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Januvia (SITAGLIPTIN)

Januvia works by blocking an enzyme that breaks down hormones that help the body release insulin.

Januvia (sitagliptin) is a small molecule dipeptidyl peptidase 4 inhibitor originally developed by Merck Sharp Dohme and currently owned by Zydus Lifesciences. It was FDA approved in 2006 for the treatment of diabetes mellitus type 2. Januvia works by inhibiting the enzyme dipeptidyl peptidase 4, which breaks down incretin hormones that stimulate insulin release. As a result, Januvia increases insulin secretion and decreases glucagon levels, leading to improved glycemic control. Januvia has a half-life of 12 hours and 87% bioavailability.

At a glance

Mechanism of action

Sitagliptin is DPP-4 inhibitor, which is believed to exert its actions in patients with type 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. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic g

Approved indications

• Diabetes mellitus type 2

Boxed warnings

• WARNING: LACTIC ACIDOSIS WARNING: LACTIC ACIDOSIS See full prescribing information for complete boxed warning . Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. Symptoms included malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Laboratory abnormalities included elevated blood lactate levels, anion gap acidosis, increased lactate/pyruvate ratio, and metformin plasma levels generally >5 mcg/mL. ( 5.1 ) Risk factors include renal impairment, concomitant use of certain drugs, age ≥65 years old, radiological studies with contrast, surgery and other procedures, hypoxic states, excessive alcohol intake, and hepatic impairment. Steps to reduce the risk of and manage metformin-associated lactic acidosis in these high-risk groups are provided in the Full Prescribing Information. ( 5.1 ) If lactic acidosis is suspected, discontinue ZITUVIMET and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended. ( 5.1 ) Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. The onset of metformin-associated lactic acidosis is often subtle, accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Metformin-associated lactic acidosis was characterized by elevated blood lactate levels (>5 mmol/Liter), anion gap acidosis (without evidence of ketonuria or ketonemia), an increased lactate/pyruvate ratio, and metformin plasma levels generally >5 mcg/mL [see Warnings and Precautions ( 5.1 )] . Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (e.g., carbonic anhydrase inhibitors such as topiramate), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (e.g., acute congestive heart failure), excessive alcohol intake, and hepatic impairment. Steps to reduce the risk of and manage metformin-associated lactic acidosis in these high risk groups are provided in the full prescribing information [see Dosage and Administration ( 2.2 )>, Contraindications ( 4 ), Warnings and Precautions ( 5.1 ), Drug Interactions ( 7 ), and Use in Specific Populations ( 8.6 , 8.7 )] . If metformin-associated lactic acidosis is suspected, immediately discontinue ZITUVIMET and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended [see Warnings and Precautions ( 5.1 )] .

Common side effects

• Female genital mycotic infections
• Urinary tract infections
• Headache
• Increased urination
• Vaginal pruritus
• Nasopharyngitis
• Back pain
• Weight decreased
• Thirst
• Ketoacidosis
• Volume Depletion

Drug interactions

• ciprofloxacin
• gatifloxacin
• levofloxacin
• norfloxacin
• ofloxacin

Key clinical trials

• The Role of Phosphodiesterase Inhibitors in Incretin Secretion (PHASE1)
• Comparative Effectiveness of Oral Semaglutide vs Sitagliptin Among Individuals With Heart Failure With Preserved Ejection Fraction (STEP-HFpEF DM ORAL)
• Comparative Effectiveness of Two Initial Combination Therapies in Patients With Recent Onset Diabetes (PHASE3)
• Metformin, Empagliflozin With Sitagliptin vs Linagliptin in Type 2 Diabetes (PHASE4)
• Effect of Dapagliflozin vs Sitagliptin on Liver Fat Accumulation and Body Composition in Patients With Diabetes Mellitus and Liver Transplantation (NA)
• Dose Optimization of Sitagliptin and Duloxetine in Diabetic Cirrhosis (PHASE4)
• Comparative Study Between (SGLT-2i) and (DPP-4i) in the Prevention of DIC (PHASE4)
• Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes. (PHASE4)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Januvia CI brief — competitive landscape report
• Januvia updates RSS · CI watch RSS
• Zydus Lifesciences portfolio CI