抗2型糖尿病药物靶标计量分析及趋势研究  

Quantitative analysis and developing trends of anti-type 2 diabetes drug targets

作　　者：郝博济[1] 刘序[1] 赵梓辰[1] 杜鹏[1] 

机构地区：[1]天津市科学技术信息研究所,天津300074

出　　处：《中国新药杂志》2013年第11期1236-1241,共6页Chinese Journal of New Drugs

基　　金：天津市科技支撑计划重大项目(11SYSYJH00100);天津市科技型中小企业服务网关键技术研究与开发(11ZXPTJH00200)

摘　　要：本文借助Thomson Reuters Pharma信息平台,以不同靶标药物在各研发阶段的数量分布为主要参考指标,辅以相关文献和典型药物资料,对抗2型糖尿病药物的研发现状进行了统计、分析和研究(截至2012年5月),并对其可能的发展趋势和方向做出了判断和预测。得出以下主要结论:①IR是目前2型糖尿病常用药物普遍采用的靶标,但在研药物靶标正呈现多样化。②GLP-1受体和DPP-IV是新药开发最具潜力的靶标,大批新药项目在研,已上市药物也取得了巨大成功。③PPAR靶标药物已被大量研究用于2型糖尿病的治疗,在研药物关注瞄准两个以上PPAR靶点的多重激动剂,然而,一大批终止研发的PPAR新药项目以及对PPAR药物安全性的忧虑使PPAR靶标药物的研发前景蒙上阴影。④SGLT2靶标药物已有多例进入III期临床试验,距离成功只有一步,考虑到该类药物终止研发的数量较少以及还未发现明显的不良反应,SGLT2靶标药物具有较大的研发空间和良好的发展前景。⑤GK和GPR119是抗2型糖尿病领域的新兴靶标,最高研发阶段为II期临床试验。With the Thomson Reuters Pharma information platform, anti-type 2 diabetes drug targets at development stages were searched by statistical analysis method. The major trends and directions of anti-type 2 diabetes drug development were analyzed. The main conclusions of this article can be summarized as follows： ① Insulin receptor is the most common target of the listed anti-type 2 diabetes drugs, while targets of drugs under investigation become more diverse. ② GLP-1 receptor and DPP-IV are involved in a large number of new drug programs, have achieved a great success in listed drugs, and are the most promising targets in new drug R＆D. ③ Multiple PPAR agonists have two or more targets, and represent the research direction of new PPAR drugs. However, safety doubts of the PPAR class due to high-profile discontinuations cast a shadow over the prospects of PPAR drugs. ④ As more SGLT2 drugs have accessed into phase III clinical trials, the application of SGLT2 targets is much closer to success. Low-profile discontinuations and a relatively clear side effect profile of SGLT-2 inhibitors make a large R＆D field and good prospect. ⑤ GK and GPR119 are emerging targets in the research field of anti-type 2 diabetes drugs; they are in the development stages, some of them are investigated in phase II clinical trials.

关 键 词：胰岛素受体 胰高血糖素样肽-1受体 二肽基肽酶IV 过氧化物酶体增殖物活化受体 钠-葡萄糖协同转运蛋白2 葡萄糖激酶 G蛋白偶联受体119 

分 类 号：R95[医药卫生—药学]