Alogliptin API Manufacturers & Suppliers

Alogliptin (CAS 850649-61-5) is an orally active, selective inhibitor of the dipeptidyl peptidase‑4 enzyme used to improve glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise. It is marketed in several regions as alogliptin benzoate and exists predominantly as the R‑enantiomer with minimal in vivo chiral conversion.

The compound enhances endogenous incretin activity by preventing the degradation of GLP‑1 and GIP. This increases glucose‑dependent insulin secretion from pancreatic beta cells and suppresses glucose‑dependent glucagon release. In controlled studies, peak DPP‑4 inhibition occurs within 2 to 3 hours, exceeding 93 percent across a wide dose range. Inhibition remains above 80 percent for at least 24 hours at doses of 25 mg or higher, supporting once‑daily administration. Alogliptin also increases postprandial active GLP‑1 levels and reduces postprandial glucagon without producing QTc prolongation.

Alogliptin shows high oral bioavailability and moderate distribution, with plasma protein binding of approximately 20 to 30 percent. It undergoes minimal hepatic metabolism and is excreted primarily unchanged in the urine. The terminal elimination half‑life is about 21 hours. Renal clearance is the dominant elimination route, and dose adjustment is required in patients with reduced kidney function.

Safety considerations include the potential for hypersensitivity reactions such as angioedema and rare cases of pancreatitis. Clinicians also monitor for hypoglycemia when alogliptin is used with agents that independently increase insulin levels. As a DPP‑4 inhibitor with limited CYP involvement, the risk of drug interactions is comparatively low, though caution is advised in polypharmacy settings.

Alogliptin is available globally as single‑agent products such as Nesina and in fixed‑dose combinations with metformin or pioglitazone.

For API procurement, sourcing should prioritize confirmation of enantiomeric purity, control of benzoate salt form, and verification of impurities aligned with ICH guidelines, given the low therapeutic dose and prolonged systemic exposure.