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Vemurafenib

Brand and Other Names: ZELBORAF®
Mechanism of Action:

Vemurafenib is a selective BRAF kinase inhibitor targeting mutated BRAF V600E, which leads to inhibition of the MAPK/ERK signaling pathway and tumor cell proliferation.

Indications:
  • Unresectable or metastatic melanoma with BRAF V600E mutation

  • Erdheim-Chester Disease (ECD) with BRAF V600 mutation

Route: oral
Dose:

Standard adult dose: 960 mg orally twice daily (4 tablets of 240 mg), taken approximately 12 hours apart, with or without food

Adverse Reactions:
  • Common (≥30% in melanoma): Arthralgia, rash, alopecia, fatigue, photosensitivity, nausea, pruritus, skin papilloma

  • Serious: Cutaneous squamous cell carcinoma (cuSCC), QT prolongation, hepatotoxicity, severe dermatologic reactions (e.g., SJS, TEN), hypersensitivity, uveitis, renal failure

Contraindication:

None

Warnings and Precautions:
  • Risk of new primary malignancies (cuSCC, keratoacanthoma, melanoma)

  • Tumor promotion in BRAF wild-type melanoma

  • QT prolongation and potential arrhythmias

  • Photosensitivity—avoid sun exposure

  • Liver and renal toxicity—monitor liver enzymes and creatinine

  • Serious skin reactions, hypersensitivity, ophthalmologic toxicity

  • Radiation sensitization/recall

  • Dupuytren's contracture and plantar fascial fibromatosis

 

See package insert for full prescribing information.