Sitagliptin / Metformin Hydrochloride

What it is and how it works

Mechanism of Action ZITUVIMET ZITUVIMET combines two antihyperglycemic agents with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes mellitus: sitagliptin, a DPP- 4 inhibitor, and metformin HCl, a member of the biguanide class. Sitagliptin Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones.

Mechanism class: Dipeptidyl Peptidase 4 Inhibitors

Indications

is a combination of sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and metformin hydrochloride (HCl), a biguanide, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use: ZITUVIMET is not recommended in patients with type 1 diabetes mellitus. ZITUVIMET has not been studied in patients with a history of pancreatitis. ZITUVIMET is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use ZITUVIMET is not recommended in patients with type 1 diabetes mellitus. ZITUVIMET has not been studied in patients with a history of pancreatitis. It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using ZITUVIMET. .

Dosage and administration (summary)

Take ZITUVIMET orally twice daily with meals. Individualize the dosage of ZITUVIMET on the basis of the patient's current regimen, effectiveness, and tolerability. The maximum recommended daily dose is 100 mg of sitagliptin and 2,000 mg of metformin HCl. The recommended starting dose in patients not currently treated with metformin is 50 mg sitagliptin and 500 mg metformin HCl twice daily, with gradual dose escalation recommended to reduce gastrointestinal side effects associated with metformin. The starting dose in patients already treated with metformin should provide sitagliptin dosed as 50 mg twice daily (100 mg total daily dose) and the dose of metformin already being taken.

Contraindications

Severe renal impairment: (eGFR below 30 mL/min/1.73 m 2 ) Metabolic acidosis, including diabetic ketoacidosis. History of a serious hypersensitivity reaction to ZITUVIMET, sitagliptin, or metformin, such as anaphylaxis or angioedema. ZITUVIMET is contraindicated in patients with: Severe renal impairment (eGFR below 30 mL/min/1.73 m 2 ) . Acute or chronic metabolic acidosis, including diabetic ketoacidosis.

Warnings and precautions

Lactic Acidosis: See boxed warning . Pancreatitis: There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue ZITUVIMET. Heart Failure : Has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of ZITUVIMET in patients who have known risk factors for heart failure. Monitor patients for signs and symptoms. Acute Renal Failure: Has been reported postmarketing, sometimes requiring dialysis.

Pregnancy

Pregnancy Risk Summary Available data with ZITUVIMET and sitagliptin use in pregnant women are not sufficient to inform a ZITUVIMET-associated or sitagliptin-associated risk for major birth defects and miscarriage.

Storage and supply

Tablets supplied as follows: Contents Description How Supplied NDC 50 mg sitagliptin and 500 mg metformin HCl White to off-white, oval shaped, biconvex, film coated tablets debossed with "1786" on one side and plain on the other side. Bottles of 60 tablets with child-resistant closure.

Source: Sitagliptin And Metformin Hydrochloride (Zituvimet) — US FDA prescribing information, 2026-08-12, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.