# Ripretinib

Source: https://onco.cc/drugs/ripretinib/  
OnCo record `ripretinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-07
- 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: US 2020: Advanced GIST after ≥3 prior kinase inhibitors including imatinib
- Dosing: Oral; 150 mg once daily; 150 mg twice daily on progression
- Toxicity (grade 3+): Hypertension 4%

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Ripretinib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Ripretinib

## Connected records

- cancers: [Gastrointestinal stromal tumour (GIST)](https://onco.cc/cancers/gist/), [Imatinib-resistant GIST](https://onco.cc/cancers/gist-imatinib-resistant/), [KIT exon 11-mutant GIST](https://onco.cc/cancers/gist-kit-exon-11/), [Sarcomas (soft tissue, bone, GIST)](https://onco.cc/cancers/sarcoma/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [KIT](https://onco.cc/targets/kit/), [PDGFRA](https://onco.cc/targets/pdgfra/)
- companies: [Deciphera Pharmaceuticals (Ono)](https://onco.cc/companies/deciphera/)
- trials: [A Study of Inlexisertib (DCC-3116) in Combination With Anticancer Therapies in Participants With Advanced Malignancies](https://onco.cc/trials/nct05957367/), [A Study of Ripretinib vs Sunitinib in Advanced GIST Patients After Treatment With Imatinib](https://onco.cc/trials/nct03673501/), [INSIGHT](https://onco.cc/trials/insight-gist/), [INVICTUS](https://onco.cc/trials/invictus/)
- pairings: [ctDNA KIT genotyping → TKI selection in GIST](https://onco.cc/pairings/ctdna-genotype-gist-tki/)
- key papers: [INTRIGUE: ripretinib versus sunitinib in advanced gastrointestinal stromal tumour after imatinib](https://onco.cc/key-papers/paper-intrigue-ripretinib-vs-sunitinib-jco-2022/), [INVICTUS: ripretinib in advanced gastrointestinal stromal tumours after three or more prior kinase inhibitors](https://onco.cc/key-papers/paper-invictus-ripretinib-lancet-oncol-2020/)

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