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Dabrafenib

  • BRAF and MEK inhibitorsBRAF and MEK inhibitors
  • High alertAn error with this medicine can cause serious harm: double checks and protocols are used.
  • Pregnancy: avoidAvoid 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…

An oral inhibitor of mutant BRAF, paired with trametinib in BRAF V600 melanoma, lung and thyroid cancer. Watch fever, skin and eyes.

Updated

Also called: dabrafenib mesylate

Quick facts

Group
BRAF and MEK inhibitors
Target
BRAF serine/threonine kinase (V600E/K mutants)
Used for
BRAF V600E/K melanoma · BRAF V600E low-grade glioma
Key effects
Fever and chills · Skin thickening · Headache
Monitor
BRAF V600 mutation test · Skin examinations before
ATC
L01EC02

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

Mechanism of action

The figure shows dabrafenib in the ATP pocket of the human BRAF V600E kinase domain.

Target in 3D: BRAF serine/threonine kinase (V600E/K mutants). PDB structure 4XV2 (RCSB PDB, public domain). View the structure at RCSB PDB

Dabrafenib blocks the ATP site of mutant BRAF (V600E, V600K, V600D) and, at higher concentrations, wild-type BRAF and CRAF. This cuts the MAPK signal that drives the tumour. Resistance to the drug alone appears within months, so it is combined with the MEK inhibitor trametinib, which also delays the new skin squamous cell cancers seen with BRAF inhibitors alone.

  1. BRAF V600E keeps the MAPK pathway switched on
  2. Dabrafenib blocks the ATP site of mutant BRAF
  3. Paired with trametinib to block MEK and delay resistance

Indications

Adverse effects

Common

  • Fever and chills (especially with trametinib)
  • Skin thickening, papillomas, rash, dry skin, hair loss
  • Headache, joint and muscle pain
  • Nausea, diarrhoea, decreased appetite
  • Cough and fatigue

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 CYP2C8 or CYP3A4 inducers
Lower dabrafenib levels and can cause loss of effect.

What is monitored

  • BRAF V600 mutation test of the tumour before starting
  • Skin examinations before, during and for months after treatment
  • Temperature and kidney function when fever occurs
  • Blood glucose in people with diabetes
  • Eye symptoms

Administration and safety

  • Oral, on an empty stomach, away from meals; capsules are swallowed whole.
  • Tablets for oral suspension are dispersed in water and drunk at once.
  • Dabrafenib (BRAF) and trametinib (MEK) are separate drugs given together: check both on the order.

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

  • Teach to check temperature and to call promptly for fever, chills or shaking.
  • Teach to report new warts, sores or changing moles; arrange skin examinations.
  • Report eye pain, redness or blurred vision.
  • Confirm a negative pregnancy test and teach non-hormonal contraception (the pill may fail).

Pharmacokinetics

Absorption
Oral, twice daily, on an empty stomach.
Metabolism
Liver, CYP2C8 and CYP3A4.
Half-life
About 8 hours.

Test yourself

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

Why is dabrafenib combined with trametinib?

To block BRAF and MEK together, which delays resistance and reduces new skin squamous cell cancers.

What is the most typical reaction of the dabrafenib + trametinib pair?

Fever (pyrexia) with chills.

Which contraceptive method is advised with dabrafenib, and why?

A non-hormonal method, because dabrafenib makes hormonal contraceptives less effective.

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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: Dabrafenib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Dabrafenib Mesylate - NCI (National Cancer Institute, 2024); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.