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Dabrafenib + Trametinib

 
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    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
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