PMID: 32350132). 32350132
KIT P551_E554delinsQ KIT S645_L647dup KIT D820Y gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT P551_E554delinsQ and D820Y progressed on third-line treatment with Qinlock (ripretinib) after 29 months and was found to have acquired KIT S645_L647dup (reported as L647_G648insSYL) in the metastatic lesion (PMID: 38408285). 38408285
KIT W557_K558del KIT Y823D Advanced Solid Tumor decreased response Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT Y823D demonstrated a decreased response to treatment with Qinlock (ripretinib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). 32350132
KIT Y823D melanoma predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, Qinlock (ripretinib) treatment resulted in a complete response in a patient with metastatic melanoma harboring KIT Y823D (PMID: 35753087; NCT02571036). 35753087
KIT V559D KIT T670I Advanced Solid Tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V559D and T670I were resistant to Qinlock (ripretinib) treatment in culture (PMID: 35194937). 35194937
KIT W557_K558del Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) treatment resulted in decreased viability of transformed cells expressing KIT W557_K558del in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132). 32350132
KIT V560D KIT D820A Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D and KIT D820A demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT T670E Advanced Solid Tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT T670E demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 35194937). 35194937
KIT A502_Y503dup KIT N822K gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT A502_Y503dup and expressing KIT N822K in culture (PMID: 38408285). 38408285
KIT K642E KIT N822Y gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT N822Y progressed on sixth-line treatment with Qinlock (ripretinib) after 7.3 months and was found to have acquired KIT K642E in the metastatic lesion (PMID: 38408285). 38408285
KIT W557_K558del KIT V654A gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT W557_K558del progressed on second-line treatment with Qinlock (ripretinib) after 3 months and was found to have acquired KIT V654A in the metastatic lesion (PMID: 38408285). 38408285
KIT V560D KIT V654A Advanced Solid Tumor decreased response Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D and KIT V654A demonstrated a decreased response to treatment with Qinlock (ripretinib) compared to cells expressing KIT V560D alone in culture (PMID: 32350132). 32350132
KIT exon 11 del KIT V654A gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT V654A demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT exon 11 del KIT D820A gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT D820A in culture (PMID: 38408285). 38408285
KIT V559_G565del KIT V654A KIT A829P gastrointestinal stromal tumor predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, treatment with Qinlock (ripretinib) decreased circulating tumor DNA, resulted in stable disease lasting over 26 months in a patient with gastrointestinal stromal tumor harboring a primary KIT V559_G565del mutation and two acquired resistance mutations, KIT V654A and KIT A829P (PMID: 31085175; NCT02571036). 31085175
KIT V559_E561del KIT T670I gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT V559_E561del and KIT D820Y progressed on third-line treatment with Qinlock (ripretinib) after 2.5 months and was found to have lost KIT D820Y but acquired KIT T670I in the metastatic lesion (PMID: 38408285). 38408285
KIT N822K acute myeloid leukemia sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). 31085175
KIT N822K acute myeloid leukemia sensitive Ripretinib Preclinical - Pdx Actionable In a preclinical study, Qinlock (ripretinib) induced tumor regression in a patient-derived xenograft (PDX) model of acute myeloid leukemia harboring KIT N822K (Cancer Res 2015;75(15 Suppl):Abstract nr 2690). detail...
KIT Y568_L576delinsCV KIT D816E KIT D820Y gastrointestinal stromal tumor predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, treatment with Qinlock (ripretinib) decreased circulating tumor DNA, resulted in stable disease lasting over 21 months in a patient with gastrointestinal stromal tumor harboring a primary KIT Y568_L576delinsCV mutation and two acquired resistance mutations, KIT D816E and KIT D820Y (PMID: 31085175; NCT02571036). 31085175
KIT W557_K558del KIT V654A KIT D820V gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT W557_K558del progressed on fourth-line treatment with Qinlock (ripretinib) after 3.0 months and was found to have acquired KIT V654A and D820V in the metastatic lesion (PMID: 38408285). 38408285
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 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...
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 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 W557_K558del KIT N822K Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT N822K demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT K550_K558del KIT V654A KIT A829P gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT K550_K558del and KIT A829P progressed on fifth-line treatment with Qinlock (ripretinib) after 8.0 months and was found to have acquired KIT V654A in the metastatic lesion (PMID: 38408285). 38408285
KIT Q556_V559delinsH KIT T670I gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT Q556_V559delinsH progressed on third-line treatment with Qinlock (ripretinib) after 5.0 months and was found to have acquired KIT T670I in the metastatic lesion (PMID: 38408285). 38408285
KIT V560D KIT D579G KIT D816N melanoma predicted - sensitive Ripretinib Case Reports/Case Series Actionable In a Phase I trial, Qinlock (ripretinib) treatment resulted in a partial response in a patient with metastatic melanoma harboring KIT D579G, V560D, and D816N (PMID: 35753087; NCT02571036). 35753087
KIT D816V Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of transformed cells expressing KIT D816V in culture (PMID: 31085175). 31085175
KIT exon 11 del KIT V654A KIT D816A gastrointestinal stromal tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT V654A and D816A demonstrated resistance to Qinlock (ripretinib) in culture (PMID: 38408285). 38408285
KIT W557_K558del KIT V654A Advanced Solid Tumor resistant Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) failed to reduce cell viability and inhibit KIT signaling in transformed cells expressing KIT W557_K558del and KIT V654A in culture (PMID: 32350132). 32350132
KIT exon 11 del KIT N822K gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT N822K in culture (PMID: 38408285). 38408285
KIT A502_Y503dup KIT T574_P577del KIT V654A KIT N822K gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT A502_Y503dup progressed on third-line treatment with Qinlock (ripretinib) after 7.0 months and was found to have acquired KIT T574_P577del (reported as P573_L576del), V654A, and N822K in one of the metastatic lesions (PMID: 38408285). 38408285
KIT exon 11 del KIT D816A gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT D816A in culture (PMID: 38408285). 38408285
KIT V560G mast cell neoplasm sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of mast cells harboring KIT V560G in culture (PMID: 31085175). 31085175
KIT W557_K558del KIT A829P Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT A829P demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT A502_Y503dup gastrointestinal stromal tumor resistant 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 K558_V559delinsN KIT T670E gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, KIT K558_V559delinsN and T670E were identified in a post-progression biopsy of a patient with a gastrointestinal stromal tumor who had been on third-line treatment with Qinlock (ripretinib) for 5.1 months (PMID: 38408285). 38408285
KIT W557_K558del KIT D820A Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT D820A demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT exon 11 del KIT D820Y gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT D820Y in culture (PMID: 38408285). 38408285
KIT K550_V555del KIT V654A KIT C809G gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT K550_V555del progressed on sixth-line treatment with Qinlock (ripretinib) after 18 months and was found to have acquired KIT K550_V555del and V654A KIT C809G in one metastatic lesion and KIT V654A in a second metastatic lesion (PMID: 38408285). 38408285
KIT exon 11 del KIT C809G gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT C809G in culture (PMID: 38408285). 38408285
KIT Q556_K558delinsE KIT V654A KIT Y823H gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT Q556_K558delinsE and KIT V654A progressed on fourth-line treatment with Qinlock (ripretinib) after 8.5 months and was found to have acquired KIT Y823H in the metastatic lesion (PMID: 38408285). 38408285
KIT W557_K558del KIT D816H Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT D816H demonstrated sensitivity to Qinlock (ripretinib) in culture, resulting in reduced cell viability (PMID: 32350132). 32350132
KIT W557_K558del KIT Y823D gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Pdx Actionable In a preclinical study, Qinlock (ripretinib) induced tumor regression in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and KIT Y823D (PMID: 31085175). 31085175
KIT exon 11 del KIT D816E gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT D816E in culture (PMID: 31085175). 31085175
KIT exon 11 del KIT D816E gastrointestinal stromal tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited viability of a gastrointestinal stromal tumor cell line harboring a KIT exon 11 deletion and expressing KIT D816E in culture (PMID: 38408285). 38408285
KIT M552_E554delinsK KIT V654A gastrointestinal stromal tumor predicted - resistant Ripretinib Case Reports/Case Series Actionable In a retrospective study, a patient with a gastrointestinal stromal tumor harboring KIT M552_E554delinsK progressed on second-line treatment with Qinlock (ripretinib) after 2.5 months and was found to have acquired KIT V654A in the metastatic lesion (PMID: 38408285). 38408285

Filtering

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  • Use simple literal full or partial string matches
  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03673501 Phase III Sunitinib Ripretinib A Study of DCC-2618 vs Sunitinib in Advanced GIST Patients After Treatment With Imatinib (intrigue) Active, not recruiting USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS 12
NCT02571036 Phase I Ripretinib A Safety, Tolerability and PK Study of DCC-2618 in Patients With Advanced Malignancies Completed USA | NLD | ITA | GBR | DEU | CAN 0
NCT05734105 Phase III Ripretinib Sunitinib A Study of Ripretinib vs Sunitinib in Patients With Advanced GIST With Specific KIT Exon Mutations Who Were Previously Treated With Imatinib (INSIGHT) Recruiting USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | AUS 5
NCT03353753 Phase III Ripretinib Phase 3 Study of DCC-2618 vs Placebo in Advanced GIST Patients Who Have Been Treated With Prior Anticancer Therapies (invictus) Completed USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS 3


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