Clinical experience with MEK inhibitors and future developments

Aberrant activation of the RAS–RAF–MEK–ERK pathway occurs in more than 30% of human cancers. As part of this pathway, MEK1 and MEK2 have crucial roles in tumorigenesis, cell proliferation and inhibition of apoptosis. Highly selective and potent MEK inhibitors have been developed and assessed in numerous clinical studies. However, only hints of antitumour activity have been seen in tumours other than melanoma. In an article published in the Nature Reviews Clinical Oncology, Drs Yujie Zhao and Alex Adjei of the Roswell Park Cancer Institute in Buffalo, NY, USA review MEK1/2 signalling, activity of MEK inhibitors and common toxic effects. Read more here.