Ripretinib (Specialist drug)
Brand names: Qinlock
Ripretinib is an oral switch-control kinase inhibitor used as a specialist treatment for advanced gastrointestinal stromal tumour after prior therapies.
Adult dose
Dose auto-extracted from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.
Contraindications
- None — section 4 of the US label states 'None'
Side effects
- Alopecia
- Fatigue
- Nausea and vomiting
- Abdominal pain, constipation and diarrhoea
- Myalgia and decreased appetite
- Palmar-plantar erythrodysaesthesia syndrome
- Serious/clinically significant: new primary cutaneous malignancies, hypertension, cardiac dysfunction (left ventricular systolic dysfunction), photosensitivity; most common Grade 3-4 laboratory abnormalities were increased lipase and decreased phosphate
Interactions
- Strong CYP3A inhibitors — increase exposure to ripretinib and its active metabolite (DP-5439); monitor patients more frequently for adverse reactions
- Strong CYP3A inducers — avoid concomitant use; they decrease exposure to ripretinib and its active metabolite and may decrease anti-tumour activity
- Moderate CYP3A inducers — avoid concomitant use; if unavoidable, increase the ripretinib dosing frequency to 150 mg twice daily
Clinical monograph
How it works
It broadly inhibits KIT and PDGFRA kinase signalling, including a wide range of resistance mutations, by binding the kinase switch pocket and activation loop.
Prescribing in practice
- Palmar-plantar erythrodysaesthesia (hand-foot skin reaction) and other skin toxicities, including new cutaneous malignancies, occur and warrant regular skin assessment.
- Hypertension and reduced cardiac function (left ventricular dysfunction) can occur and require monitoring.
- Initiation is restricted to specialist oncology services experienced in kinase inhibitor toxicity.
Monitoring
Monitor blood pressure, cardiac (left ventricular) function and the skin regularly during treatment.
Counselling the patient
- Report painful or blistering skin on the hands or feet and any new or changing skin lesions.
- Tell the team about breathlessness, swollen ankles or new fatigue.
- Attend for regular blood pressure and follow-up checks.
Evidence & guidelines
Use is supported by the INVICTUS phase III trial and the product SPC in advanced GIST.
Reference: NICE TA790; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).
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