MEK inhibitors: a patent review 2008 – 2010

Abstract

Introduction: MAPK/extracellular signal-regulated kinase (MEK) inhibitors target the Ras/Raf/MEK/ERK signaling pathway, which is important in cell growth, differentiation and development. The pathway has been implicated in the progression of a variety of diseases, in particular cancer, as well as in immune and inflammatory diseases such as rheumatoid arthritis, organ transplant rejection, septic shock, asthma and viral infection.

Areas covered: A comprehensive review of the patent literature (2008 – 2010) covering MEK inhibitors and combinations thereof is provided in this paper.

Expert opinion: The first MEK inhibitor was described in the literature in 1995, and several companies are still active in the research and development of MEK inhibitors for various disease states. The emerging role of MEK inhibitors in disease has prompted further investigations of this important target. The combination of MEK inhibitors with other agents/therapies in the treatment of diseases, particularly cancer, is a key development in the field.

Keywords::

• ARRY-162 (ARRY-438162)
• AS703026 (MSC1936369B)
• AZD6244 (ARRY-142866)
• AZD8330 (ARRY424704)
• BAY869766 (RDEA119)
• cancer
• CI-1040
• CI-1040/PD-184352
• extracellular signal-regulated kinase
• GSK1120212 (JTP-74057)
• GSK2118436
• MAPK
• MEK
• MEK inhibitor
• MEK1
• MEK2
• PD-0325901
• Ras/Raf/MEK/ERK
• RO4987655 (CH4987655)
• RO5068760
• RO5126766
• TAK-733
• XL518 (GDC0973)

Notes