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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors
ripretinib
L01EX19
Forms & Strengths
- 50mg tablets
- Oral administration
Adult Dosing
- 150mg once daily
- Dose reduction to 100mg daily if not tolerated
Pediatric Dosing
- Safety and efficacy not established
- Not recommended for patients under 18 years old
Indications
- Adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors
- Fourth-line or later treatment for GIST
Mechanism of Action
- Inhibits multiple receptor tyrosine kinases including KIT, PDGFRα, and KDR
- Blocks KIT and PDGFRα mutant kinases
Contraindications
- Hypersensitivity to ripretinib or any component of the formulation
Adverse Reactions
- Fatigue
- Nausea
- Diarrhea
- Abdominal pain
- Vomiting
- Constipation
- Myalgia
- Arthralgia
- Anemia
- Neutropenia
- Hypertension
- Tumor lysis syndrome
Drug Interactions
- Strong CYP3A4 inhibitors may increase ripretinib concentrations
- Strong CYP3A4 inducers may decrease ripretinib concentrations
- Coadministration with substrates of P-gp may increase concentrations of the substrate
Curated Content: Needs Vetting Before Put to Clinical Use