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Switch-control KIT/PDGFRA tyrosine-kinase inhibitor Pregnancy: Can cause fetal harm when administered to a pregnant woman, based on findings from animal studies and its mechanism of action; malformations primarily of the cardiovascular and skeletal systems, reduced fetal body weight and increased post-implantation loss occurred in rats and rabbits at maternal exposures approximately equal to the human exposure at the recommended 150 mg dose. There are no available data in pregnant women. Advise pregnant women of the potential risk to a fetus and advise females of reproductive potential to use effective contraception.

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.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 150 mg
Route: Oral — swallow tablets whole, with or without food
Frequency: Once daily at the same time each day, until disease progression or unacceptable toxicity
Take a missed dose only if less than 8 hours have passed since the missed scheduled dose. If vomiting occurs after taking a dose, do not take an additional dose — continue with the next scheduled dose. Dose reduction for adverse reactions is 100 mg orally once daily; permanently discontinue in patients unable to tolerate 100 mg once daily. Grade 2 palmar-plantar erythrodysaesthesia syndrome (PPES), arthralgia or myalgia: withhold until Grade <=1 or baseline — if recovered within 7 days resume at the same dose, otherwise resume at a reduced dose; on recurrence resume at a reduced dose regardless of time to improvement. Grade 3 PPES, arthralgia or myalgia: withhold for at least 7 days or until Grade <=1 or baseline (maximum 28 days), then resume at a reduced dose. Grade 3 hypertension: if symptomatic withhold until symptoms resolve and blood pressure is controlled, then resume at the same dose if controlled to Grade <=1 or baseline, otherwise at a reduced dose; permanently discontinue for Grade 4. Permanently discontinue for Grade 3 or 4 left ventricular systolic dysfunction. Other Grade 3 or 4 adverse reactions: withhold until Grade <=1 or baseline (maximum 28 days) then resume at a reduced dose, otherwise permanently discontinue; permanently discontinue if Grade 3 or 4 recurs. Re-escalation may be considered if maintained at Grade <=1 or baseline for at least 28 days. Moderate CYP3A inducers: avoid; if unavoidable, increase the dosing frequency from 150 mg once daily to 150 mg twice daily during co-administration, and resume 150 mg once daily 14 days after the inducer is discontinued (for patients on twice-daily dosing who miss a dose: take it if less than 4 hours have passed, otherwise skip it). Withhold for at least 1 week prior to elective surgery and do not administer for at least 2 weeks after major surgery and until adequate wound healing. Paediatric: safety and effectiveness in paediatric patients have not been established. CLINICIAN CHECK: this draft is from the US FDA prescribing information (QINLOCK, Deciphera Pharmaceuticals, label date 2025-05-12) — no UK SPC posology was fetched; verify against the UK SPC.

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).

Related

Curated clinical cross-links plus same-class fallbacks.