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Sitagliptin (Januvia)

National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) · 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.

At a glance

Generic nameSitagliptin (Januvia)
Also known asJanuvia
SponsorNational Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Drug classDPP-4 inhibitor
TargetDPP-4 (dipeptidyl peptidase-4)
ModalitySmall molecule
Therapeutic areaDiabetes
PhaseFDA-approved

Mechanism of action

By blocking DPP-4, sitagliptin prolongs the activity of GLP-1 and GIP, incretin hormones that stimulate insulin release when blood glucose rises. This mechanism is glucose-dependent, meaning it primarily works when blood sugar is elevated, reducing the risk of hypoglycemia. The drug improves glycemic control without causing weight gain and is generally well-tolerated.

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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