Vemurafenib
ZELBORAF
What it isBRAF V600 kinase inhibitor; BRAF-mutant melanoma.
Why this oneRapid and often dramatic tumor regression within weeks.
What limits itSevere photosensitivity, and paradoxical squamous cell carcinomas in a quarter of patients. Resistance emerges within months unless a MEK inhibitor is added.
FDA-approved for
- BRAF+ melanoma (2011)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| BRAF V600E-mutation melanoma (unresectable/metastatic) and Erdheim-Chester disease | Adults | 960 mg BID (~12 h apart) | 960 mg BID | 960 mg BID |
Renal Undefined
Hepatic Undefined
Missed dose may be taken up to 4 h before the next dose; do not take an extra dose after vomiting.
Instructions
- Confirm BRAF V600E mutation before initiating
- With or without a meal, ~12 h apart; do not crush or chew
- A missed dose can be taken up to 4 h before the next dose; skip the extra dose if vomiting occurs
- Unavoidable strong CYP3A4 inducer: increase dose by 240 mg as tolerated
Cautions
- New primary cutaneous and non-cutaneous malignancies
- Tumor promotion in BRAF wild-type melanoma
- Serious hypersensitivity/anaphylaxis and DRESS
- Severe dermatologic reactions (SJS/TEN)
- QT prolongation (monitor ECG/electrolytes)
- Hepatotoxicity
- Photosensitivity
- Ophthalmologic reactions (uveitis)
- Embryo-fetal toxicity
- Radiation sensitization and recall
- Renal failure
- Dupuytren's contracture and plantar fascial fibromatosis
Adverse reactions
- Arthralgia
- Rash
- Alopecia
- Fatigue
- Photosensitivity reaction
- Nausea
- Pruritus
- Skin papilloma
Pregnancy Can cause fetal harm based on mechanism; placental transfer reported.
Lactation Do not breastfeed during treatment and for 2 weeks after the final dose.
NO BOXED WARNINGS
Principal riskPhotosensitivity; paradoxical squamous carcinomas
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2032 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Vemurafenib ballicule
