MEK1/2, the third component within the RAS-RAF-MEK-ERK cascade known as the “classical” MAPK oncology pathway, acts as the intermediary in transmitting signals from RAS and RAF to ERK, thereby modulating critical cellular processes such as survival and proliferation. Consequently, MEK1/2 has emerged as a promising target for cancer therapy. Currently, four MEK inhibitors have received regulatory approval for the treatment of various cancers, while more than 19 MEK inhibitors have been or are currently undergoing clinical development. It is worth noting that these known MEK inhibitors exhibit substantial structural similarity, with only a few exceptions such as E6201 serving as outliers.
