nerigliatin

Nerigliatin (PF-04937319) is a small molecule, partial glucokinase activator (GKA) developed by Pfizer for the treatment of type 2 diabetes mellitus. It acts as a dual-acting agent, targeting the glucokinase enzyme in both the liver and the pancreas. By increasing the enzyme's affinity for glucose, nerigliatin enhances glucose-stimulated insulin secretion from pancreatic beta cells and promotes hepatic glucose uptake and glycogen synthesis. This dual mechanism aims to improve glycemic control while minimizing the risk of hypoglycemia, a common side effect of full glucokinase activators. Although the drug reached Phase 2 clinical development and was evaluated in various populations, including Japanese subjects, Pfizer ultimately discontinued its development for type 2 diabetes mellitus.

Other names

nerigliatin