Therapy Detail

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Therapy Name Ripretinib
Synonyms
Therapy Description

Ripretinib (DCC-2618) is a dual inhibitor of KIT and PDGFRa, resulting in growth inhibition and anti-tumor effects (PMID: 29439183, PMID: 31085175, PMID: 31201392).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Ripretinib Qinlock DCC-2618|DCC2618 KIT Inhibitor 50 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 amp PDGFRA amp glioblastoma multiforme sensitive Ripretinib Phase I Actionable In a Phase I trial, Qinlock (ripretinib) demonstrated preliminary safety and efficacy in patients with advanced solid tumors, including a partial response in a glioblastoma multiforme patient harboring KIT and PDGFRA amplification (EORTC-NCI-AACR 2016, Abs 7LBA). detail...
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
PDGFRA D842V Advanced Solid Tumor sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of transformed cells expressing PDGFRA D842V in culture (PMID: 31085175). 31085175
Unknown unknown gastrointestinal stromal tumor not applicable Ripretinib FDA approved Actionable In a Phase III trial (INVICTUS) that supported FDA approval, Qinlock (ripretinib) treatment significantly improved median progression-free survival (6.3 vs 1 mo, HR=0.15, p<0.0001) and median overall survival (15.1 vs 6.6 mo, HR=0.36, p=0.0004) compared to placebo in patients with advanced gastrointestinal stromal tumor who have received 3 or more prior kinase inhibitor therapies (PMID: 32511981; NCT03353753). 32511981 detail...
Unknown unknown gastrointestinal stromal tumor not applicable Ripretinib Phase I Actionable In a Phase I study, Qinlock (ripretinib) treatment resulted in an overall response rate of 16% (16/99) in patients with drug resistant gastrointestinal stromal tumors, 71% (55/77) of analyzed patients harbored baseline KIT or PDGFRA activating mutations (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11511-11511; NCT02571036). detail...
KIT D816Y mast cell neoplasm predicted - sensitive 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 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 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 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 exon 11 del KIT T670I gastrointestinal stromal tumor decreased response 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 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 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 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 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 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 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 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
PDGFRA amp lung cancer sensitive Ripretinib Preclinical - Cell culture Actionable In a preclinical study, Qinlock (ripretinib) inhibited proliferation of lung cancer cells harboring PDGFRA amplification in culture, and resulted in tumor regression in cell line xenograft models (PMID: 31085175). 31085175
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

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Clinical Trial Phase Therapies Title Recruitment Status
NCT03673501 Phase III Sunitinib Ripretinib A Study of DCC-2618 vs Sunitinib in Advanced GIST Patients After Treatment With Imatinib (intrigue) Recruiting
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) Active, not recruiting
NCT02571036 Phase I Ripretinib A Safety, Tolerability and PK Study of DCC-2618 in Patients With Advanced Malignancies Recruiting


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