Last reviewed 2026-04-20 · How we verify

sitagliptin and metformin

Sitagliptin and metformin, marketed by the University Medical Centre Ljubljana, is a combination therapy for Type 2 Diabetes Mellitus. The key composition patent expires in 2028, providing a strong barrier to generic competition until then. The primary risk is the lack of revenue data, which makes it difficult to assess the drug's market performance and financial impact.

At a glance

Approved indications

• Type 2 Diabetes Mellitus

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

• Upper respiratory tract infection
• Nasopharyngitis
• Peripheral edema
• Headache
• Hypoglycemia

Drug interactions

• Carbonic Anhydrase Inhibitors (Topiramate, zonisamide, acetazolamide, dichlorphenamide)
• Drugs that Reduce Metformin Clearance (Ranolazine, vandetanib, dolutegravir, cimetidine)
• Alcohol
• Insulin Secretagogues or Insulin
• Drugs Affecting Glycemic Control (Thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers, isoniazid)

Key clinical trials

• 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)
• Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes. (PHASE4)
• Triple Hypoglycemic Regimens In Patients With Newly Diagnosed Type 2 Diabetes Mellitus (PHASE1, PHASE2)
• Evaluate the Efficacy and Safety of Empagliflozin or Glimepiride Combination Therapy in Type 2 Diabetes Mellitus Patients (PHASE4)
• iSGLT2 Inhibitor and a iDPP -4 Inhibitor in Treatment of Type 2 Diabetes Mellitus in Patients Treated With Metformin (TRIAD) (PHASE3)
• Canagliflozin and Myocardial Fibrosis (PHASE4)

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:

• sitagliptin and metformin CI brief — competitive landscape report
• sitagliptin and metformin updates RSS · CI watch RSS
• University Medical Centre Ljubljana portfolio CI