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Nesina (ALOGLIPTIN)

Nesina works by blocking an enzyme that breaks down incretin hormones, allowing more insulin to be released and less glucagon.

Nesina (alogliptin) is a small molecule dipeptidyl peptidase 4 (DPP-4) inhibitor developed by Takeda Pharms USA, targeting the DPP-4 enzyme to treat type 2 diabetes mellitus. It was FDA-approved in 2013 and remains a patented product with no generic manufacturers. Nesina works by inhibiting the DPP-4 enzyme, which breaks down incretin hormones, thereby increasing insulin release and decreasing glucagon levels. Key safety considerations include its potential to increase the risk of heart failure and pancreatitis. Commercially, Nesina is still under patent protection.

At a glance

Mechanism of action

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 glucose-dependent manner but are inactivated by the dipeptidyl peptidase-4 (DPP-4) enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, reducing hepatic glucose production. In patients with type diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Alogliptin is DPP-4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in glucose-dependent manner in patients with type diabetes mellitus. Alogliptin selectively binds to and inhibits DPP-4 but not DPP-8 or DPP-9 activity in v

Approved indications

• Diabetes mellitus type 2

Boxed warnings

• WARNING: LACTIC ACIDOSIS 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 (greater than 5 mmol/L), anion gap acidosis (without evidence of ketonuria or ketonemia), an increased lactate/pyruvate ratio; and metformin plasma levels generally greater than 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) , Use in Specific Populations (8.6 , 8.7) ] . If metformin-associated lactic acidosis is suspected, immediately discontinue alogliptin and metformin HCl tablets and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended [see Warnings and Precautions (5.1) ]. 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 greater than 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 alogliptin and metformin HCl tablets and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended. ( 5.1 )

Common side effects

• Renal impairment
• Decreased glomerular filtration rate
• Decreased renal clearance
• Hypoglycemia
• Decreased creatinine clearance
• Increased blood creatinine
• Nasopharyngitis
• Upper Respiratory Tract Infection
• Headache

Key clinical trials

• The Effect of Alogliptin Combined With Actoplus Met on Glucose and Lipid Metabolism and Pancreatic Function in Patients With T2DM Complicated With MAFLD (PHASE4)
• A Study to Evaluate the Effect of add-on Pioglitazone or Dapagliflozin in Participants With Type 2 Diabetes Mellitus Inadequately Controlled by DPP-4 Inhibitor and Metformin Therapy (PHASE4)
• Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study
• Comparison of Type 2 Diabetes Pharmacotherapy Regimens
• A Bioequivalence Study of CT-L02 Compared to Co-administration (CTL0201 and CTL0202) in Healthy Volunteers (PHASE1)
• Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM)- Semaglutide v DPP4 Inhibitors
• Using Secondary Data to Evaluate Sex-based Heterogeneity of GLP-1 Agonists and SGLT2 Inhibitors on Cardiovascular-Kidney-Metabolic Health (CKMH) Outcomes in Real-world Settings (DASH-CKMH)
• Efficacy and Safety of Add-On Therapy With Empagliflozin in Patients With Type 2 Diabetes on a Background of Alogliptin and Metformin (PHASE3)

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:

• Nesina CI brief — competitive landscape report
• Nesina updates RSS · CI watch RSS
• Takeda portfolio CI