Encorafenib

BRAF and MEK inhibitors
BRAF and MEK inhibitors
High alert
An error with this medicine can cause serious harm: double checks and protocols are used.
Pregnancy: avoid
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting and non-hormonal contraception is used during and after treatment, because the drug makes…

A BRAF inhibitor given with binimetinib in BRAF V600 melanoma and lung cancer, and with cetuximab in BRAF V600E colorectal cancer.

Updated Nov 1, 2026

Quick facts

Group: BRAF and MEK inhibitors
Target: BRAF serine/threonine kinase (V600E mutant), also wild-type BRAF and CRAF
Used for: BRAF V600E/K unresectable
Key effects: Fatigue · Joint and muscle pain · Skin thickening
Monitor: BRAF V600 mutation test · Skin examinations before
ATC: L01EC03

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

Mechanism of action

BRAF serine/threonine kinase (V600E mutant), also wild-type BRAF and CRAFEncorafenib

No encorafenib structure was used: the figure shows dabrafenib, which occupies the same ATP pocket of human BRAF V600E.

Target in 3D: BRAF serine/threonine kinase (V600E mutant), also wild-type BRAF and CRAF. PDB structure 4XV2 (RCSB PDB, public domain). View the structure at RCSB PDB

Encorafenib blocks the ATP site of BRAF V600E, as well as wild-type BRAF and CRAF, cutting the MAPK growth signal. It is paired with the MEK inhibitor binimetinib in melanoma and lung cancer. In colorectal cancer, BRAF blockade alone works poorly, and it is combined instead with the anti-EGFR antibody cetuximab.

Blocks the ATP site of BRAF V600E
Melanoma and lung: paired with the MEK inhibitor binimetinib
Colorectal: paired with the anti-EGFR antibody cetuximab

Indications

BRAF V600E/K unresectable or metastatic melanoma, with binimetinib. Melanoma →
BRAF V600E metastatic non-small cell lung cancer in adults, with binimetinib. Lung cancer →
BRAF V600E metastatic colorectal cancer, with cetuximab (with or without chemotherapy). Colorectal cancer →

Adverse effects

Common

Fatigue, nausea, vomiting, abdominal pain
Joint and muscle pain
Skin thickening, acne-like rash, dry or itchy skin, hair loss
Redness, numbness or peeling of the palms and soles
Headache, dizziness, taste changes

Contraindications

Tumours without a BRAF V600 mutation (no benefit)

Key interactions

Hormonal contraceptives (pills, patches, rings, injections): Made less effective; a non-hormonal method is used.
Strong CYP3A4 inhibitors (clarithromycin, itraconazole, ketoconazole, ritonavir) and grapefruit: Raise its levels and its toxicity.
Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, St John's wort): Lower its levels and can make it fail.
Other QT-prolonging drugs (some antiarrhythmics, macrolides, antipsychotics): Additive risk of QT prolongation and arrhythmia.

What is monitored

BRAF V600 mutation test of the tumour before starting
Skin examinations before, during and for months after treatment
ECG with potassium, calcium and magnesium
Eye examinations and echocardiogram as ordered
Liver tests

Administration and safety

Oral; swallowed whole, never split, crushed, chewed or opened.
Grapefruit, its juice and St John's wort are avoided because they change its levels.
If the patient vomits after a dose, the dose is not repeated; the next one is taken at the usual time.

Pregnancy and breastfeeding

Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting and non-hormonal contraception is used during and after treatment, because the drug makes hormonal contraceptives less effective; breastfeeding is avoided.

Nursing care

Review the medication list for QT-prolonging drugs and check electrolyte results.
Teach to report fainting, palpitations, vision changes or new skin lesions.
Inspect palms and soles at each visit.
Confirm a negative pregnancy test and teach non-hormonal contraception (the pill may fail).

Pharmacokinetics

Absorption: Oral capsules, once daily, with or without food.
Metabolism: Liver, mainly CYP3A4.
Half-life: About 3.5 hours.

Test yourself

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

Which partner does encorafenib need in BRAF V600E colorectal cancer?

Cetuximab, an anti-EGFR antibody (with or without chemotherapy).

Which MEK inhibitor is paired with encorafenib in melanoma?

Binimetinib.

Which heart rhythm problem is monitored with encorafenib?

QT prolongation, with ECG and electrolytes.

Add to my cards (3)

Connections

← Back to the class: BRAF and MEK 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: Encorafenib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Encorafenib - NCI (National Cancer Institute, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.