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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › B-Raf serine-threonine kinase (BRAF) inhibitors
vemurafenib
L01EC01
Forms & Strengths
- Tablets: 240mg
- Film-coated, scored
Adult Dosing
- 960mg twice daily
- Dose reduction for intolerability
- Dose modification for hepatic impairment
Pediatric Dosing
- Safety and efficacy not established
- No data available for pediatric use
Indications
- Unresectable or metastatic melanoma with BRAF V600E mutation
- Erdheim-Chester disease with BRAF V600 mutation
Mechanism of Action
- Selective inhibitor of BRAF V600 kinase
- Inhibits tumor cell growth and proliferation
Contraindications
- Hypersensitivity to vemurafenib or its components
- No absolute contraindications in pregnancy or lactation, but caution advised
Adverse Reactions
- Skin reactions (rash, photosensitivity, hyperkeratosis)
- Arthralgia, fatigue, alopecia, keratoacanthoma
- Squamous cell carcinoma, QT interval prolongation
Drug Interactions
- CYP3A4 inhibitors (e.g. ketoconazole): avoid co-administration
- CYP3A4 inducers (e.g. rifampicin): monitor for reduced efficacy
- Warfarin: monitor INR for increased anticoagulant effect
Curated Content: Needs Vetting Before Put to Clinical Use