Review of sitagliptin phosphate: a novel treatment for type 2 diabetes.
Sitagliptin (Januvia, Merck Pharmaceuticals) is a dipeptidyl-peptidase inhibitor (DPP-4 inhibitor) that has recently been approved for the therapy of type 2 diabetes. Like other DPP-4 inhibitors its action is mediated by increasing levels of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). Sitagliptin is effective in lowering HbA1c, and fasting as well as postprandial glucose in monotherapy and in combination with other oral antidiabetic agents. It stimulates insulin secretion when hyperglycemia is present and inhibits glucagon secretion. In clinical studies it is weight neutral. This article gives an overview of the mechanism of action, the pharmacology, and the clinical efficacy and safety of sitagliptin in type 2 diabetes therapy.
Gallwitz
Baptist
B
Dept. Medicine IV, Eberhard Karls University, Tuebingen, Germany. baptist.gallwitz@med.uni-tuebingen.de
D000243:Adenosine Deaminase / Q000097:blood; D058892:Adenosine Deaminase Inhibitors; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects / Q000378:metabolism; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy*; D018819:Dipeptidyl Peptidase 4 / Q000097:blood; D054873:Dipeptidyl-Peptidase IV Inhibitors; D052216:Glucagon-Like Peptide 1 / Q000819:agonists* / Q000097:blood; D006023:Glycoproteins / Q000037:antagonists & inhibitors / Q000097:blood; D006801:Humans; D007527:Isoenzymes; D011719:Pyrazines / Q000627:therapeutic use*; D000068900:Sitagliptin Phosphate; D016896:Treatment Outcome; D014230:Triazoles / Q000627:therapeutic use*
D058892:Adenosine Deaminase Inhibitors; D001786:Blood Glucose; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006023:Glycoproteins; D007527:Isoenzymes; D011719:Pyrazines; D014230:Triazoles; D052216:Glucagon-Like Peptide 1; C042807:DPP4 protein, human; D018819:Dipeptidyl Peptidase 4; D000243:Adenosine Deaminase; D000068900:Sitagliptin Phosphate