Saxagliptin
Also known as: BMS-477118, Kombiglyze XR, Onglyza, saxagliptin hydrochloride
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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
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.
Frequently Asked Questions
What is Saxagliptin?
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.
What is Saxagliptin used for?
Saxagliptin is educationally associated with: Reduction of postprandial hyperglycemia, Weight neutrality, Low hypoglycemia risk, Glycemic control in type 2 diabetes, Combination therapy with metformin. Educational only — not medical advice.
How is Saxagliptin administered?
Recorded routes of administration: Oral.
What are the potential side effects of Saxagliptin?
Reported adverse effects include: Pancreatitis, Heart failure hospitalization, Urinary tract infection, Upper respiratory tract infection, Hypoglycemia (when combined with insulin or sulfonylurea), Angioedema. This list is not exhaustive — consult a qualified clinician.
Who should avoid Saxagliptin?
Recorded contraindications: Diabetic ketoacidosis, Type 1 diabetes mellitus, History of serious hypersensitivity to saxagliptin, Heart failure (NYHA class III–IV). Consult a qualified clinician before use.