Discovery of Trametinib, the First-in-Class MEK Inhibitor
2018 Volume 28 Issue 2 Pages 71-76
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2018 Volume 28 Issue 2 Pages 71-76
Trametinib is a highly potent, highly selective allosteric inhibitor of MEK1 and MEK2. This compound was licensed to GSK from JT in 2006, and then it was approved in the U.S. as a first-in-class MEK inhibitor in 2013, and was also approved in Japan in 2016. Although a drug discovery research of trametinib has already been published in MEDCHEM NEWS Vol.27 No.3, we would like to supplement it from a chemistry perspective since we have received the Breakthrough Award, Division of Medicinal Chemistry, PSJ.
