Current Topics in Medicinal Chemistry

Author(s): Roger A. Smith, Jacques Dumas, Lila Adnane and Scott M. Wilhelm

DOI: 10.2174/156802606777812077

Recent Advances in the Research and Development of RAF Kinase Inhibitors

Page: [1071 - 1089] Pages: 19

  • * (Excluding Mailing and Handling)

Abstract

The RAS-RAF-MEK-ERK signaling pathway (ERK pathway) plays a key role in tumorigenesis and cancer progression. Mutations of RAS or B-RAF lead to a constitutive activation of the ERK pathway, which ultimately results in increased cell division, and cell survival. This review article focuses on the recent literature related to ERK pathway inhibitors, with a particular emphasis on RAF kinase inhibitors. Preclinical and clinical data for the RAF kinase inhibitor sorafenib (BAY 43-9006 tosylate), that was recently approved in the US for the treatment of advanced renal cell carcinoma, are also outlined.

Keywords: Sorafenib, BAY 43-9006, RAF-1, C-RAF, B-RAF, kinase inhibitor, MAP kinase