Fixed-dose combination: DPP-4 inhibitor plus biguanide
ATC code: A10BD07 (Sitagliptin and metformin)
Sitagliptin inhibits DPP-4 and prolongs endogenous GLP-1 and GIP action – glucose-dependent insulin secretion rises and glucagon falls. Metformin lowers hepatic gluconeogenesis and improves insulin sensitivity. TECOS (NEJM 2015) confirmed sitagliptin's cardiovascular safety: neutral MACE effect.
Second line
Type 2 diabetes in adults with above target on metformin monotherapy. Per / 2024 and redGDPS 2024, second-line when ASCVD, HF, and CKD are absent. Dose: 50/850, 50/1000 mg twice daily with meals (Janumet) or 100/1000 mg once daily (Janumet XR). HbA1c at 3 months. With ASCVD, HFrEF, or CKD, GLP-1 RA or SGLT2 inhibitor takes priority.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Metformin is permitted in pregnancy for type 2 diabetes or gestational diabetes. Sitagliptin is not studied – switch to insulin.
Metformin is compatible with breastfeeding (RID 0.28-0.65%, Hale L1). No milk data for sitagliptin – prefer metformin monotherapy or insulin in nursing women.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Sitagliptin + Metformin is evaluated for the following indications with varying evidence strength: Type 2 diabetes mellitus (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Sitagliptin + Metformin (≥ 1 in 100): Nausea, diarrhea, metallic taste (metformin), Headache, Nasopharyngitis, Hypoglycemia when combined with sulfonylurea or insulin. See the Safety section for uncommon and serious reactions.
FDA category B. Metformin is permitted in pregnancy for type 2 diabetes or gestational diabetes. Sitagliptin is not studied – switch to insulin.
Metformin is compatible with breastfeeding (RID 0.28-0.65%, Hale L1). No milk data for sitagliptin – prefer metformin monotherapy or insulin in nursing women.
Sitagliptin + Metformin is contraindicated in: Hypersensitivity; Type 1 diabetes; Diabetic ketoacidosis; Severe renal impairment (CrCl <30); Acute conditions with renal risk (dehydration, shock, sepsis). Full list in the Safety section.