General Information

Nesina (alogliptin) is a small-molecule, orally available dipeptidyl peptidase IV (DPP IV) inhibitor. DPP-4 inhibitors slow the inactivation of incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide), both of which play a role in regulating blood glucose levels.

Nesina is specifically indicated as an adjunct to diet and exercise to improve glycemic control in adults with type II diabetes mellitus.

Nesina is supplied as a tablet for oral administration. The recommended dose is 25 mg once daily, with or without food.

Clinical Results

FDA Approval
The FDA approval of Nesina was based on three double-blind studies to evaluate the efficacy and safety in 1,768 patients with inadequate glycemic control on diet and exercise. All three studies had a 4-week, single-blind, placebo run-in period followed by a 26-week randomized treatment period.
In a 26-week, double-blind, placebo-controlled study, a total of 329 patients (mean baseline A1C = 8%) were randomized to receive Nesina 12.5 mg, 25 mg, or placebo once daily. Treatment with Nesina 25 mg resulted in statistically significant improvements from baseline in A1C and fasting plasma glucose (FPG) compared to placebo at Week 26: 44% in the Nesina arm achieved A1C <7% versus 23% in the placebo arm and in the Nesina arm there was a -16 change in FPG from baseline versus a 11 increase in the placebo arm. . A total of 8% of patients receiving Nesina 25 mg and 30% of those receiving placebo required glycemic rescue therapy.
In a 26-week, double-blind, active-controlled study, a total of 655 patients (mean baseline A1C = 8.8%) were randomized to receive Nesina 25 mg alone, pioglitazone 30 mg alone, Nesina 12.5 mg with pioglitazone 30 mg, or Nesina 25 mg with pioglitazone 30 mg once daily. Coadministration of Nesina 25 mg with pioglitazone 30 mg resulted in statistically significant improvements from baseline in A1C and FPG compared to Nesina 25 mg alone and to pioglitazone 30 mg alone.
In a 26-week, double-blind, placebo-controlled study, a total of 784 patients inadequately controlled on diet and exercise alone (mean baseline A1C = 8.4%) were randomized to 1 of 7 treatment groups: placebo; metformin HCl 500 mg or metformin HCl 1000 mg twice daily, Nesina 12.5 mg twice daily, or Nesina 25 mg daily;Nesina 12.5 mg in combination with metformin HCl 500 mg or metformin HCl 1000 mg twice daily. Both coadministration treatment arms (Nesina 12.5 mg + metformin HCl 500 mg and Nesina 12.5 mg + metformin HCl 1000 mg) resulted in statistically significant improvements in A1C and FPG when compared with their respective individual alogliptin and metformin component regimens. Coadministration treatment arms demonstrated improvements in 2-hour postprandial glucose (PPG) compared to Nesina alone or metformin alone.

Side Effects

Adverse events associated with the use of Nesina may include, but are not limited to, the following:

• nasopharyngitis
• headache
• upper respiratory tract infection

Mechanism of Action

Nesina (alogliptin) is a small-molecule, orally available dipeptidyl peptidase IV (DPP IV) inhibitor. DPP-4 inhibitors slow the inactivation of incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide), both of which play a role in regulating blood glucose levels.

Literature References

DeFronzo RA, Fleck PR, Wilson CA, Mekki Q; Alogliptin Study 010 Group Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes and inadequate glycemic control: a randomized, double-blind, placebo-controlled study. Diabetes Care 2008 Dec;31(12):2315-7

Additional Information

For additional information regarding Nesina or type II diabetes, please visit the Takeda Products web page.