pharmacopeia
GET
/api/v1/drug/sitagliptin
2D structure
(3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
SMILES C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N
InChIKey MFFMDFFZMYYVKS-SECBINFHSA-N

Mechanism of action

Sourced from openFDA

Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones.

Dipeptidyl Peptidase 4

Indications

Sourced from openFDA
  • JANUVIA ® is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. JANUVIA is 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.ICD-10: E11.9

Contraindications

Sourced from openFDA
  • History of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema.contraindicated

Dosage & administration

Sourced from openFDA

The recommended dose of JANUVIA is 100 mg once daily. JANUVIA can be taken with or without food. ( 2.1 ) Dosage adjustment is recommended for patients with eGFR less than 45 mL/min/1.73 m 2 . ( 2.2 ) Dosage Adjustment in Patients with Renal Impairment ( 2.2 ) eGFR greater than or equal to 30 mL/min/1.73 m 2 to less than 45 mL/min/1.73 m 2 eGFR less than 30 mL/min/1.73 m 2 (including patients with end stage renal disease [ESRD] on dialysis) 50 mg once daily 25 mg once daily 2.1 Recommended Dosing The recommended dose of JANUVIA is 100 mg once daily. JANUVIA can be taken with or without food. 2.2 Recommendations for Use in Renal Impairment Assess renal function prior to initiation of JANUVIA and periodically thereafter. For patients with an estimated glomerular filtration rate [eGFR] greater than or equal to 45 mL/min/1.73 m 2 to less than 90 mL/min/1.73 m 2 , no dosage adjustment for JANUVIA is required. For patients with moderate renal impairment (eGFR greater than or equal to 30 mL/min/1.73 m 2 to less than 45 mL/min/1.73 m 2 ), the dose of JANUVIA is 50 mg once daily. For patients with severe renal impairment (eGFR less than 30 mL/min/1.73 m 2 ) or with end-stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of JANUVIA is 25 mg once daily. JANUVIA may be administered without regard to the timing of dialysis.

Warnings & precautions

Sourced from openFDA

Pancreatitis: There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue JANUVIA. ( 5.1 ) Heart failure : Heart failure has been observed with two other members of the DPP-4 inhibitor class. Consider risks and benefits of JANUVIA in patients who have known risk factors for heart failure. Monitor patients for signs and symptoms. ( 5.2 ) Acute Renal Failure: Has been reported postmarketing, sometimes requiring dialysis. Assessment of renal function is recommended prior to initiating JANUVIA and periodically thereafter. ( 5.3 ) Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues: Increased risk of hypoglycemia when used in combination with insulin and/or an insulin secretagogue. Lower dose of insulin or insulin secretagogue may be required. ( 5.4 , 7.1 ) Hypersensitivity Reactions: There have been postmarketing reports of serious allergic and hypersensitivity reactions in patients treated with JANUVIA such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. Promptly stop JANUVIA, assess for other potential causes, institute appropriate monitoring and treatment. ( 5.5 , 6.2 ) 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. ( 5.6 ) Bullous Pemphigoid: There have been postmarketing reports requiring hospitalization in patients taking DPP-4 inhibitors.

Adverse reactions

Sourced from openFDA

The following adverse reactions are also discussed elsewhere in the labeling: Pancreatitis [see Warnings and Precautions (5.1) ] Heart Failure [see Warnings and Precautions (5.2) ] Acute Renal Failure [see Warnings and Precautions (5.3) ] Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues [see Warnings and Precautions (5.4) ] Hypersensitivity Reactions [see Warnings and Precautions (5.5) ] Severe and Disabling Arthralgia [see Warnings and Precautions (5.6) ] Bullous Pemphigoid [see Warnings and Precautions (5.7) ] Adverse reactions reported in ≥5% of patients treated with JANUVIA and more commonly than in patients treated with placebo are: upper respiratory tract infection, nasopharyngitis and headache. In the add-on to sulfonylurea and add-on to insulin studies, hypoglycemia was also more commonly reported in patients treated with JANUVIA compared to placebo. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme LLC at 1-877-888-4231 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.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary The limited available data with JANUVIA in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations ]. No adverse developmental effects were observed when sitagliptin was administered to pregnant rats and rabbits during organogenesis at oral doses up to 30-times and 20-times, respectively, the 100 mg clinical dose, based on AUC [see Data ] . The estimated background risk of major birth defects is 6-10% in women with pre-gestational diabetes with a Hemoglobin A1c >7% and has been reported to be as high as 20-25% in women with a Hemoglobin A1c >10%. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, still birth, and macrosomia related morbidity.

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetics of sitagliptin have been extensively characterized in healthy subjects and patients with type 2 diabetes mellitus. Following a single oral 100-mg dose to healthy volunteers, mean plasma AUC of sitagliptin was 8.52 μM•hr, C max was 950 nM, and apparent terminal half-life (t 1/2 ) was 12.4 hours.

Overdosage

Sourced from openFDA

In the event of an overdose with JANUVIA, contact the Poison Control Center. In the event of an overdose, it is reasonable to employ supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy as dictated by the patient's clinical status. Sitagliptin is modestly dialyzable. In clinical studies, approximately 13.5% of the dose was removed over a 3- to 4-hour hemodialysis session. Prolonged hemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialyzable by peritoneal dialysis.

Approval history

Sourced from openFDA
  • Oct 16, 2006NDANDA021995Msd
  • Mar 30, 2007NDANDA022044Msd Sub Merck
  • Feb 2, 2012NDANDA202270Msd Sub Merck
  • Dec 19, 2017NDANDA209805Msd Sub Merck
  • Oct 18, 2023NDANDA211566Zydus Lifesciences
  • Nov 3, 2023NDANDA216743Zydus Lifesciences
  • Jul 18, 2024NDANDA216778Zydus Lifesciences
  • Jan 16, 2025NDANDA219122Azurity

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.
91,110 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. 1Blood Glucose Increased5,8786.5%
  2. 2Nausea4,8495.3%
  3. 3Diarrhoea4,7815.2%
  4. 4Drug Ineffective4,3924.8%
  5. 5Fatigue3,7554.1%
  6. 6Vomiting3,1013.4%
  7. 7Headache3,0783.4%
  8. 8Dizziness3,0423.3%
  9. 9Acute Kidney Injury2,9673.3%
  10. 10Dyspnoea2,9373.2%
  11. 11Pancreatitis2,7413.0%
  12. 12Death2,6832.9%
  13. 13Asthenia2,6242.9%
  14. 14Weight Decreased2,5942.8%
  15. 15Malaise2,3972.6%

Literature

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Recent PubMed references pinned to Sitagliptin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 564 ClinicalTrials.gov registrations naming Sitagliptin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Sitagliptin work?
Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones.
What is Sitagliptin used for?
According to FDA labeling, Sitagliptin carries indications including: JANUVIA ® is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. JANUVIA is 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Sitagliptin?
Sitagliptin is classified as Dipeptidyl peptidase 4 (DPP-4) inhibitors, Dipeptidyl Peptidase 4 Inhibitor, Dipeptidyl Peptidase 4 Inhibitors, Decreased Glucagon Secretion, Increased Insulin Secretion.
What are the brand names for Sitagliptin?
Sitagliptin is marketed under brand names including Brynovin, Janumet, Januvia, Steglujan, Zituvimet, Zituvio.
What are the contraindications for Sitagliptin?
Sitagliptin labeling lists contraindications including: History of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema.. Always consult the full prescribing information and a clinician.
Note. Data for sitagliptin 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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