Tafinlar (dabrafenib)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Company:

Approval Status:

Approved May 2013

Specific Treatments:

unresectable or metastatic melanoma with BRAF V600E mutation

Therapeutic Areas

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General Information

Tafinlar (dabrafenib) is an inhibitor of some mutated forms of BRAF kinases, as well as wild-type BRAF and CRAF kinases. 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.

Tafinlar is specifically indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. Tafinlar is not indicated for treatment of patients with wild-type BRAF melanoma.

Tafinlar is supplied as a capsule for oral administration. The recommended dose is 150 mg orally taken twice daily, approximately 12 hours apart, until disease progression or unacceptable toxicity occurs. Take either at least 1 hour before or at least 2 hours after a meal. A missed dose can be taken up to 6 hours prior to the next dose.

Clinical Results

FDA Approval
The FDA approval of Tafinlar was based on an international, multicenter, randomized, open-label, active-controlled trial conducted in 250 patients with previously untreated BRAF V600E mutation-positive, unresectable or metastatic melanoma. Patients with any prior use of BRAF inhibitors or MEK inhibitors were excluded. Patients were randomized to receive Tafinlar 150 mg by mouth twice daily (n = 187) or dacarbazine 1,000 mg/m2 intravenously every 3 weeks (n = 63). The primary endpoint was progression free survival (PFS). The number of PFS events occurred in 42% of the Tafinlar arm versus 65% of the dacarbazine arm. The median number of months to progression was 5.1 versus 2.7 months.(p <0.0001)

Side Effects

Adverse events associated with the use of Tafinlar may include, but are not limited to, the following:

  • hyperkeratosis
  • headache
  • pyrexia
  • arthralgia
  • papilloma
  • alopecia
  • palmar-plantar erythrodysesthesia syndrome

Mechanism of Action

Tafinlar (dabrafenib) is an inhibitor of some mutated forms of BRAF kinases, as well as wild-type BRAF and CRAF kinases. 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.

Literature References

Hauschild A, Grob JJ, Demidov LV, Jouary T, Gutzmer R, Millward M, Rutkowski P, Blank CU, Miller WH Jr, Kaempgen E, Martín-Algarra S, Karaszewska B, Mauch C, Chiarion-Sileni V, Martin AM, Swann S, Haney P, Mirakhur B, Guckert ME, Goodman V, Chapman PB Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 2012 Jul 28;380(9839):358-65.

Additional Information

For additional information regarding Tafinlar or melanoma with BRAF mutations, please visit the Tafinlar web page.