Despite about half a dozen distinct targets having been innovated and introduced in the market for the oral treatment of Type 2 diabetes, ~60% of diabetics still exhibit progressive worsening of glycemic control and ~half of them end up with daily insulin. Increasing epidemiology of Type 2 diabetes due to genetic/lifestyle changes, as well as micro/macrovascular (CV) complication associated with diabetes, demands the researcher to find newer options for treating diabetes which can address other consequences along with HbA1c reduction. Selective PPAR agonists, DGAT1 (diglyceride Acyltransferase 1) inhibitors, GPR (G-protein receptor) agonist, Glucokinase inhibitors are some of the early targets which are in clinical development and have the potential to come into the clinic in the next decade.

Amongst these novel targets, a few candidates from GPR (G-protein couple receptors) agonist are nearing late stage development. Ability to directly modulate insulin and GLP-1 secretion in glucose depended manner is the key trait of this class. Through this, GPR agonist controls hyperglycemia without hypoglycemia, and provides weight loss advantage. Recent publications suggest GPR agonist have complementary action with DPP-IV inhibitors. This report discuss in details about the merits/demerits of developing GPR agonist, pipeline GPR agonist together with sales estimate of key pipeline candidate through 2020 across the world.