Saxagliptin

Dipeptidyl Peptidase 4 (DPP 4) InhibitorRx: PrescriptionCompound: Approved

Also known as: BMS-477118, Kombiglyze XR, Onglyza, saxagliptin hydrochloride

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Saxagliptin is an orally active DPP-4 inhibitor approved for the treatment of type 2 diabetes mellitus as an adjunct to diet and exercise. It is marketed under the brand name Onglyza and improves glycemic control via incretin-based mechanisms.

Mechanism of Action

Competitively inhibits dipeptidyl peptidase-4 (DPP-4), preventing the degradation of incretin hormones GLP-1 and GIP, thereby increasing their active concentrations, enhancing glucose-dependent insulin secretion, and suppressing glucagon release from the pancreas.

Routes of Administration

Oral

Goals & Uses

  • Reduction of postprandial hyperglycemiaMetabolic / EndocrineHigh
  • Weight neutralityBody CompositionModerate
  • Low hypoglycemia riskSafety / TolerabilityHigh
  • Glycemic control in type 2 diabetesMetabolicHigh
  • Combination therapy with metforminMetabolic / EndocrineHigh

Contraindications

  • Diabetic ketoacidosisMetabolicHigh
  • Type 1 diabetes mellitusEndocrineHigh
  • History of serious hypersensitivity to saxagliptinAllergic / ImmunologicHigh
  • Heart failure (NYHA class III–IV)CardiovascularModerate

Adverse Effects

  • PancreatitisGastrointestinalRareInflammation of the pancreas
  • Heart failure hospitalizationCardiovascularUncommon
  • Urinary tract infectionGenitourinaryCommon
  • Upper respiratory tract infectionInfectiousCommon
  • Hypoglycemia (when combined with insulin or sulfonylurea)MetabolicCommon
  • AngioedemaImmunologicRare

Drug Interactions

  • Insulin or insulin secretagogues (sulfonylureas)Moderate
  • CYP3A4/5 inducers (e.g., rifampin, carbamazepine)Moderate
  • Strong CYP3A4/5 inhibitors (e.g., ketoconazole, clarithromycin, atazanavir)Moderate
  • ACE inhibitorsLow

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Hepatic impairment (severe)HepaticRelative
  • Pediatric patients (<18 years)AgeAbsolute
  • Heart failure (established)CardiovascularRelative
  • Renal impairment (eGFR ≤50 mL/min/1.73m²)RenalRelative

Regulatory Status

  • European UnionApprovedApproved: Type 2 diabetes mellitus in adults — as monotherapy or add-on combination therapyEMA approved October 1, 2009 (Onglyza). Also approved as Komboglyze (saxagliptin/metformin).
  • United StatesApprovedApproved: Type 2 diabetes mellitus — adjunct to diet and exercise to improve glycemic control in adultsFDA approved July 31, 2009. Available as Onglyza (monotherapy) and Kombiglyze XR (with metformin XR). Label includes heart failure hospitalization warning.
  • United KingdomApprovedApproved: Type 2 diabetes mellitus in adultsApproved via EMA prior to Brexit; continued approval maintained under MHRA post-Brexit.

FDA approved in 2009. EMA approved in 2009. Post-marketing cardiovascular outcomes trial (SAVOR-TIMI 53) showed a possible increased risk of heart failure hospitalization; label carries a warning for this risk.

Evidence & Sources

No sources recorded yet.

Browse All PeptidesBuild My Stack