Drug Class: BRAF kinase inhibitor
Specifically targets BRAF V600E mutation
Indication
- Unresectable or metastatic melanoma with BRAF V600E mutation
- Confirm mutation with an FDA-approved test before starting
- Also approved for Erdheim-Chester disease with BRAF V600E
Mechanism of Action
- Selectively inhibits mutated BRAF V600E, a serine/threonine kinase
- Blocks the MAPK/ERK pathway, reducing tumor cell proliferation
Dosing
- 960 mg orally twice daily
- Taken with or without food
- Swallow tablets whole
Pharmacist Considerations
- CYP3A4 substrate: caution with inducers/inhibitors
- QT prolongation risk: monitor ECG and electrolytes
- Dermatologic monitoring: risk of cutaneous squamous cell carcinoma (cuSCC), new primary melanomas
- Photosensitivity: recommend sun protection
- Hepatotoxicity: monitor LFTs
- Other AEs: arthralgia, rash, alopecia, fatigue
Boxed Warning
None, but serious risks include secondary malignancies and severe skin reactions
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