Sitagliptin
JANUVIA
What it isDPP-4 inhibitor that raises endogenous incretin signaling; type 2 diabetes.
Why this oneIt has the longest clinical track record in its class and broad renal use with dose adjustment.
What limits itGlucose lowering is modest with no cardiovascular benefit; pancreatitis, severe arthralgia, and bullous pemphigoid are rare.
FDA-approved for
- type 2 diabetes (2006)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Type 2 diabetes mellitus | Adults | 100 mg QD | 100 mg QD | 100 mg QD |
Renal eGFR 30–<45: 50 mg QD; eGFR <30 or ESRD on dialysis: 25 mg QD
Hepatic Undefined
Instructions
- Take with or without food
- Assess renal function before initiation and periodically
Cautions
- Pancreatitis (incl. hemorrhagic/necrotizing)
- Heart failure
- Acute renal failure
- Hypoglycemia with concomitant insulin or insulin secretagogues
- Hypersensitivity reactions (anaphylaxis, angioedema, Stevens-Johnson syndrome)
- Severe and disabling arthralgia
- Bullous pemphigoid
Adverse reactions
- Upper respiratory tract infection
- Nasopharyngitis
- Headache
- Hypoglycemia (with sulfonylurea or insulin)
Pregnancy Limited human data insufficient to determine drug-associated risk
Lactation No human data; present in rat milk
NO BOXED WARNINGS
Principal riskLittle; rare pancreatitis and arthralgia
Cost, est. cash$300–$1,000/month
Generic entry2026
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityAgent-specific hypoglycemia, ketoacidosis, volume, renal or gastrointestinal toxicity.
Mechanism of action: Sitagliptin ballicule
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