Ghrelin receptor modulators: a patent review (2011-2014)

Introduction: Over the past three years, several patents appeared dealing with the discovery of compounds able to modulate ghrelin actions: agonists for the treatment of cachexia, as diagnostic agents for GH deficiency or for the increase in gastrointestinal motility, antagonists and inverse agonists as anorexigenic agents for the treatment of obesity and type 2 diabetes. These researches have been conducted by several pharmaceutical companies and some compounds have entered clinical trial, but, to date, compounds acting on the ghrelin receptor do not represent clinical options yet. Areas covered: A comprehensive description and categorization of patents related to each type of compounds is provided, together with data related to these compounds that appeared in the scientific literature. Expert opinion: Ghrelin appears to mediate a myriad of actions, and some of these appear to be due to unknown mechanisms (a second putative ghrelin receptor, putative receptors for unacylated ghrelin); several agonists, antagonists and inverse agonists at the ghrelin receptor have been developed but their mechanism of action into CNS is poorly understood. The therapeutic potential of compounds acting on ghrelin receptor is still to be fully assessed, but the results obtained to date are encouraging for the successful clinical translation of compounds able to treat several pathologies.