This strategy has been vindicated by the FDA’s approval of three MEK1/2 inhibitors: trametinib in 2013, cobimetinib in 2015, and MEK162/binimetinib in 2018 (in combination with the Raf inhibitors dabrafenib, vemurafenib, and encorafenib, respectively) for the treatment of advanced melanoma with a BRAF V600E or V600K mutation [82–85]. The gene discussed is MAP2K1; the disease is melanoma.