{"entity":{"id":"ripretinib","kind":"drug","name":"Ripretinib","aka":[],"tldr":"A fourth-line GIST drug that locks KIT in an off state regardless of which resistance mutation the tumour has acquired.","summary":"INVICTUS: PFS 6.3 vs 1.0 months vs placebo (HR 0.15), OS HR 0.36; approved May 2020 after ≥3 TKIs. INTRIGUE (second line vs sunitinib) not superior overall but superior in KIT exon 11 + 17/18 mutations, prompting INSIGHT (ctDNA-selected phase 3, positive on PFS 2025-26 per interim reports). Deciphera/Ono.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Ripretinib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Ripretinib"}],"tags":[],"related":[],"cancers":["sarcoma","gist-imatinib-resistant"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["kit"],"drugs":[],"companies":["deciphera"],"institutions":[],"pathways":[],"terms":[],"trials":["invictus","insight-gist","nct03673501"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Qinlock","modality":"Small-molecule kinase inhibitor (KIT/PDGFRA switch-control)","mechanism":"Binds the switch pocket and activation loop of KIT/PDGFRA, inhibiting primary and secondary mutations (exons 9, 11, 13, 14, 17, 18).","approvals":[{"region":"US","year":2020,"indication":"Advanced GIST after ≥3 prior kinase inhibitors including imatinib"}],"mechanismSteps":[],"dosing":{"route":"Oral","schedule":"150 mg once daily; 150 mg twice daily on progression","monitoring":"Skin exams (new cutaneous SCC), hypertension, cardiac function, palmar-plantar erythrodysaesthesia"},"toxicity":[{"event":"Alopecia","anyGradePct":52,"note":"INVICTUS"},{"event":"Palmar-plantar erythrodysaesthesia","anyGradePct":21},{"event":"Hypertension","grade3PlusPct":4},{"event":"Cutaneous squamous cell carcinoma","anyGradePct":4.7}],"access":[],"regulatoryEvents":[{"date":"2020-05-15","type":"approval","region":"US","note":"INVICTUS"},{"date":"2022-05","type":"label-change","region":"US","note":"Label updated with INTRIGUE data"}]},"route":"/drugs/ripretinib/","neighbours":{"cancer":[{"id":"gist","kind":"cancer","name":"Gastrointestinal stromal tumour (GIST)","route":"/cancers/gist/"},{"id":"gist-imatinib-resistant","kind":"cancer","name":"Imatinib-resistant GIST","route":"/cancers/gist-imatinib-resistant/"},{"id":"gist-kit-exon-11","kind":"cancer","name":"KIT exon 11-mutant GIST","route":"/cancers/gist-kit-exon-11/"},{"id":"sarcoma","kind":"cancer","name":"Sarcomas (soft tissue, bone, GIST)","route":"/cancers/sarcoma/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"kit","kind":"target","name":"KIT","route":"/targets/kit/"},{"id":"pdgfra","kind":"target","name":"PDGFRA","route":"/targets/pdgfra/"}],"company":[{"id":"deciphera","kind":"company","name":"Deciphera Pharmaceuticals (Ono)","route":"/companies/deciphera/"}],"trial":[{"id":"nct05957367","kind":"trial","name":"A Study of Inlexisertib (DCC-3116) in Combination With Anticancer Therapies in Participants With Advanced Malignancies","route":"/trials/nct05957367/"},{"id":"nct03673501","kind":"trial","name":"A Study of Ripretinib vs Sunitinib in Advanced GIST Patients After Treatment With Imatinib","route":"/trials/nct03673501/"},{"id":"insight-gist","kind":"trial","name":"INSIGHT","route":"/trials/insight-gist/"},{"id":"invictus","kind":"trial","name":"INVICTUS","route":"/trials/invictus/"}],"pairing":[{"id":"ctdna-genotype-gist-tki","kind":"pairing","name":"ctDNA KIT genotyping → TKI selection in GIST","route":"/pairings/ctdna-genotype-gist-tki/"}],"paper":[{"id":"paper-intrigue-ripretinib-vs-sunitinib-jco-2022","kind":"paper","name":"INTRIGUE: ripretinib versus sunitinib in advanced gastrointestinal stromal tumour after imatinib","route":"/key-papers/paper-intrigue-ripretinib-vs-sunitinib-jco-2022/"},{"id":"paper-invictus-ripretinib-lancet-oncol-2020","kind":"paper","name":"INVICTUS: ripretinib in advanced gastrointestinal stromal tumours after three or more prior kinase inhibitors","route":"/key-papers/paper-invictus-ripretinib-lancet-oncol-2020/"}]}}