Last reviewed 2026-04-23 · How we verify

Saxagliptin plus metformin IR

Saxagliptin inhibits dipeptidyl peptidase-4 (DPP-4) to increase incretin levels and lower blood glucose, while metformin reduces hepatic glucose production and improves insulin sensitivity.

Saxagliptin inhibits dipeptidyl peptidase-4 (DPP-4) to increase incretin levels and lower blood glucose, while metformin reduces hepatic glucose production and improves insulin sensitivity. Used for Type 2 diabetes mellitus.

At a glance

Mechanism of action

Saxagliptin is a DPP-4 inhibitor that prevents the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), thereby enhancing insulin secretion in response to meals and reducing glucagon secretion. Metformin is a biguanide that decreases hepatic glucose output and increases peripheral glucose uptake and utilization. Together, they provide complementary mechanisms for glycemic control in type 2 diabetes.

Approved indications

• Type 2 diabetes mellitus

Common side effects

• Hypoglycemia
• Nasopharyngitis
• Urinary tract infection
• Headache
• Gastrointestinal disturbance (metformin-related)

Key clinical trials

• Evaluate the Efficacy and Safety of Saxagliptin in Combination With Metformin IR Compared to Saxagliptin Monotherapy and to Metformin IR Monotherapy in Drug Naive Chinese Subjects With Type 2 Diabetes Who Have Inadequate Glycaemic Control (PHASE3)
• Study to Evaluate the Efficacy, Safety, Tolerability, and Pharmacokinetics of Saxagliptin as Monotherapy in Pediatric Patients With Type 2 Diabetes (PHASE3)
• A Multicenter, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of Saxagliptin (BMS-477118) in Combination With Metformin IR or Metformin XR in Pediatric Patients With Type 2 Diabetes Who Have Inadequate Glycemic Control on Metformin Alone (PHASE3)
• Safety and Efficacy of Dapagliflozin in Triple Therapy to Treat Subjects With Type 2 Diabetes (PHASE3)
• Safety and Efficacy of Saxagliptin in Triple Therapy to Treat Subjects With Type 2 Diabetes (PHASE3)
• Study of Saxagliptin, 5-Hydroxy Saxagliptin, and Metformin Concentrations/Levels in Pediatric Subjects With T2DM (PHASE1)
• Efficacy and Safety Study of Saxagliptin + Metformin Immediate Release (IR) Versus Metformin IR Alone in Type 2 Diabetes Mellitus (PHASE3)
• Bioequivalence Study of Saxagliptin and Glucophage Combination Formulations in Healthy Subjects (A) (PHASE1)

Primary sources

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