Study the effect of Dipeptidyl Peptidase 4 Inhibitors as an Antidiabetic in Type 2 Diabetes Mellitus (T2DM)

A. Yadav, P. Wal, P. Verma
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Abstract

Dipeptidyl peptidase IV is a key regulator of insulin- stimulating hormones, glucagon-like peptide and glucose dependent insulinotrophic polypeptide. Thus it is a promising target for treatment of type 2 Diabetes mellitus. Inhibition of plasma Dipeptidyl peptidase IV enzyme lead to enhanced endogenous glucagon like peptide-1, GIP activity which ultimately results in the potentiating of insulin secretion by pancreatic cell and subsequent lowering blood glucose level, HbA [1c], glucose secretion, liver glucose production. One of the principal goals of diabetes management is to attain haemoglobin HbA [1c] treatment goals and prevent the onset or decrease the rate of occurrence of Microvascular conditions.2, 6 numerous treatment options are available for management of Type 2 Diabetes mellitus, various class of DPP IV inhibitor being explored such as Sitagliptin and Vildagliptin successfully launched. Several other novel DPP IV inhibitors are in pipeline, Unless there are clear contraindications, metformin monotherapy is prescribed, and if HbA [1c] targets are not attained after 3 months, 1 of several classes of agents could be added, such as sulfonylurea’s, Thiazolidinediones, dipeptidyl peptidase-4 inhibitors, - glucagon like peptide-1 receptor agonists, or basal insulin.2,6 Despite the broad range of therapeutic options, the attainment of HbA [1c] goals among patients with diabetes remains challenging, with just slightly more than half (52%) of diabetes patients attaining the common HbA [1c] goal of < 7.0%. The present review summarizes latest preclinical and clinical trial data of different DPP IV inhibitors with a special emphasis on their DPP8/9 fold selectivity and therapeutic advantages over GLP-1 based approach. Keywords: Diabetes 2, Dipeptidyl Peptidase-4, glucose-dependent insulinot
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二肽基肽酶4抑制剂对2型糖尿病(T2DM)的降糖作用研究
二肽基肽酶IV是胰岛素刺激激素、胰高血糖素样肽和葡萄糖依赖性胰岛素营养多肽的关键调节因子。因此,它是治疗2型糖尿病的一个有希望的靶点。抑制血浆二肽基肽酶IV酶导致内源性胰高血糖素如肽-1、GIP活性增强,最终导致胰腺细胞胰岛素分泌增强,进而降低血糖水平、HbA [1c]、葡萄糖分泌、肝糖生成。糖尿病管理的主要目标之一是达到血红蛋白HbA [1c]的治疗目标,防止微血管疾病的发生或降低微血管疾病的发生率。2,6 2型糖尿病有多种治疗方案可供选择,各种类型的DPP IV抑制剂正在探索中,如西格列汀和维格列汀成功上市。其他几种新型DPP IV抑制剂正在开发中,除非有明确的禁忌症,否则应采用二甲双胍单药治疗,如果3个月后未达到HbA [1c]目标,则可添加几种药物中的一种,如磺脲类、噻唑烷二酮类、二肽基肽酶-4抑制剂、-胰高血糖素样肽-1受体激动剂或基础胰岛素。2,6尽管有广泛的治疗选择,但糖尿病患者达到HbA [1c]目标仍然具有挑战性,只有略多于一半(52%)的糖尿病患者达到了HbA [1c] < 7.0%的共同目标。本文综述了不同DPP IV抑制剂的最新临床前和临床试验数据,特别强调了它们的DPP8/9倍选择性和相对于GLP-1的治疗优势。关键词:2型糖尿病,二肽基肽酶-4,葡萄糖依赖性胰岛素
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