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正在研究用于治疗糖尿病的小分子二肽基肽酶 IV 抑制剂。

Small molecule dipeptidylpeptidase IV inhibitors under investigation for diabetes mellitus therapy.

机构信息

Eberhard-Karls-University, Dept Medicine IV, Otfried-Müller-Str. 10, 72076 Tübingen, Germany.

出版信息

Expert Opin Investig Drugs. 2011 Jun;20(6):723-32. doi: 10.1517/13543784.2011.576667. Epub 2011 Apr 18.

DOI:10.1517/13543784.2011.576667
PMID:21500969
Abstract

INTRODUCTION

A recent treatment advance for type 2 diabetes is the oral therapy with DPP IV inhibitors. New substances of this class are in development in order to increase alternatives for treating this important metabolic disease. The reader will gain detailed pharmacological and clinical information on alogliptin, dutogliptin and linagliptin and will learn how these DPP IV inhibitors may widen the whole drug class. Possible special indications for the various DPP IV inhibitors are discussed.

AREAS COVERED

The DPP IV inhibitors and their current role in type 2 diabetes are highlighted. Preclinical and clinical studies of the novel DPP IV inhibitors alogliptin, dutogliptin and linagliptin, including published data since 2007, are presented and a comparison of these compounds is made.

EXPERT OPINION

The efficacy and safety profile of DPP IV inhibitors are promising and advantageous so far. In contrast to sulfonylureas, DPP IV inhibitors do not have an intrinsic risk for causing hypoglycemia and they are body weight neutral. Their tolerability profile is good and no specific adverse reactions have been reported. Experience so far suggests that there are no safety issues associated with inhibition of DPP IV activity by itself. Novel DPP IV inhibitors with distinct properties may offer alternative choices within this drug class.

摘要

简介

2 型糖尿病的一种新的治疗进展是使用 DPP-IV 抑制剂进行口服治疗。为了增加治疗这种重要代谢疾病的选择,该类别的新药正在开发中。读者将获得关于阿格列汀、度格列汀和利格列汀的详细药理学和临床信息,并了解这些 DPP-IV 抑制剂如何拓宽整个药物类别。还讨论了各种 DPP-IV 抑制剂的可能特殊适应症。

涵盖领域

强调了 DPP-IV 抑制剂及其在 2 型糖尿病中的当前作用。介绍了新型 DPP-IV 抑制剂阿格列汀、度格列汀和利格列汀的临床前和临床研究,包括 2007 年以来的已发表数据,并对这些化合物进行了比较。

专家意见

迄今为止,DPP-IV 抑制剂的疗效和安全性特征很有希望且有利。与磺酰脲类药物不同,DPP-IV 抑制剂本身没有引起低血糖的内在风险,且对体重无影响。它们的耐受性良好,没有报告特定的不良反应。迄今为止的经验表明,DPP-IV 活性抑制本身没有安全性问题。具有独特特性的新型 DPP-IV 抑制剂可能为该药物类别提供替代选择。

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Management of patients with type 2 diabetes and mild/moderate renal impairment: profile of linagliptin.
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Safety and efficacy of linagliptin in type 2 diabetes patients with common renal and cardiovascular risk factors.利格列汀治疗伴有常见肾脏和心血管风险因素的 2 型糖尿病患者的安全性和有效性。
Ther Adv Endocrinol Metab. 2013 Jun;4(3):95-105. doi: 10.1177/2042018813486165.
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