Sitagliptin phosphate: a DPP-4 inhibitor for the treatment of type 2 diabetes mellitus

Clinical Therapeutics
Tina Zerilli, Eunice Y Pyon

Abstract

Sitagliptin phosphate, the first dipeptidyl peptidase 4 (DPP-4) inhibitor, provides a new treatment option for patients with type 2 diabetes. The purpose of this article is to review the pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, adverse effects, and cost of sitagliptin in adults with type 2 diabetes. A literature search of MEDLINE (1966-May 10, 2007), Iowa Drug Information Service (1966-May 10, 2007), and International Pharmaceutical Abstracts (1970-May 10, 2007) was performed using the terms sitagliptin and MK-0431. English-language, original research and review articles were reviewed, as were citations from these articles. The 2005 and 2006 American Diabetes Association Scientific Abstracts were searched, and the US Food and Drug Administration review of the new drug application for sitagliptin and select information from the manufacturer were consulted. By inhibiting DPP-4, sitagliptin enhances postprandial levels of active glucagon-like peptide-1 (GLP-1), leading to a rise in insulin release and decrease in glucagon secretion from pancreatic alpha-cells. Sitagliptin is 87% orally bioavailable, undergoes minimal hepatic metabolism, and is primarily excreted unchanged (approximately 79%) in the urin...Continue Reading

Citations

Dec 17, 2011·European Journal of Clinical Pharmacology·Arun K PSuresh B
Feb 26, 2013·European Journal of Drug Metabolism and Pharmacokinetics·Shinji FurutaYoshiyuki Furuta
Jul 2, 2010·Diabetes, Obesity & Metabolism·A J Scheen
Sep 17, 2013·Drug Design, Development and Therapy·Vinay S Eligar, Stephen C Bain
Jan 1, 2009·Diabetes, Metabolic Syndrome and Obesity : Targets and Therapy·Radha AndukuriMarc Rendell
Aug 10, 2010·Clinical Pharmacokinetics·André J Scheen
May 15, 2013·Journal of Neurogastroenterology and Motility·Takashi NonakaMasahiko Inamori
Mar 1, 2010·Expert Review of Clinical Pharmacology·Thomas D AicherAnthony Celeste
May 23, 2015·Expert Review of Cardiovascular Therapy·Maria Lee, Mary K Rhee
May 20, 2008·Expert Opinion on Drug Metabolism & Toxicology·Michael A PacanowskiChristina L Aquilante
Mar 27, 2009·The American Journal of the Medical Sciences·Daniel M RicheKrista D Riche
Nov 20, 2012·Luminescence : the Journal of Biological and Chemical Luminescence·Taiza de Paula e MancilhaWagner F Pacheco
Apr 24, 2010·Pharmacotherapy·Joshua J NeumillerR Keith Campbell
Oct 19, 2012·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Shinji FurutaSteve Warrington
Oct 16, 2012·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Sudhanshu Kumar BhartiAshok Kumar Gupta
Nov 20, 2015·Biopolymers·Yoshio Hamada, Yoshiaki Kiso
Oct 6, 2018·Endocrine Practice : Official Journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists·Eiji KutohJyunka Hayashi
Feb 20, 2015·Metabolic Brain Disease·Tomás P BachorAngela M Suburo
Aug 18, 2012·Food & Function·Hsiu-Ju Wang, Been-Huang Chiang
Dec 29, 2010·Journal of Medicinal Chemistry·Zhiyuan ZhangStephen L Gwaltney
Oct 6, 2009·Journal of the American Pharmacists Association : JAPhA·Joshua J Neumiller

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cardiovascular Biology of GLP-1

Glucagon-like peptide 1 (GLP-1) plays a role in glucose metabolism, energy homeostasis, and inflammation suppression. GLP-1 receptor signaling has been shown to impact cardiovascular function. This feed focuses on the role of GLP-1 and GLP-1 receptor agonists on cardiovascular biology.

Biomarkers for Type 2 Diabetes

Biomarkers can help understand chronic diseases and assist in risk prediction for prevention and early detection of diseases. Here is the latest research on biomarkers in type 2 diabetes, a disease in which the body is unable to produce or properly use insulin.