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Sitagliptin - DPP4i

Royal Devon and Exeter NHS Foundation Trust · FDA-approved active Small molecule

Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down incretin hormones, thereby increasing insulin secretion and reducing glucagon in response to meals.

Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down incretin hormones, thereby increasing insulin secretion and reducing glucagon in response to meals. Used for Type 2 diabetes mellitus as monotherapy or in combination with other antidiabetic agents.

At a glance

Generic nameSitagliptin - DPP4i
Also known asJanuvia
SponsorRoyal Devon and Exeter NHS Foundation Trust
Drug classDPP-4 inhibitor
TargetDPP-4 (dipeptidyl peptidase-4)
ModalitySmall molecule
Therapeutic areaDiabetes
PhaseFDA-approved

Mechanism of action

DPP-4 inhibitors work by prolonging the action of endogenous GLP-1 and GIP, which are incretin hormones released after nutrient intake. By blocking their degradation, sitagliptin enhances glucose-dependent insulin secretion and suppresses glucagon secretion, leading to improved glycemic control. This mechanism is glucose-dependent, meaning it primarily works 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

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