[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) › Vemurafenib

# Vemurafenib

## Kinase inhibitors (targeted oncology)?

Kinase inhibitors (targeted oncology)

## High alert?

An error with this medicine can cause serious harm: double checks and protocols are used.

An oral inhibitor of mutant BRAF V600E for melanoma that carries this mutation; it causes photosensitivity and new skin squamous cell cancers.

Updated Nov 1, 2026

Also called: PLX4032

## Quick facts

**Group**
[Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

**Target**
BRAF kinase with the V600E mutation

**Used for**
Unresectable or metastatic melanoma

**Key effects**
Joint pain · Rash · Photosensitivity and sunburn

**Monitor**
BRAF V600 mutation test before starting · Liver tests

**ATC**
L01EC01

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**BRAF kinase with the V600E mutation**Vemurafenib

ⓘ The crystal shows vemurafenib in the ATP site of the human BRAF V600E kinase domain.

**Target in 3D:** BRAF kinase with the V600E mutation. PDB structure 3OG7 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3OG7) · Drag to rotate · pinch to zoom

Many melanomas carry a BRAF V600 mutation that keeps the RAF–MEK–ERK pathway switched on. Vemurafenib, whose name comes from «V600E», inhibits the mutant BRAF kinase (also V600K) and shuts down this pathway, so the melanoma cells stop growing. Melanomas without the mutation do not respond. It may be combined with a MEK inhibitor (cobimetinib), as is done with other BRAF inhibitors to delay resistance.

- BRAF V600E keeps RAF–MEK–ERK switched on
- Vemurafenib blocks mutant BRAF
- MAPK signalling stops; melanoma cells stop growing
- No effect without the BRAF V600 mutation

## Indications

- Unresectable or metastatic melanoma with a BRAF V600E mutation, confirmed by testing. [Melanoma →](https://durgical.com/en/conditions/melanoma/)
- Erdheim-Chester disease with a BRAF V600 mutation.

## Adverse effects

### Common

- Joint pain
- Rash, thickened skin (hyperkeratosis), skin papillomas
- Photosensitivity and sunburn
- Hair loss
- Fatigue, headache, fever
- Hand-foot skin reaction

### Serious (rare, important)

- New cutaneous squamous cell carcinomas and other new primary cancers
- QT prolongation
- Severe skin reactions
- Liver injury
- Severe photosensitivity
- Worsened radiation injury

## Contraindications

- Melanoma without a BRAF V600 mutation (no benefit, possible harm)
- Caution: long QT, heart failure, low potassium, magnesium or calcium

## Key interactions

**Tizanidine and other narrow-margin CYP1A2 substrates**
Vemurafenib raises their levels; tizanidine is avoided.

**Strong CYP3A4 inducers and inhibitors, St John's wort**
Change vemurafenib levels; avoided.

**Other QT-prolonging drugs**
Add to QT prolongation.

## What is monitored

- BRAF V600 mutation test before starting
- Full skin examination before starting and regularly during and after treatment
- ECG and electrolytes
- Liver tests

## Administration and safety

- Oral; swallowed whole at about the same time each day.
- Check the name carefully: kinase inhibitors with similar «-tinib» names are not interchangeable.
- Taken twice daily about twelve hours apart, with or without food; a vomited dose is not repeated.

## Pregnancy and breastfeeding

May harm the fetus; contraception is used during treatment and for a short time after, and breastfeeding is avoided.

## Nursing care

- Look at the skin at every visit and report new growths or sores.
- Check that ECG and electrolyte results are up to date.
- Teaching: avoid sun exposure, wear protective clothing, lip balm and broad-spectrum sunscreen; report palpitations, fainting or yellow skin.

## Pharmacokinetics

**Absorption**
Oral, with or without food.

**Metabolism**
Substrate of CYP3A4; substrate and inhibitor of P-glycoprotein; it raises levels of CYP1A2 substrates.

**Half-life**
Long, about two to three days.

## Memory aid

«VEMURAFENIB = V600E MUtant RAF»: the name tells the target. Sun and new skin cancers are its signature.

## Test yourself

Think of the answer, then tap the question to see it.

## Which test is required before vemurafenib?

A test confirming a BRAF V600E mutation in the melanoma.

## Which new skin lesion appears in some patients on vemurafenib?

Cutaneous squamous cell carcinoma.

## Which muscle relaxant is avoided with vemurafenib, and why?

Tizanidine, because vemurafenib raises the levels of CYP1A2 substrates.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/vemurafenib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

## Connections

## Related drugs 2

- [Sorafenib](https://durgical.com/en/pharmacology/sorafenib/)
- [Atezolizumab](https://durgical.com/en/pharmacology/atezolizumab/)

## Related conditions 1

- [Melanoma](https://durgical.com/en/conditions/melanoma/)

[← Back to the class: Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Vemurafenib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a612009.html) (MedlinePlus (U.S. National Library of Medicine), 2018); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EC01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/vemurafenib/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/vemurafenib/