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Tafinlar (dabrafenib)

Tafinlar blocks the activity of a mutated protein called BRAF that is involved in cancer cell growth.

Tafinlar (dabrafenib) is a small molecule kinase inhibitor developed by Novartis, targeting the serine/threonine-protein kinase B-raf. It was FDA-approved in 2013 for the treatment of malignant melanoma with BRAF V600E mutation and metastatic malignant melanoma. Tafinlar is a patented medication with no generic manufacturers available. Key safety considerations include its potential to cause skin reactions, fever, and liver damage. As a kinase inhibitor, Tafinlar works by blocking the activity of the BRAF protein, which is mutated in certain cancer cells.

At a glance

Mechanism of action

Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth [see Indications and Usage (1)]. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.Dabrafenib and trametinib target two different kinases in the RAS/RAF/MEK/ERK pathway. Use of dabrafenib and trametinib in combination resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation positive tumor xen

Approved indications

• Malignant Melanoma with BRAF V600E Mutation
• Metastatic malignant melanoma

Common side effects

• Pyrexia
• Hyperkeratosis
• Headache
• Arthralgia
• Palmar-plantar erythrodysesthesia syndrome
• Rash
• Fatigue
• Nausea
• Diarrhea
• Vomiting
• Cough
• Chills

Drug interactions

• SLCO1B1 Substrates
• axitinib
• boceprevir
• bosutinib
• clarithromycin
• cobicistat
• conivaptan
• dienestrol
• enzalutamide
• estradiol
• estrone
• estropipate

Key clinical trials

• A Study Comparing GSK2118436 to Dacarbazine (DTIC) in Previously Untreated Subjects With BRAF Mutation Positive Advanced (Stage III) or Metastatic (Stage IV) Melanoma (PHASE3)
• Dabrafenib Plus Trametinib vs Vemurafenib Alone in Unresectable or Metastatic BRAF V600E/K Cutaneous Melanoma (PHASE3)
• Study to Evaluate Treatment of Dabrafenib Plus Trametinib in Subjects With BRAF Mutation-Positive Melanoma That Has Metastasized to the Brain (PHASE2)
• Efficacy and Safety of the Combination Therapy of Dabrafenib and Trametinib in Subjects With BRAF V600E- Mutated Rare Cancers (PHASE2)
• Study of Selective BRAF Kinase Inhibitor Dabrafenib Monotherapy Twice Daily and in Combination With Dabrafenib Twice Daily and Trametinib Once Daily in Combination Therapy in Subjects With BRAF V600E Mutation Positive Metastatic (Stage IV) Non-small Cell Lung Cancer. (PHASE2)
• A Study Comparing Trametinib and Dabrafenib Combination Therapy to Dabrafenib Monotherapy in Subjects With BRAF-mutant Melanoma (PHASE3)
• A Study of GSK2118436 in BRAF Mutant Metastatic Melanoma to the Brain (PHASE2)
• Testing the Addition of Navitoclax to the Combination of Dabrafenib and Trametinib in People Who Have BRAF Mutant Melanoma (PHASE1,PHASE2)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Tafinlar CI brief — competitive landscape report
• Tafinlar updates RSS · CI watch RSS
• Novartis portfolio CI