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药品评价 2012年第34期9卷 26-26页

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dpp‐4抑制剂类药物使用风险新进展

DPP‐4抑制剂类药物使用风险新进展

2013年中国药学大会暨第十三届中国药师周

作者：王婧雯王聪聪陆遥文爱东第四军医大学西京医院药剂科

我国糖尿病患者人数已居世界首位,双胍类、磺脲类、胰岛素等经典降糖药物在临床使用多年,医生已积累了丰富的经验,对于可能出现的不良反应具备较好预测和处理能力。二肽基肽酶Ⅳ(dpp-4)抑制剂作为新一代降糖药,2006年首次在美国上市,时... 详细信息

我国糖尿病患者人数已居世界首位,双胍类、磺脲类、胰岛素等经典降糖药物在临床使用多年,医生已积累了丰富的经验,对于可能出现的不良反应具备较好预测和处理能力。二肽基肽酶Ⅳ(dpp-4)抑制剂作为新一代降糖药,2006年首次在美国上市,时间短,临床使用经验不足。国内更多报道集中在安全性较好,不良反应发生率低。随着该类药物的广泛使用,更多的不良反应已逐渐成为关注焦点。通过文献检索,对于近3年来国际dpp-4抑制剂临床使用不良反应的报道进行分析、归纳和总结。

关键词： dpp-4 药物不良反应糖尿病

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新型口服降糖药:dpp-4抑制剂

江苏卫生保健 2016年第5期 15-15页

二肽基肽酶-4(dpp-4)抑制剂是一种新型口服抗高血糖药物。它在人体内的作用机制是多方面的:在胰岛方面,它可以在刺激β细胞分泌胰岛素的同时抑制胰高糖素的分泌,而且这种作用机制是具有葡萄糖浓度依赖性的,因而可以

关键词： dpp-4 抑制剂浮选药剂口服降糖药

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新型口服降糖药:dpp-4抑制剂

江苏卫生保健（今日保健） 2016年第3期 15-15页

二肽基肽酶-4（dpp-4）抑制剂是一种新型口服抗高血糖药物。它在人体内的作用机制是多方面的：在胰岛方面,它可以在刺激β细胞分泌胰岛素的同时抑制胰高糖素的分泌,而且这种作用机制是具有葡萄糖浓度依赖性的。

关键词：抗高血糖药物 dpp-4 口服降糖药胰高糖素葡萄糖浓度 β细胞二肽基肽酶作用机制格列胞分泌

2型糖尿病患者:dpp-4抑制剂是否导致心衰风险增加

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临床药物治疗杂志 2017年第1期15卷 86-86页

作者：李潇潇

研究背景：近日美国食品药品管理局（FDA）根据SAVOR-TIMI 53和EXAMINE两项大型临床研究的安全审查结果,就沙格列汀、阿格列汀以及含上述成分降糖药物的心衰风险进行了警告,尤其是对于伴有心血管疾病或肾脏疾病的患者。

关键词： dpp-4 沙格格列心血管疾病肾脏疾病

Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 agonists as potential neuroprotective agents

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Neural Regeneration Research 2019年第5期14卷 745-748页

作者： Shaker A.Mousa Bassam M.Ayoub Pharmaceutical Research Institute Albany College of Pharmacy and Health Sciences The Center for Drug Research and Development (CDRD) Pharmaceutical Chemistry Department Faculty of Pharmacy The British University in Egypt

Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists is a breakthrough in the field of neural regeneration research increasing glucagon like peptide-1 bioavailability, hence its neuroprotective activities. In this article, the authors suggest not only crossing blood-brain barrier and neurodegenerative disease as off target for dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists, but also for ophthalmic preparations for diabetic retinopathy, which may be the latest breakthrough in the field if prepared and used in an appropriate nano-formulation to target the retinal nerves. The relation of neurodegenerative diseases' different mechanisms to the dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 receptor agonists should be further examined in preclinical and clinical settings. The repositioning of already marketed antidiabetic drugs for neurodegenerative diseases should save the high cost of the time-consuming normal drug development process. Drug repositioning is a hot topic as an alternative to molecular target based drug discovery or therapeutic switching. It is a relatively inexpensive pathway due to availability of previous pharmacological and safety data. The glucagon like peptide-1 produced in brain has been linked to enhanced learning and memory functions as a physiologic regulator in central nervous system by restoring insulin signaling. Intranasal administration of all marketed gliptins(or glucagon like peptide-1 receptor agonists) may show enhanced blood-brain barrier crossing and increased glucagon like peptide-1 levels in the brain after direct crossing of the drug for the olfactory region, targeting the cerebrospinal fluid. Further blood-brain barrier crossing tests may extend dipeptidyl peptidase-4 inhibitors' effects beyond the anti-hyperglycemic control to intranasal spray, intranasal powder, or drops targeting the blood-brain barrier and neurodegenerative diseases wit

关键词： repositioning dpp-4 inhibitors GLP-1RA neural regeneration blood-brain barrier Parkinson’s disease Alzheimer’s disease diabetic retinopathy

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嘌呤衍生物的设计、合成及其降糖活性研究

药学学报 2023年第5期58卷 1275-1282页

作者：石素梅李惠兰刘文琴叶喜德张少坤李家辉房元英杨尊华江西中医药大学药学院江西南昌330004

基于前期工作基础,本研究采用药效团拼合原理,尝试将GPR119激动剂和dpp-4抑制剂的药效片段拼接到嘌呤环的6位和9位,设计合成了12个嘌呤类衍生物作为GPR119与dpp-4双调节剂。体外降血糖活性结果显示化合物11含有2-氟-4-甲砜基苯胺片段和... 详细信息

基于前期工作基础,本研究采用药效团拼合原理,尝试将GPR119激动剂和dpp-4抑制剂的药效片段拼接到嘌呤环的6位和9位,设计合成了12个嘌呤类衍生物作为GPR119与dpp-4双调节剂。体外降血糖活性结果显示化合物11含有2-氟-4-甲砜基苯胺片段和氰基吡咯烷片段,表现出最强的GPR119激动活性(EC50=0.33μmol·L^(-1)IA=71.1%)与dpp-4抑制活性(58.4%抑制浓度为10μmol·L^(-1),21.2%抑制浓度为1μmol·L^(-1))。对化合物进行构效关系讨论与分子对接研究,为下一步化合物的设计提供指导。

关键词： GPR119 dpp-4 设计合成降血糖活性

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Synthesis of Vildagliptin-β-<i>O</i>-Glucuronide

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Advances in Chemical Engineering and Science 2012年第3期2卷 379-383页

作者： Yansong Jack Lu Yugang Liu Mahavir Prashad Wen-Chung Shieh Chemical and Analytical Development Novartis Pharmaceuticals Corporation One Health Plaza East Hanover USA

A linear 7-step synthesis of vildagliptin-β-O-glucuronide (2) starting from commercially available D-glucurono-6, 3-lactone (3) was herein achieved with 11.3% overall yield. Efficient preparation of compound 6 in pure α form was obtained, which was proved critical to achieve high anomeric selectivity in β-O-glycosylation later. The direct β-O-glycosylation of vildagliptin (1) containing both a tertiary alcohol and a secondary amine was studied and achieved in good yield. The deprotection step to afford product was delicately executed to avoid hydrolysis of nitrile group. The target compound 2 was obtained after purification by reversed-phase C18 chromatography.

关键词： Vildagliptin O-Glycosylation dpp-4 Inhibitors Type-2 Diabetes

Clinical Characteristics of Japanese Type 2 Diabetic Patients Responsive to Sitagliptin

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Journal of Diabetes Mellitus 2014年第3期4卷 172-178页

作者： Kouichi Inukai Takumi Hirata Takashi Sumita Masaki Watanabe Yuichi Ikegami Daisuke Ito Susumu Kurihara Nobuyuki Yasukawa Jiro Morimoto Nobuki Takata Kenta Kanazawa Tamotsu Neda Yoshikazu Sumitani Kiyoaki Inoue Yuichi Noguchi Toshio Hosaka Hitoshi Ishida Shigehiro Katayama Department of Internal Medicine Saitama Social Insurance Hospital Saitama Japan Division of Endocrinology and Diabetes Saitama Medical University Saitama Japan Foundation for Biomedical Research and Innovation Hyogo Japan Sakado Central Hospital Saitama Japan Third Department of Internal Medicine Division of Diabetes Endocrinology and Metabolism Kyorin University School of Medicine Tokyo Japan Watanabe Medical Clinic Hiroshima Japan

Japanese type 2 diabetic patients were treated with sitagliptin to evaluate the efficacy of this agent, and also to investigate the clinical characteristics of those who responded to sitagliptin. In total, 1001 diabetic patients, inadequately controlled (HbA1c ≥ 6.5%) with oral hypoglycemic agents (OHA) other than dpp-4 inhibitors or with diet and exercise only, were enrolled. We added 50mg of sitagliptin to the therapeutic regimens of 410 patients including 68 OHA naive patients, while the other 591 patients were switched from a single OHA to 50 mg of sitagliptin. After 6 months, glycemic control was significantly improved due to both reduced insulin resistance, as demonstrated by a significant HOMA-R reduction, and recovery of pancreatic β cell function, as assessed by HOMA-β and the proinsulin/insulin (PI/I) ratio. In the bivariable analysis, a good response, defined as an HbA1c reduction during the 6 months of at least 0.9%, was associated with high HbA1c and PI/I at baseline and combination treatments with sulfonylurea, biguanide and α-glucosidase inhibitors, but not with obesity. On the other hand, in the multivariable regression analysis, only high baseline HbA1c and combination treatment with anα-glucosidase inhibitor were significantly associated with a good response to sitagliptin. In patients with type 2 diabetes, the addition of sitagliptin or switching from another OHA to this agent achieved an HbA1c reduction without overloading β cells. In particular, we suggest that a good response to sitagliptin can be expected when this agent is combined with an α-glucosidase inhibitor (UMIN No. #000014157).

关键词： Sitagliptin Type 2 Diabetes dpp-4 Inhibitors