OBJECTIVE The pharmacology, pharmacodynamics, pharmacokinetics, safety, efficacy, and place in therapy of alogliptin and its combinations for managing type 2 diabetes mellitus are reviewed. CONCLUSIONS Alogliptin is a selective, orally bioavailable inhibitor of the enzymatic activity of dipeptidyl peptidase-4 (DPP-4). It works by slowing the inactivation of the incretin hormones, thereby increasing their concentrations in the bloodstream and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin has a moderate degree of absorption, estimated to exceed 75%, and its absorption is not affected by food. No drug interactions are known to be associated with alogliptin monotherapy. It is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. The clinical efficacy and safety of alogliptin have been demonstrated in several clinical trials, reducing patients' glycosylated hemoglobin level by 0.4-1.0% in 26 weeks. Alogliptin does not require any dosage adjustment when coadministered with ketoconazole, fluconazole, gemfibrozil, warfarin, metformin, glyburide, and pioglitazone. Alogliptin selectively binds to and inhibits DPP-4 in vitro at concentrations approximating therapeutic exposures. The most common adverse events associated with alogliptin are nasopharyngitis, headache, and upper respiratory tract infection. As with the other DPP-4 inhibitors, use of alogliptin may be associated with the development of pancreatitis during therapy. CONCLUSIONS Alogliptin, a selective DPP-4 inhibitor, does not differ greatly from the other DPP-4 inhibitors currently available. It can be used as monotherapy or in combination with metformin for the management of type 2 diabetes.