Recent advances of MEK inhibitors and their clinical progress

Curr Top Med Chem. 2007;7(14):1364-78. doi: 10.2174/156802607781696837.


The RAS/RAF/MEK/ERK signaling pathway has been a major clinical focus in oncology research in recent years. A clearer association of B-RAF mutations to cancers such as melanoma, papillary thyroid cancer and others has brought an increasing interest in chemotherapeutics that target this cellular signaling pathway. In this review, the authors summarize the current understanding of science and therapeutic use of the MEK inhibitors targeting the RAS/RAF/ MEK/ERK pathway. Clinical progresses of PD0325901 and AZD6244 are highlighted in addition to developments of new MEK inhibitors. Recently disclosed MEK inhibitors in two sub-divided classes, ATP noncompetitive and ATP competitive inhibitors are discussed.

Publication types

  • Review

MeSH terms

  • Adenosine Triphosphate / antagonists & inhibitors
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Drug Design
  • Humans
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Signal Transduction / drug effects


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Adenosine Triphosphate
  • Mitogen-Activated Protein Kinases