A Comprehensive Pharmacological and Clinical Monograph on Teneligliptin

1.0 Executive Summary

Teneligliptin is a third-generation, orally administered dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the management of type 2 diabetes mellitus (T2DM). It is distinguished by a unique, rigid, "J-shaped" molecular structure that confers high potency and a prolonged duration of action, with a terminal half-life of approximately 24 hours, permitting a convenient once-daily dosing regimen.[1]

The primary mechanism of action involves the selective and competitive inhibition of the DPP-4 enzyme. This action prevents the degradation of endogenous incretin hormones, principally glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). The resulting elevation in active incretin levels enhances glucose-dependent insulin secretion from pancreatic β-cells and suppresses glucagon release from α-cells, leading to improved glycemic control with a low intrinsic risk of hypoglycemia.[3]

A defining characteristic of Teneligliptin is its unique pharmacokinetic profile, featuring balanced, dual elimination pathways. The drug is metabolized by hepatic enzymes (cytochrome P450 3A4 and flavin-containing monooxygenase 3) and is also excreted unchanged via the kidneys.[1] This dual route of clearance is a significant clinical advantage, as it obviates the need for dose adjustments in patients with any degree of renal impairment, including those with end-stage renal disease (ESRD) requiring dialysis.[7]