Therapeutic Application of GPR119 Ligands in Metabolic Disorders

GPR119 belongs to the G protein‐coupled receptor family and exhibits dual modes of action upon ligand‐dependent activation: pancreatic secretion of insulin in a glucose‐dependent manner and intestinal secretion of incretins. Hence, GPR119 has emerged as a promising target for treating type 2 diabetes mellitus without causing hypoglycaemia. However, despite continuous efforts by many major pharmaceutical companies, no synthetic GPR119 ligand has been approved as a new class of anti‐diabetic agents thus far, nor has any passed beyond phase II clinical studies. Herein, we summarize recent advances in research concerning the physiological/pharmacological effects of GPR119 and its synthetic ligands on the regulation of energy metabolism, and we speculate on future applications of GPR119 ligands for the treatment of metabolic diseases, focusing on non‐alcoholic fatty liver disease.