ripretinib at a glance
Medicine class
Tyrosine kinase inhibitor targeting KIT and PDGFRA.
Licensed use
Advanced GIST in previously treated adults.
Food
Tablets may be taken with or without food.
Tablet handling
Swallow whole; do not chew, split, crush or take damaged tablets.
Sun protection
Minimise ultraviolet exposure and use protective clothing and high-factor sunscreen.
What is ripretinib used for?
The selected UK product is licensed for:
Treatment of adults with advanced gastrointestinal stromal tumour after prior treatment with three or more kinase inhibitors, including imatinib.
How does ripretinib work?
Ripretinib blocks KIT and PDGFRA tyrosine kinases, including several altered forms that can drive GIST growth. It also inhibits some other kinases in laboratory studies.
ripretinib preparations and strengths
Tablet
Route: Oral
Strengths: 50 mg
How to take ripretinib
Follow the anticancer specialist’s instructions and take the tablets consistently at the same time of day.
Take with or without food.
Swallow tablets whole with water.
Do not chew, split or crush tablets.
Do not take tablets that are broken, cracked or otherwise damaged.
Keep the tablets in the original tightly closed bottle, with the desiccant, protected from light and moisture.
ripretinib side effects
Common or expected effects
- Tiredness
- Hair loss
- Nausea or vomiting
- Constipation or diarrhoea
- Muscle or joint pain and muscle spasms
- Hand-foot skin reaction
- Headache
- Weight loss
- Dry or itchy skin
- Raised blood pressure
- Cough or breathlessness
- Peripheral swelling
Get urgent medical advice
- Painful redness, swelling or blistering of the palms or soles
- Symptoms of severe hypertension, such as marked headache, dizziness or light-headedness
- Possible heart failure: new or worsening breathlessness, profound tiredness, or swelling of the ankles, legs or abdomen
- New or changing skin lesions, including a non-healing sore, bleeding bump, wart or changing mole
- Severe or persistent abdominal pain, vomiting or breathlessness
ripretinib in pregnancy
Human pregnancy data are unavailable, and ripretinib may harm a developing baby. It should generally not be used during pregnancy unless a specialist considers treatment clinically necessary. Pregnancy status is checked before and during treatment; effective contraception is required, with a barrier method added when systemic hormonal contraception is used.
ripretinib while breastfeeding
It is unknown whether ripretinib enters breast milk, and harm to a breastfed child cannot be excluded. Breastfeeding must stop during treatment and for at least one week after the final dose; discuss feeding plans with the specialist team.
ripretinib interactions
The oncology team should review all prescribed, over-the-counter and herbal products before treatment.
Carbamazepine, phenytoin, rifampicin, phenobarbital and St John’s wort
These CYP3A inducers can substantially reduce ripretinib exposure and should be avoided.
Ketoconazole, itraconazole, clarithromycin, erythromycin, ritonavir, posaconazole and voriconazole
These strong CYP3A or P-glycoprotein inhibitors may increase ripretinib exposure, requiring caution and monitoring.
Grapefruit juice
Avoid because it may increase ripretinib exposure.
Common questions about ripretinib
Answers are fully visible for fast scanning and source review.
What cancer is ripretinib used to treat?
It is licensed for adults with advanced gastrointestinal stromal tumour previously treated with at least three kinase inhibitors, including imatinib.
Is ripretinib chemotherapy?
It is a targeted anticancer treatment called a tyrosine kinase inhibitor rather than conventional cytotoxic chemotherapy.
Can ripretinib be taken with food?
Yes. It may be taken with or without food.
Can ripretinib tablets be crushed or split?
No. Swallow them whole and do not take tablets that are broken, cracked or damaged.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.