- OralVemurafenibZelborafGiven 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.
- Adverse Effects