Model depicting the dual mechanism-of-action of GPR40 (FFAR1) full agonists to lower blood glucose levels.

<p>GPR40 full agonists engage both the enteroendocrine axis as well as the pancreatic β-cell axis. These pathways both lead to augmentation of glucose stimulated insulin secretion on the pancreatic β-cell. Additionally, GLP-1 has multiple physiological and pharmacological roles, such as inhibition of glucagon secretion, that could further benefit type 2 diabetics. GPR40 partial agonists such as AMG 837 engage only the pancreatic pancreatic β-cell axis <i>in vivo</i>.