Incretin therapies - highlighting common features and differences in the modes of action of GLP-1 receptor agonists and DPP-4 inhibitors.

Incretin therapies - highlighting common features and differences in the modes of action of GLP-1 receptor agonists and DPP-4 inhibitors.
Diabetes Obes Metab. 2015 Oct 22;
Authors: Nauck M
Abstract
Over the last few years, the incretin-based therapies have emerged as important agents in the treatment of type 2 diabetes (T2D). These agents exert their effect via the incretin system, specifically targeting the receptor for the incretin hormone glucagon-like peptide 1 (GLP-1), which is partly responsible for augmenting glucose-dependent insulin secretion in response to nutrient intake ('incretin effect'). In patients with T2D, pharmacological doses/concentrations of GLP-1 can compensate for the inability of diabetic beta-cells to respond to the main incretin hormone, glucose-dependent insulinotropic polypeptide (GIP), and thus is a suitable parent compound for incretin-based glucose-lowering medications. Two classes of incretin-based therapies are available: GLP-1 receptor agonists (GLP-1RAs) and dipeptidyl peptidase-4 inhibitors (DPP-4Is). GLP-1RAs promote GLP-1 receptor signalling by providing GLP-1 receptor stimulation through 'incretin mimetics' circulating at pharmacological concentrations, whereas DPP-4Is prevent the degradation of endogenously released GLP-1. Both agents produce reductions in plasma glucose and, due to their glucose-dependent mode of action, this is associated with low rates of hypoglycaemia. However, there are d...

Source: Diabetes Metab - October 22, 2015 Category: Endocrinology Authors: Nauck M Tags: Diabetes Obes Metab Source Type: research