What is the Origin of DPP-4 Inhibition?

The concept arose from the discovery of incretin hormones and the subsequent identification of DPP-4 as the key enzyme responsible for their rapid inactivation following secretion from the gut. The development of small-molecule inhibitors to target this enzyme represents a targeted therapeutic innovation. This strategy capitalizes on the body's own physiological mechanisms to enhance insulin secretion and improve metabolic control.

What is the Mechanism of DPP-4 Inhibition?

The DPP-4 enzyme normally cleaves the active forms of incretin hormones, rendering them inactive within minutes of release after a meal. By introducing a DPP-4 inhibitor, the enzyme's binding site is blocked, leading to elevated and sustained circulating concentrations of active incretins. This prolonged action enhances glucose-dependent insulin secretion from the pancreas, suppresses inappropriate glucagon release, and slows gastric emptying, resulting in a clinically significant improvement in postprandial and fasting glucose levels.

DPP-4 Inhibition ∞ Area

DPP-4 Inhibition

Meaning

DPP-4 Inhibition is a pharmacological strategy that involves administering an agent to block the enzymatic activity of Dipeptidyl Peptidase-4, a widespread enzyme that rapidly degrades specific peptide hormones. In the context of metabolic health, this inhibition is used to prevent the breakdown of naturally occurring incretin hormones, such as Glucagon-like peptide-1, thereby prolonging their beneficial effects on glucose homeostasis. This therapeutic approach is a cornerstone in the management of type 2 diabetes.