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Drug Guide


    Given as monotherapy or in combination with cobimetinib (MEK inhibitor)
  • Mechanism of Action
  • Normally, activation of RAS pathway via receptor tyrosine kinases (RTKs) results in activation of BRAF which then activates MEK, and in turn, ERK.
  • The RAS / RAF / MEK / ERK pathway stimulates cell proliferation and survival.
  • In melanoma with BRAF mutations, the mutant BRAF (most commonly V600E) is constitutionally active.
  • BRAF inhibitors bind to mutant BRAF V600 and, in turn, inhibit cellular proliferation in cells with BRAF mutations.

Clinical Use

  • Indications
  • Unresectable stage III or metastatic (stage IV) melanoma with BRAF (V600) mutation
  • Adverse Effects
  • Rash
  • Alopecia
  • Hyperkeratosis
  • Papillomas / squamous cell carcinomas
  • Nausea / vomiting / diarrhoea
  • Arthralgia / myalgia
  • Headache
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