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首页> 外文期刊>Current Diabetes Reviews >Alogliptin: a Novel Molecule for Improving Glycemic Control in Type II Diabetes Mellitus
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Alogliptin: a Novel Molecule for Improving Glycemic Control in Type II Diabetes Mellitus

机译:阿格列汀:一种新型分子,以改善II型糖尿病的血糖控制。

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Type 2 diabetes mellitus causes significant morbidity and mortality on account of its progressive nature and results in considerable burden on healthcare resources. It is characterized by high circulating levels of glucose resulting from insulin resistance and impaired insulin secretion. Current treatment strategies have only limited long-term efficacy and tolerability given the progressive nature of the disease leading to inadequate glycemic control and are also associated with undesirable side effects such as weight gain, hypoglycemia and gastrointestinal distress. In the light of these existing limitations, exploring new treatment targets and new therapies have become the need of the hour at present. The incretin pathway, in particular, glucagon-like peptide (GLP-1), plays an important pathological role in the development of type 2 diabetes mellitus, and treatments targeting the incretin system have recently generated surmount interest. These can mainly be categorized into two broad classes; GLP-1 agonists/analogs (exenatide, liraglutide), and dipeptidyl peptidase- 4 inhibitors (sitagliptin, vildagliptin). The gliptins act by prolonging the action of incretins, the gut hormones which can boost insulin levels. Alogliptin is a potent, highly selective dipeptidyl peptidase-4 inhibitor now undergoing clinical testing to support a new drug application for the treatment of type 2 diabetes. The results of Phase II and Phase III human studies, upon evaluation for clinical efficacy, safety and tolerability in patients with type 2 diabetes, have demonstrated that Alogliptin is effective and well tolerated as a treatment for type 2 diabetes, either as monotherapy or in combination with metformin, thiazolidinediones, sulfonylureas and insulin, with an excellent safety profile.
机译:2型糖尿病由于其不断发展的性质而导致明显的发病率和死亡率,并给医疗资源造成相当大的负担。它的特点是胰岛素抵抗和胰岛素分泌受损导致葡萄糖的高循环水平。鉴于疾病的进展性质导致血糖控制不足,目前的治疗策略仅具有有限的长期疗效和耐受性,并且还与不良副作用如体重增加,低血糖和胃肠道不适有关。鉴于这些现有的局限性,探索新的治疗目标和新疗法已成为当前的当务之急。肠降血糖素途径,尤其是胰高血糖素样肽(GLP-1),在2型糖尿病的发展中起着重要的病理作用,最近针对肠降血糖素系统的治疗引起了人们的极大兴趣。这些主要可以分为两大类: GLP-1激动剂/类似物(艾塞那肽,利拉鲁肽)和二肽基肽酶-4抑制剂(西格列汀,维格列汀)。脂肪素通过延长肠降血糖素的作用来发挥作用,肠降血糖素可以提高胰岛素水平。阿格列汀是一种有效的,高度选择性的二肽基肽酶-4抑制剂,目前正在接受临床测试,以支持用于治疗2型糖尿病的新药物应用。在评估2型糖尿病患者的临床疗效,安全性和耐受性后,II期和III期人体研究的结果表明,阿格列汀作为2型糖尿病的单一疗法或联合疗法均有效且耐受性良好含二甲双胍,噻唑烷二酮,磺酰脲类和胰岛素,具有出色的安全性。

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