Review of sitagliptin phosphate: a novel treatment for type 2 diabetes

被引：57

作者：

Gallwitz, Baptist ^{[1
]}

机构：

[1] Eberhard Karls Univ Tubingen, Dept Med 4, Otfried Mueller Str 10, D-72076 Tubingen, Germany

来源：

VASCULAR HEALTH AND RISK MANAGEMENT | 2007年 / 3卷 / 02期

关键词：

incretins; type; 2; diabetes; diabetes therapy; DPP-4; inhibitors; sitagliptin;

D O I：

10.2147/vhrm.2007.3.2.203

中图分类号：

R6 [外科学];

学科分类号：

1002 ; 100210 ;

摘要：

Sitagliptin (Januvia (R), 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 IIA1c, 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.

引用

页码：203 / 210

页数：8

共 33 条

[1] Beta-cell expression of a dominant-negative HNF-1α compromises the ability of inhibition of dipeptidyl peptidase-4 to elicit a long-term augmentation of insulin secretion in mice [J].

Ahrén, B ;

Winzell, MS ;

Burkey, B ;

Hughes, TE .

EUROPEAN JOURNAL OF PHARMACOLOGY, 2005, 521 (1-3) :164-168

[2] What mediates the benefits associated with dipeptidyl peptidase-IV inhibition? [J].

Ahrén, B .

DIABETOLOGIA, 2005, 48 (04) :605-607

[3]

Aschner P, 2006, DIABETOLOGIA, V49, P5

[4] Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes [J].

Aschner, Pablo ;

Kipnes, Mark S. ;

Lunceford, Jared K. ;

Sanchez, Matilde ;

Mickel, Carolyn ;

Williams-Herman, Debora E. .

DIABETES CARE, 2006, 29 (12) :2632-2637

[5]

Aschner P, 2006, DIABETES, V55, pA462

[6] Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: A double-blind, randomized, placebo-controlled study in healthy male volunteers [J].

Bergman, AJ ;

Stevens, C ;

Zhou, YY ;

Yi, BM ;

Laethem, M ;

De Smet, M ;

Snyder, K ;

Hilliard, D ;

Tanaka, W ;

Zeng, W ;

Tanen, M ;

Wang, AQ ;

Chen, L ;

Winchell, G ;

Davies, MJ ;

Ramael, S ;

Wagner, JA ;

Herman, GA .

CLINICAL THERAPEUTICS, 2006, 28 (01) :55-72

[7] Exenatide [J].

Bray, GM .

AMERICAN JOURNAL OF HEALTH-SYSTEM PHARMACY, 2006, 63 (05) :411-418

[8] Dipeptidyl peptidase IV inhibition as an approach to the treatment and prevention of type 2 diabetes: a historical perspective [J].

Deacon, CF ;

Holst, JJ .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2002, 294 (01) :1-4

[9] Type 2 diabetes - Therapy with dipeptidyl peptidase IV inhibitors [J].

Demuth, HU ;

McIntosh, CHS ;

Pederson, RA .

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS, 2005, 1751 (01) :33-44

[10] The biology of incretin hormones [J].

Drucker, DJ .

CELL METABOLISM, 2006, 3 (03) :153-165

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