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Dabrafenib + Trametinib

  •  
    Oral
    Dabrafenib + Trametinib
    Tafinlar + Mekinist 
    • 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.
      MEK inhibitors bind to MEK, which is downstream of BRAF.

Clinical Use

    • Indications
    • Unresectable stage III or metastatic (stage IV) melanoma with BRAF (V600) mutation
    • Adjuvant treatment of melanoma with BRAF (V600) mutation and lymph node involvement
    • Adverse Effects
    • Paradoxically have less side effects than BRAF inhibitors alone.
    • Rash
    • Alopecia
    • Hyperkeratosis
    • Visual disturbance
    • Photosensitivity
    • Papillomas / squamous cell carcinomas
    • Nausea / vomiting / diarrhoea
    • Arthralgia / myalgia
    • Headache

Potential Indications
BETA

Associated Adverse Effects
BETA

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