New Therapy UpdateLinagliptin: The Newest Dipeptidyl Peptidase-4 Inhibitor for Type 2 Diabetes MellitusAletti, Rachael BS, PharmD; Cheng-Lai, Angela PharmDAuthor Information Department of Pharmacy, Montefiore Medical Center/Jack D. Weiler Hospital of the Albert Einstein College of Medicine, Bronx, NY Disclosure: The authors declare no conflict of interest. Correspondence: Angela Cheng-Lai, PharmD, Department of Pharmacy, Montefiore Medical Center, 1825 Eastchester Road, Bronx, NY 10461. E-mail: Acheng@montefiore.org. Cardiology in Review: January/February 2012 - Volume 20 - Issue 1 - p 045-051 doi: 10.1097/CRD.0b013e31823a3afc Buy Metrics Abstract Dipeptidyl peptidase-4 (DPP-4) inhibitors are some of the newest medications in our armamentarium for the management of type 2 diabetes mellitus. Through inhibition of the DPP-4 enzyme, these agents increase the amount of circulating incretin hormones, leading to an increase in insulin release and a suppression of glucagon secretion. Linagliptin is the third DPP-4 inhibitor approved by the Food and Drug Administration in the United States. It has been studied as monotherapy and as an adjunctive therapy to other oral agents in a dual or triple combination regimen. Linagliptin lowers glycosylated hemoglobin by about 0.4% when used as monotherapy and by about 0.5% to 1.1% when used in combination with other oral antihyperglycemic agents. Since linagliptin is mostly eliminated via the enterohepatic system (80%) and not to a significant extent through renal excretion, dosage adjustment is not necessary in patients with renal impairment. Linagliptin also has a favorable safety profile; nasopharyngitis is one of the more common observed side effects. Given its encouraging safety and efficacy profile, linagliptin is a good alternative to the other 2 agents in this class, especially for patients with renal impairment. This article provides a review of the pharmacologic and pharmacokinetic properties of linagliptin. The differences among the 3 available DPP-4 inhibitors will also be examined. © 2012 Lippincott Williams & Wilkins, Inc.