[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/) › Saxagliptin

[Pharmacology](https://durgical.com/en/pharmacology/) · [DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)

# Saxagliptin

A DPP-4 inhibitor metabolized by CYP3A4. It raised heart failure hospitalizations in a large trial, so it is avoided in heart failure.

Updated 2026-11-01

- Class: [DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)
- Enzyme: Dipeptidyl peptidase-4 (DPP-4)
- ATC code: A10BH03

✂**Dipeptidyl peptidase-4 (DPP-4)**Saxagliptin

ⓘ The figure shows saxagliptin (BMS-477118) in the active site of human DPP-4, where it binds the catalytic serine covalently and reversibly.

**Target in 3D:** Dipeptidyl peptidase-4 (DPP-4). PDB structure 3BJM (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3BJM) · Drag to rotate · pinch to zoom

## Mechanism of action

Saxagliptin is a cyanopyrrolidine that forms a reversible covalent bond with the catalytic serine of DPP-4. The enzyme stays blocked for long, active GLP-1 and GIP rise after meals, and insulin increases and glucagon falls when glucose is high. Its active metabolite also inhibits DPP-4.

- Blocks the DPP-4 enzyme in plasma and on cells
- Active GLP-1 and GIP last longer after meals
- More insulin and less glucagon when glucose is high
- Glucose falls without weight change

## Pharmacokinetics

**Absorption**
Oral, with or without food.

**Metabolism**
By CYP3A4/5 in the liver to an active metabolite.

**Elimination**
Kidney and liver; the dose is lowered in moderate to severe kidney impairment.

## Indications

- Type 2 diabetes, with diet and exercise [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

## Adverse effects

### Common

- Upper respiratory and urinary tract infections, headache
- Hypoglycemia with insulin or a sulfonylurea

### Serious (rare, important)

- Acute pancreatitis
- Serious allergic reactions: anaphylaxis, angioedema, Stevens–Johnson syndrome
- Bullous pemphigoid
- Severe, disabling joint pain
- Heart failure hospitalization

## Contraindications

- Serious hypersensitivity to saxagliptin
- Not for type 1 diabetes or ketoacidosis

## Key interactions

**Strong CYP3A4/5 inhibitors (ketoconazole, clarithromycin, ritonavir)**
Raise saxagliptin levels; the dose is limited.

**Insulin or sulfonylureas**
Higher risk of hypoglycemia.

## What is monitored

- Kidney function
- Signs of heart failure (weight gain, edema, breathlessness)
- HbA1c

## Administration and safety

- Oral tablet, once a day, with or without food.
- Not given together with a GLP-1 receptor agonist.

## Nursing care

- Before: kidney function, history of pancreatitis and heart failure.
- During: abdominal pain, skin blisters, joint pain, swelling or breathlessness.
- Capillary glucose when combined with insulin or a sulfonylurea.
- Ask about new antifungal, antibiotic or HIV drugs (CYP3A4 inhibitors).

## Pregnancy and breastfeeding

Data in pregnancy are limited; insulin is the usual choice.

## Memory aid

Saxagliptin: 'S' for 'swelling' and 'CYP3A4': the gliptin to avoid in heart failure and to watch with azoles and macrolides.

## Test yourself

Think of the answer, then tap the question to see it.

## Which DPP-4 inhibitor is linked to more heart failure hospitalizations?

Saxagliptin, in a large cardiovascular outcomes trial.

## Why does ketoconazole matter for saxagliptin?

It strongly inhibits CYP3A4, the enzyme that metabolizes saxagliptin, raising its levels.

## How does saxagliptin bind DPP-4?

Through a reversible covalent bond with the catalytic serine of the enzyme.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/saxagliptin/)

## Related drugs

- [Sitagliptin](https://durgical.com/en/pharmacology/sitagliptin/)
- [Linagliptin](https://durgical.com/en/pharmacology/linagliptin/)
- [Vildagliptin](https://durgical.com/en/pharmacology/vildagliptin/)

## Related conditions

- [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

[← Back to the class: DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Saxagliptin: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a610003.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - SAXAGLIPTIN tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e286ffd4-c598-47fb-af06-2e15f7e6f99f) (DailyMed (U.S. National Library of Medicine), 2026); [Crystal structure of human DPP-IV in complex with (1S,3S, 5S)-2-[(2S)-2-AMINO-2-(3-HYDROXYTRICYCLO[3.3.1.13,7]DEC-1- YL)ACETYL]-2-AZABICYCLO[3.1.0]HEXANE-3-CARBONITRILE (CAS), (1S,3S,5S)-2-((2S)-2-AMINO-2-(3-HYDROXYADAMANTAN-1- YL)ACETYL)-2-AZABICYCLO[3.1.0]HEXANE-3-CARBONITRILE (IUPAC), OR BMS-477118](https://www.rcsb.org/structure/3BJM) (RCSB Protein Data Bank, 2008); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BH03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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