Recent developments in the discovery of MCH-1R antagonists for the treatment of obesity – an update

Since the discovery and characterisation of melanin-concentrating hormone (MCH) and its role in the regulation of food intake and energy expenditure, there has been increasing interest in this cyclic peptide. The identification of the MCH-1 receptor (MCH-1R) in 1999 initiated the search for small molecules that could block the effects of MCH and provide novel agents for the treatment of obesity. A large number of companies is now actively pursuing MCH-1R antagonists and a wide range of structural types have been reported. Several compounds have been reported to be efficacious in rodent models of obesity and two compounds have recently entered into human clinical trials.