Drug Guide
 

Vemurafenib + Cobimetinib

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    Oral
    Vemurafenib + Cobimetinib
    Zelboraf + Cotellic 
    • 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
    • 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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