The therapeutic potential of GPR120: a patent review

Abstract

Introduction: Type 2 diabetes (T2D) is a complex metabolic disorder characterized by persistent hyperglycemia and a wide range of underlying metabolic defects. The prevalence and incidence of T2D are expected to dramatically increase in the near-future and consequently, there is a significant medical need for diabetes care. Many targets are under investigation to lower the plasma glucose levels or increase the insulin sensitivity. Despite newer drug classes emerging as viable long-term treatment options for the management of T2D, achieving an optimal glycemic control along with sufficient effectiveness over the course of the disease remains a challenge. In this regard, among several G-protein-coupled receptors (GPCRs), GPR120 and GPR40 have recently been considered as viable targets for diabetes and metabolic disorders.

Areas covered: This article reviews the current literature on the discovery and development of GPR120 agonists in diabetes and metabolic disorders and updates on the published patents in this field. The patent study for this review has been carried out using multiple electronic databases including SciFinder and Thomson Reuters Integrity.

Expert opinion: A paradigm shift in the treatment of diabetes is needed, wherein a single therapeutic agent could target diabetes and its associated disorders such as high plasma glucose level and inflammation, with excellent safety and tolerability profile. In this regard, agonists of GPR120 or dual-agonist GPR120 and GPR40 are highly anticipated as therapeutic approaches for the treatment of diabetes on the basis of their novel glucose-dependent mechanism of action.

Keywords::

• diabetes
• GLP-1
• GPR120
• GPR40
• G-protein-coupled receptors
• GSIS
• inflammation
• insulin
• metabolic disorders
• obesity

Acknowledgements

We are thankful to S Buch and R Sharma for their critical comments and review of the manuscript. We also thank S Mukherjee and N Dubash for their stimulating discussions and feedback on this manuscript.

Notes

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