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DPP4 inhibitor

AstraZeneca · FDA-approved active Small molecule

DPP4 inhibitors block the enzyme dipeptidyl peptidase-4, which prolongs the activity of incretin hormones that stimulate insulin secretion in response to glucose.

DPP4 inhibitors block the enzyme dipeptidyl peptidase-4, which prolongs the activity of incretin hormones that stimulate insulin secretion in response to glucose. Used for Type 2 diabetes mellitus.

At a glance

Generic nameDPP4 inhibitor
Also known asSitagliptin, Januvia, Janumet, Ristaben, Tesavel
SponsorAstraZeneca
Drug classDPP4 inhibitor
TargetDPP4 (dipeptidyl peptidase-4)
ModalitySmall molecule
Therapeutic areaDiabetes
PhaseFDA-approved

Mechanism of action

DPP4 inhibitors work by inhibiting the degradation of GLP-1 and GIP, incretin hormones released after meals that enhance glucose-dependent insulin secretion and suppress glucagon. By preventing the breakdown of these hormones, DPP4 inhibitors increase their circulating levels and duration of action, leading to improved glycemic control in type 2 diabetes. This mechanism is glucose-dependent, meaning insulin is only stimulated when blood glucose is elevated, reducing hypoglycemia risk.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results