Vemurafenib
Pronunciation: pronunciation varies by local usage.
- Generic name
- vemurafenib
- Brand names
- Zelboraf
- Drug class
- BRAF kinase inhibitor
- Form
- Film-coated tablet
- Route
- Oral
- Legal status
- Prescription antineoplastic (anticancer) medicine
Availability and supply rules vary by country
Trade names by country: United States · Canada
Australia: · Full directory
What vemurafenib is and how it works
Vemurafenib is an oral BRAF kinase inhibitor used for specific cancers or conditions with a BRAF V600 mutation. (1)
The US label indicates vemurafenib for unresectable or metastatic melanoma with a BRAF V600E mutation detected by an FDA-approved test, and for Erdheim-Chester Disease with a BRAF V600 mutation. Tumour mutation testing is required before starting treatment for melanoma.
Mechanism of action: how vemurafenib works
Vemurafenib is a BRAF kinase inhibitor. (1)
What vemurafenib is used for
BRAF V600E mutation-positive unresectable or metastatic melanoma
The US label indicates vemurafenib for patients with unresectable or metastatic melanoma with a BRAF V600E mutation, as detected by an FDA-approved test. (1)
Erdheim-Chester Disease with a BRAF V600 mutation
The US label indicates vemurafenib for patients with Erdheim-Chester Disease with a BRAF V600 mutation. (1)
Before taking vemurafenib
Do not take / not appropriate for
- Vemurafenib is not indicated for melanoma with wild-type BRAF. The presence of a BRAF V600E mutation in tumour specimens must be confirmed before treatment for melanoma is initiated. (Melanoma) (1)
- No contraindications are stated in the reviewed US FDA label. (US FDA label reviewed) (1)
Tell your clinician about
- All medicines, including medicines that may be strong CYP3A4 inhibitors or inducers, CYP1A2 substrates with a narrow therapeutic index, and P-glycoprotein substrates with a narrow therapeutic index.
- Any heart-rhythm concern or medicines that may affect heart rhythm, so ECG and electrolyte monitoring can be planned.
- Any liver or kidney problem.
- Any eye symptoms or previous eye inflammation.
- Pregnancy, plans for pregnancy, or breastfeeding.
How to take vemurafenib
- The US recommended dose is 960 mg by mouth twice daily, approximately 12 hours apart, with or without food.
- Swallow tablets whole. Tablets should not be crushed or chewed.
- Use the dose and any dose modification directed by the oncology prescriber; do not alter the dose yourself.
- Avoid sun exposure and use broad-spectrum UVA/UVB sunscreen with SPF 30 or higher while taking vemurafenib.
Procedures and treatment changes
Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1)
Missed dose
The US label states that a missed dose may be taken up to 4 hours before the next scheduled dose. If it is less than 4 hours before the next dose, contact the prescribing team or pharmacist for advice. Do not take an extra dose.
Overdose
Overdose-management instructions were not established in the reviewed source. If more than the prescribed amount may have been taken, contact the prescribing oncology service, poison-information service, or urgent medical care service promptly. (1)
Side effects
Side effects differ between melanoma and Erdheim-Chester Disease populations. The reviewed US label reports important risks including new primary malignancies, QT prolongation, liver-test abnormalities, creatinine elevations, photosensitivity, and eye inflammation.
Joint pain, rash, hair loss, tiredness, photosensitivity reaction, nausea, itching, or skin papilloma
What to notice: These were common adverse reactions in melanoma patients. In Erdheim-Chester Disease, joint pain, maculo-papular rash, hair loss, fatigue, QT prolongation, and skin papilloma occurred in more than 50% of patients.
What to do: Tell the oncology team about persistent, severe, or troublesome effects so they can assess them. (1)
Creatinine elevation
What to notice: In Trial 1, 26% of patients had Grade 1 to 2 creatinine elevations and 1.2% had Grade 3 to 4 elevations. In Erdheim-Chester Disease patients, Grade 1 to 2 elevations occurred in 86% and Grade 3 elevations in 9.1%.
What to do: Renal function requires clinical monitoring during treatment. (1)
Uveitis
What to notice: Uveitis occurred in 2.1% of patients receiving vemurafenib in the melanoma study.
What to do: Report eye concerns promptly to the oncology team for assessment. (1)
Possible new skin malignancy
What to notice: New or changing skin findings require assessment. Cutaneous squamous cell carcinoma and keratoacanthoma occurred during treatment.
What to do: Contact the oncology or dermatology team promptly for assessment. (1)
Possible liver-test abnormality
What to notice: The reviewed label reports shifts to Grade 3 or 4 liver laboratory abnormalities involving GGT, AST, ALT, alkaline phosphatase, and bilirubin.
What to do: Attend planned liver-test monitoring and contact the oncology team promptly about concerns. (1)
Serious warnings
New primary malignancies, including cutaneous squamous cell carcinoma — serious
Symptoms: Dermatologic evaluation may identify cutaneous squamous cell carcinoma or keratoacanthoma. In Trial 1, cutaneous squamous cell carcinoma occurred in 24% of vemurafenib-treated patients; in the Erdheim-Chester Disease group, cutaneous squamous cell carcinoma or keratoacanthoma occurred in 40.9%.
Action: Dermatologic evaluations are recommended before treatment, every 2 months during treatment, and for up to 6 months after treatment discontinuation. Seek prompt assessment for new or changing skin findings. (1)
QT prolongation — serious
Symptoms: Vemurafenib has a concentration-dependent QTc-prolonging effect. The largest mean QTc change from baseline was 15.1 ms within the first 6 months of treatment.
Action: ECG and electrolytes, including potassium, magnesium, and calcium, should be monitored before treatment, after 15 days, monthly during the first 3 months, and then every 3 months or more often as clinically indicated. Decisions about withholding or permanently discontinuing treatment must be made by the responsible clinician. (1)
Fetal harm — serious
Symptoms: Vemurafenib can cause fetal harm.
Action: Females of reproductive potential should use effective contraception during treatment and for at least 2 weeks after the final dose. Discuss pregnancy-related concerns promptly with the prescribing team. (1)
Interactions
| Medicine or test | Effect | Action |
|---|---|---|
| Strong CYP3A4 inhibitors | Coadministration increases vemurafenib exposure (AUC) by approximately 40%. | Tell the oncology prescriber and pharmacist about all medicines. If a strong CYP3A4 inhibitor must be coadministered, the clinician may consider a dose reduction. (1) |
| Strong CYP3A4 inducers | Coadministration decreases vemurafenib exposure (AUC) by approximately 40%. | Avoidance should be considered by the prescriber. If an inducer cannot be avoided, the clinician may increase the vemurafenib dose by 240 mg. (1) |
| CYP1A2 substrates with a narrow therapeutic index | Coadministration with tizanidine increased tizanidine AUC 4.7-fold. | Avoid coadministration where appropriate or ensure close clinical monitoring directed by the prescriber. (1) |
| P-glycoprotein substrates with a narrow therapeutic index | Coadministration with digoxin increased digoxin AUC 1.8-fold. | The prescriber should arrange close monitoring if these medicines are coadministered. (1) |
Pregnancy, breastfeeding, kidney/liver function, age
Children and adolescents
Safety and effectiveness in pediatric patients have not been established. No pediatric dosing is provided in the reviewed source. (1)
Pregnancy and breastfeeding
Vemurafenib can cause fetal harm. Females of reproductive potential should use effective contraception during treatment and for at least 2 weeks after the final dose. Patients should not breastfeed during treatment and for 2 weeks after the final dose. (1)
Renal or hepatic impairment
No dose adjustment is needed for mild-to-moderate renal or hepatic impairment according to the reviewed US label. The appropriate dose in severe renal impairment has not been established; data were available from only 1 patient. The appropriate dose in severe hepatic impairment has not been established; data were available from only 3 patients. (1)
Monitoring
Before starting
- For melanoma, confirm BRAF V600E mutation status in tumour specimens using an FDA-approved test.
- Perform a dermatologic evaluation.
- Obtain ECG and electrolytes, including potassium, magnesium, and calcium.
- Check liver enzymes, including transaminases and alkaline phosphatase, and bilirubin.
During treatment
- Perform dermatologic evaluations every 2 months during treatment and for up to 6 months after treatment discontinuation.
- Monitor ECG and electrolytes after 15 days, monthly during the first 3 months, then every 3 months thereafter or more often as clinically indicated.
- Monitor liver enzymes and bilirubin monthly during treatment or as clinically indicated.
- Monitor renal function clinically, given reported creatinine elevations.
Storage
Storage instructions were not established in the reviewed research notes. Follow the dispensing pharmacy label and the current product information.
Professional information
Clinician-facing context only. Use the current local product information, mutation-testing requirements, adverse-reaction management guidance, interaction assessment, and oncology protocols.
United States
Indication: BRAF V600E mutation-positive unresectable or metastatic melanoma; Erdheim-Chester Disease with a BRAF V600 mutation
Dose summary: The reviewed US FDA label recommends 960 mg orally twice daily, approximately 12 hours apart, with or without food. Tablets should not be crushed or chewed. Dose modifications for toxicity or interactions require the current label and clinician assessment.
Renal context: No dose adjustment is needed for mild-to-moderate renal impairment. The appropriate dose for severe renal impairment has not been established; available data were from 1 patient. (1)
Hepatic guidance
No dose adjustment is needed for mild-to-moderate hepatic impairment. The appropriate dose for severe hepatic impairment has not been established; available data were from 3 patients.
Overdose note
Overdose-management details were not established in the reviewed research notes. (1)
Frequently asked questions
Do I need tumour testing before vemurafenib for melanoma?
Yes. The US label requires confirmation of a BRAF V600E mutation in tumour specimens using an FDA-approved test before treatment for melanoma is started. Vemurafenib is not indicated for wild-type BRAF melanoma. (1)
Can I take vemurafenib with food?
Yes. The reviewed US label states that vemurafenib is taken by mouth approximately 12 hours apart, with or without food. Tablets should not be crushed or chewed. (1)
Why are skin checks needed with vemurafenib?
Vemurafenib can cause new primary malignancies, including cutaneous squamous cell carcinoma. The US label recommends dermatologic evaluation before treatment, every 2 months during treatment, and for up to 6 months after treatment discontinuation. (1)
What is the mechanism of action of vemurafenib?
Vemurafenib is a BRAF kinase inhibitor. (1)
What is the generic name of Vemurafenib?
The generic name is vemurafenib. It is sold under brand names including Zelboraf. (1)
What class of drug is vemurafenib?
Vemurafenib is classed as: BRAF kinase inhibitor. (1)
References
- ZELBORAF (vemurafenib) tablet, film coated — prescribing informationU.S. Food and Drug Administration · United States · accessed 2026-08-05 · source 1
- Vemurafenib — patient drug information (MedlinePlus)U.S. National Library of Medicine (MedlinePlus) · US · accessed 2026-08-14 · source 2
- ZELBORAF — FDA approval record (Drugs@FDA NDA202429)U.S. Food and Drug Administration · US · accessed 2026-08-14 · source 3
- vemurafenib — RxNorm normalized drug concept (RXCUI 1147220)U.S. National Library of Medicine (RxNorm) · US · accessed 2026-08-14 · source 4
Brand names by country
Single-ingredient vemurafenib names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.
Priority countries
United States
- ZELBORAF240 mg · genentech, inc.
Canada
- ZELBORAF