GPR119 agonists for type 2 diabetes: past failures and future hopes for preclinical and early phase candidates

Abstract

Introduction: Type 2 diabetes (T2D) is metabolic disorder associated with a decrease in insulin activity and/or secretion from the β-cells of the pancreas, leading to elevated circulating glucose. Current management practices for T2D are complex with varying long-term effectiveness. Agonism of the G protein-coupled receptor GPR119 has received a lot of recent interest as a potential T2D therapeutic. Areas covered: This article reviews studies focused on GPR119 agonism in animal models of T2D and in patients with T2D. Expert opinion: GPR119 agonists in vitro and in vivo can potentially regulate incretin hormone release from the gut, then pancreatic insulin release which regulates blood glucos..