Sitagliptin and metformin hydrochloride

Mechanism of action

DPP-4 inhibitor + biguanide (fixed-dose combination)

In plain language

Combines two diabetes medicines in one tablet: sitagliptin, which helps the body release more of its own insulin after meals, and metformin, which tells the liver to release less sugar into the blood and helps the body use insulin more effectively.

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ClinicalPlain language

How it works

JANUMET combines sitagliptin, a DPP-4 inhibitor, and metformin hydrochloride, a biguanide. Per the FDA label, sitagliptin slows the inactivation of the incretin hormones GLP-1 and GIP by inhibiting DPP-4, increasing and prolonging their action, which stimulates glucose-dependent insulin release and lowers glucagon secretion. Metformin acts through a separate pathway, decreasing hepatic glucose production, reducing intestinal glucose absorption, and improving peripheral insulin sensitivity, without stimulating insulin secretion itself. The two mechanisms are complementary, which is the basis for combining them in one product.

Therapeutic applications

JANUMET is FDA-indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It should not be used in patients with type 1 diabetes and has not been studied in patients with a history of pancreatitis. Because it contains metformin, JANUMET carries a boxed warning for lactic acidosis, a rare but serious risk of metformin-containing products.

Class

Fixed-dose combination

Therapeutic area

Metabolic / Diabetes

Source

FDA label (DailyMed) ↗