pharmacopeia
GET
/api/v1/drug/saxagliptin
2D structure
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
SMILES C1[C@@H]2C[C@@H]2N([C@@H]1C#N)C(=O)[C@H](C34CC5CC(C3)CC(C5)(C4)O)N
InChIKey QGJUIPDUBHWZPV-SGTAVMJGSA-N

Mechanism of action

Sourced from openFDA

Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the DPP-4 enzyme within minutes.

Dipeptidyl Peptidase 4

Indications

Sourced from openFDA
  • Saxagliptin tablets are a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ( 1.1 ) Limitations of use: • Not recommended for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.ICD-10: E10.9, E11.9

Contraindications

Sourced from openFDA
  • Saxagliptin tablets are contraindicated in patients with a history of a serious hypersensitivity reaction to saxagliptin or any of the ingredients in saxagliptin tablets. Reactions such as anaphylaxis, angioedema, or exfoliative skin conditions have been reported with saxagliptin tablets [ see Warnings and Precautions (5.4) and Adverse Reactions (6.2) ].contraindicated

Dosage & administration

Sourced from openFDA

• Recommended dosage is 2.5 mg or 5 mg orally once daily taken regardless of meals. ( 2.1 ) • Patients with an eGFR < 45 mL/min/1.73 m 2 (moderate or severe renal impairment, or end-stage renal disease): Recommended dosage is 2.5 mg once daily regardless of meals. ( 2.2 ) • Assess renal function before starting saxagliptin tablets and periodically thereafter. ( 2.2 ) • Limit the dosage of saxagliptin tablets to 2.5 mg daily for patients also taking strong cytochrome P450 3A4/5 (CYP3A4/5) inhibitors (e.g., ketoconazole). ( 2.3 ) 2.1 Recommended Dosage The recommended dosage of saxagliptin tablets is 2.5 mg or 5 mg orally once daily taken regardless of meals. Do not cut, crush, or chew saxagliptin tablets. If a dose is missed, advise patients not to take an extra dose. Resume treatment with the next dose. 2.2 Dosage in Patients with Renal Impairment Assess renal function prior to initiation of saxagliptin tablets and then as clinically indicated [ see Use in Specific Populations (8.6) ]. The recommended dosage of saxagliptin tablets in patients with an eGFR greater than or equal to 45 mL/minute/1.73 m 2 is the same as the recommended dosage in patients with normal renal function [ see Dosage and Administration (2.1) ]. The dosage of saxagliptin tablets is 2.5 mg orally once daily for patients with eGFR < 45 mL/min/1.73 m 2 [which includes a subset of moderate or severe renal impairment, or with end-stage renal disease (ESRD) requiring hemodialysis] [ see Clinical Pharmacology (12.3) and Clinical Studies (14.2) ].

Warnings & precautions

Sourced from openFDA

• Pancreatitis: There have been postmarketing reports of acute pancreatitis. If pancreatitis is suspected, promptly discontinue saxagliptin tablets. ( 5.1 ) • Heart Failure: Consider the risks and benefits of saxagliptin tablets in patients who have known risk factors for heart failure. Monitor patients for signs and symptoms. ( 5.2 ) • Hypoglycemia with Concomitant Use of Insulin or Insulin Secretagogues: Consider a lower dosage of insulin or insulin secretagogue when used in combination with saxagliptin tablets. ( 5.3 ) • Hypersensitivity-Related Events: There have been postmarketing reports of serious hypersensitivity reactions such as anaphylaxis, angioedema, and exfoliative skin conditions. If hypersensitivity reactions occur, discontinue saxagliptin tablets, treat promptly, and monitor until signs and symptoms resolve. ( 5.4 ) • Arthralgia : Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors. Consider as a possible cause for severe joint pain and discontinue drug if appropriate. ( 5.5 ) • Bullous Pemphigoid: There have been postmarketing reports of bullous pemphigoid requiring hospitalization in patients taking DPP-4 inhibitors. Tell patients to report development of blisters or erosions. If bullous pemphigoid is suspected, discontinue saxagliptin tablets. ( 5.6 ) 5.1 Pancreatitis There have been postmarketing reports of acute pancreatitis in patients taking saxagliptin tablets.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described below or elsewhere in the prescribing information: • Pancreatitis [ see Warnings and Precautions (5.1) ] • Heart Failure [ see Warnings and Precautions (5.2) ] • Hypoglycemia with Concomitant Use of Insulin or Insulin Secretagogues [ see Warnings and Precautions (5.3) ] • Hypersensitivity Reactions [ see Warnings and Precautions (5.4) ] • Severe and disabling arthralgia [ see Warnings and Precautions (5.5) ] • Bullous pemphigoid [ see Warnings and Precautions (5.6) ] • Most common adverse reactions (incidence ≥ 5% and more often than placebo) are upper respiratory tract infection, urinary tract infection, and headache. ( 6.1 ) • Peripheral edema was reported more commonly in patients treated with the combination of saxagliptin tablets and a thiazolidinedione (TZD) than in patients treated with the combination of placebo and TZD. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Mylan at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse Reactions in Placebo-Controlled Trials in Adults with Type 2 Diabetes Mellitus The data in Table 1 are derived from a pool of 5 placebo-controlled clinical trials [ see Clinical Studies (14) ].

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary Limited data with saxagliptin tablets in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriages. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [ see Clinical Considerations ]. No adverse developmental effects independent of maternal toxicity were observed when saxagliptin was administered to pregnant rats and rabbits during the period of organogenesis and in pregnant and lactating rats during the pre- and postnatal period [ see Data ]. The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with an HbA1c greater than 7 and has been reported to be as high as 20 to 25% in women with an HbA1c greater than 10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, still birth and delivery complications.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of saxagliptin and its active metabolite, 5-hydroxy saxagliptin were similar in healthy subjects and in patients with type 2 diabetes mellitus. The C max and AUC values of saxagliptin and its active metabolite increased proportionally in the 2.5 to 400 mg dose range.

Overdosage

Sourced from openFDA

In a controlled clinical trial, once-daily, orally-administered saxagliptin tablets in healthy patients at doses up to 400 mg daily for 2 weeks (80-times the MRHD) had no dose-related clinical adverse reactions and no clinically meaningful effect on QTc interval or heart rate. In the event of an overdose, initiate appropriate supportive treatment as dictated by the patient’s clinical status. Saxagliptin and its active metabolite are removed by hemodialysis (23% of dose over 4 hours). Contact the Poison Help Line, (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.

Approval history

Sourced from openFDA
  • Jul 31, 2023ANDAANDA205972Aurobindo Pharma
  • Jul 31, 2023ANDAANDA205980Mylan
  • Jul 31, 2023ANDAANDA205981Mylan
  • Jul 31, 2023ANDAANDA205994Glenmark Pharms Ltd
  • Aug 9, 2023ANDAANDA207678Dr Reddys Labs Sa
  • Apr 6, 2026ANDAANDA211533Msn

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
1,440 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Acute Kidney Injury745.1%
  2. 2Nausea714.9%
  3. 3Hypoglycaemia654.5%
  4. 4Vomiting654.5%
  5. 5Diarrhoea644.4%
  6. 6Renal Failure Acute533.7%
  7. 7Dehydration483.3%
  8. 8Abdominal Pain473.3%
  9. 9Diabetes Mellitus473.3%
  10. 10Hypertension463.2%
  11. 11Dyspnoea443.1%
  12. 12Dizziness433.0%
  13. 13Asthenia422.9%
  14. 14Fatigue402.8%
  15. 15Hypotension402.8%

Clinical trials

View JSON

The 10 most recently updated of 157 ClinicalTrials.gov registrations naming Saxagliptin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Saxagliptin work?
Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the DPP-4 enzyme within minutes.
What is Saxagliptin used for?
According to FDA labeling, Saxagliptin carries indications including: Saxagliptin tablets are a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ( 1.1 ) Limitations of use: • Not recommended for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Saxagliptin?
Saxagliptin is classified as Dipeptidyl peptidase 4 (DPP-4) inhibitors, Dipeptidyl Peptidase 4 Inhibitors, Decreased Glucagon Secretion, Increased Insulin Secretion.
What are the brand names for Saxagliptin?
Saxagliptin is marketed under brand names including Kombiglyze, Onglyza, Qtern.
What are the contraindications for Saxagliptin?
Saxagliptin labeling lists contraindications including: Saxagliptin tablets are contraindicated in patients with a history of a serious hypersensitivity reaction to saxagliptin or any of the ingredients in saxagliptin tablets. Reactions such as anaphylaxis, angioedema, or exfoliative skin conditions have been reported with saxagliptin tablets [ see Warnings and Precautions (5.4) and Adverse Reactions (6.2) ].. Always consult the full prescribing information and a clinician.
Note. Data for saxagliptin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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