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Kinase inhibitor

Ripretiinib (brand name QINLOCK) is a medicine used to treat adults with advanced gastrointestinal stromal tumor (GIST) who have already tried three or more other kinase inhibitors, including imatinib. It works by blocking specific proteins (kinases) that help cancer cells grow.

How it worksRipretiinib is a tyrosine kinase inhibitor. It blocks certain receptors like KIT and PDGFR alpha that help tumor cells grow and survive.

Brand names:QINLOCK

Used for
Advanced gastrointestinal stromal tumor (GIST) in adults who have received 3 or more prior kinase inhibitor treatments.
Conditions
Advanced gastrointestinal stromal tumor (GIST)
Class
Kinase InhibitorTyrosine Kinase InhibitorKinase inhibitorIntegumentaryGastrointestinalCardiovascularHematologic

How to take

FormsOral tablet
RoutesOral

The standard dose is 150 mg once daily, which can be taken with or without food. Tablets should be swallowed whole.

Take the medicine at the same time every day. If you miss a dose, take it if it has been less than 8 hours since your scheduled time. If you vomit after taking it, do not take an extra dose; just continue with your next scheduled dose.

Missed dose: Take a missed dose if less than 8 hours have passed since the scheduled dose.

Key warnings

  • ·Skin issues like redness or pain on palms and soles may require pausing treatment.
  • ·Regular skin checks are needed to monitor for new skin cancers.
  • ·Blood pressure should be monitored, and treatment may be paused if blood pressure is uncontrolled.
  • ·Heart function should be checked before and during treatment.
  • ·Stop using this drug at least 1 week before elective surgery and wait at least 2 weeks after major surgery before restarting.
  • ·Avoid direct sunlight as the drug may make your skin more sensitive.
  • ·This medicine can cause birth defects; use effective birth control during treatment.

Do not use if

  • ·None listed.

Side effects

Common

Hair lossFatigueNauseaAbdominal painConstipationMuscle painDiarrheaLoss of appetiteHand-foot syndrome (palmar-plantar erythrodysesthesia)Vomiting

Serious

  • ·Palmar-plantar erythrodysesthesia syndrome (skin changes on palms and soles)
  • ·New skin cancers
  • ·High blood pressure (hypertension)
  • ·Heart problems (cardiac dysfunction)
  • ·Sensitivity to sunlight (photosensitivity)
  • ·Risk of poor wound healing after surgery
  • ·Potential harm to an unborn baby

Seek help if

  • ·Palmar-plantar erythrodysesthesia syndrome
  • ·Uncontrolled hypertension
  • ·Cardiac dysfunction
  • ·New skin malignancies

Interactions

  • ·Strong CYP3A inhibitors (may increase risk of side effects; monitor closely).
  • ·Strong or moderate CYP3A inducers (may make the drug less effective; avoid use if possible).
  • ·If a moderate CYP3A inducer must be used, the dose frequency may need to change to twice daily.
FoodCan be taken with or without food.

Special populations

PregnancyRipretiinib can cause harm to a fetus. Animal studies showed potential for skeletal and heart issues in offspring. Females of reproductive age should use effective contraception while taking this medication.

PediatricThe safety and effectiveness of QINLOCK in children have not been studied.

GeriatricStudies did not include enough patients aged 65 or older to know if they respond differently than younger adults.

Talk to your doctor

Monitor

  • ·Blood pressure
  • ·Heart ejection fraction
  • ·Skin changes/moles
  • ·Hand and foot skin condition
  • ·Lipase levels
  • ·Phosphate levels

Questions to ask

  • ·Is my blood pressure controlled enough to start QINLOCK?
  • ·How will we monitor my heart function while on this drug?
  • ·What should I do if I notice skin changes on my hands or feet?
  • ·When is the safest time to schedule any upcoming surgeries?

Pharmacokinetics

BioavailabilityRipretiinib AUC 0-24h increased proportionally over a dose range of 20-250 mg, but C max was less than dose proportional.
MetabolismCharacterized by its active metabolite DP-5439; affected by CYP3A inhibitors and inducers.

Ingredients

Allergens

lactose

Inactive

crosspovidonehypromellose acetate succinatelactose monohydratemagnesium stearatemicrocrystalline cellulosesilicon dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.