title: Linagliptin:  the newest dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus.
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.
authors.affiliation: Department of Pharmacy, Montefiore Medical Center/Jack D. Weiler Hospital of the Albert Einstein College of Medicine, Bronx, NY, USA.
authors.forename: Rachael
authors.initials: R
authors.lastname: Aletti
authors.forename: Angela
authors.initials: A
authors.lastname: Cheng-Lai
mesh_terms: D001786:Blood Glucose / Q000378:metabolism; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D016527:Drug Costs; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D006442:Glycated Hemoglobin / Q000378:metabolism; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D000069476:Linagliptin; D011687:Purines / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D011799:Quinazolines / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D013607:Tablets; D016896:Treatment Outcome
chemical_list: D001786:Blood Glucose; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006442:Glycated Hemoglobin; D007004:Hypoglycemic Agents; D000069476:Linagliptin; D011687:Purines; D011799:Quinazolines; D013607:Tablets