ripretinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
ripretinib: clinical details
Prescribing considerations
- Treatment should be initiated by a clinician experienced in anticancer therapy.
- Control blood pressure before initiation.
- Assess potential CYP3A and transporter interactions, including herbal products.
- Consider wound-healing risk around surgery.
- Advise ultraviolet avoidance and effective contraception.
- Evidence is limited in severe renal or hepatic impairment; closer safety monitoring is appropriate.
Contraindications and cautions
- Hypersensitivity to ripretinib or any excipient.
- The lactose-containing product should not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
Monitoring
- Blood pressure at baseline and as clinically indicated.
- Left ventricular ejection fraction before treatment and during treatment when clinically indicated.
- Dermatological examination at initiation and routinely thereafter.
- Hands and feet for palmar-plantar erythrodysaesthesia syndrome.
- Clinical and laboratory toxicity, including hepatic markers, bilirubin, phosphate and lipase as appropriate.
- Pregnancy status before treatment and during treatment in people of reproductive potential.
- Wound healing when treatment is interrupted for surgery.
Clinical pharmacology
Ripretinib inhibits KIT and PDGFRA, including wild-type and primary or secondary mutant forms. CYP3A4/5 is the main metabolic pathway, producing the active metabolite DP-5439; both parent and metabolite are highly protein-bound.
Formulation and product differences
- The selected product is an oral, lactose-containing tablet.
- Tablets must remain intact and should not be chewed, split or crushed.
- The bottle contains a desiccant and must be kept tightly closed to protect the tablets from light and moisture.
ripretinib preparations and strengths
Tablet
Route: Oral
Strengths: 50 mg
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.