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二肽基肽酶-4抑制剂

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DPP-4抑制剂和GLP-1
DPP-4抑制剂和GLP-1

二肽基肽酶-4抑制剂(英语:Dipeptidyl peptidase-4 inhibitor,或称DPP-4 抑制剂列汀类药物,是一种通过抑制二肽基肽酶-4来发挥作用的口服抗糖尿病药 ,用来治疗2型糖尿病

第一种二肽基肽酶-4抑制剂是西格列汀,于2006年通过了美国食品药品监督管理局(USFDA)的审批。[1]

胰高血糖素提高血糖水平,DPP-4抑制剂可以减少胰高血糖素和降低血糖水平。DPP-4抑制剂的原理为增加可以抑制胰高血糖素释放的肠促胰岛素激素的水平(GLP-1(胰高血糖素样多肽-1)和GIP(葡萄糖依赖性促胰岛素多肽)),增加胰岛素分泌,减慢胃排空,降低血糖水平。[2][3][4]

近期的芸萃分析(meta)发现,DPP-4抑制剂不会影响全因死亡率、心血管疾病死亡率及中风的风险,但是发生心力衰竭的几率有轻微的统计学上的上升。[5]

药物列表

其它也可抑制二肽基肽酶-4的成分:

引用

  1. ^ FDA Approves New Treatment for Diabetes (新闻稿). U.S. Food and Drug Administration. October 17, 2006 [2006-10-17]. 
  2. ^ McIntosh, C; Demuth, H; Pospisilik, J; Pederson, R. Dipeptidyl peptidase IV inhibitors: How do they work as new antidiabetic agents?. Regulatory Peptides. 2005, 128 (2): 159–65. PMID 15780435. doi:10.1016/j.regpep.2004.06.001. 
  3. ^ Behme, Margaret T; Dupré, John; McDonald, Thomas J. Glucagon-like peptide 1 improved glycemic control in type 1 diabetes. BMC Endocrine Disorders. 2003, 3 (1): 3. PMC 154101. PMID 12697069. doi:10.1186/1472-6823-3-3. 
  4. ^ Dupre, J.; Behme, M. T.; Hramiak, I. M.; McFarlane, P.; Williamson, M. P.; Zabel, P.; McDonald, T. J. Glucagon-like peptide I reduces postprandial glycemic excursions in IDDM. Diabetes. 1995, 44 (6): 626–30. PMID 7789625. doi:10.2337/diabetes.44.6.626. 
  5. ^ Wu S, Hopper I, Skiba M, Krum H. Dipeptidyl peptidase-4 inhibitors and cardiovascular outcomes: Meta-analysis of randomized clinical trials with 55,141 participants. Cardiovasc Ther. April 2014. PMID 24750644. doi:10.1111/1755-5922.12075. 
  6. ^ Banting and Best Diabetes Centre at UT sitagliptin
  7. ^ Banting and Best Diabetes Centre at UT vildagliptin
  8. ^ FDA approves new treatment for Type 2 diabetes. Fda.gov. 2011-05-02 [2013-04-15]. 
  9. ^ 存档副本 (PDF). [2013-08-07]. (原始内容 (PDF)存档于2013-07-18). 
  10. ^ Joanne Bronson, Amelia Black, T. G. Murali Dhar, Bruce A. Ellsworth, and J. Robert Merritt. Teneligliptin (Antidiabetic). Annual Reports in Medicinal Chemistry: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4.  |chapter=被忽略 (帮助)
  11. ^ LG Life Science. Lgls.com. [2013-04-15]. [永久失效链接]
  12. ^ "Forest Splits With Phenomix", San Diego Business Journal, Tuesday, April 20, 2010 http://www.sdbj.com/news/2010/apr/20/forest-splits-phenomix/
  13. ^ Safety and Efficacy of Omarigliptin (MK-3102), a Novel Once-Weekly DPP-4 Inhibitor for the Treatment of Patients With Type 2 Diabetes. [18 September 2015]. 
  14. ^ 默沙东终止长效DPP4抑制剂omarigliptin研发. 美中药源. [2018-03-16] (中文(简体)‎). 
  15. ^ Al-Masri, Ihab M.; Mohammad, Mohammad K.; Tahaa, Mutasem O. Inhibition of dipeptidyl peptidase IV (DPP IV) is one of the mechanisms explaining the hypoglycemic effect of berberine. Journal of Enzyme Inhibition and Medicinal Chemistry. 2009, 24 (5): 1061–6. PMID 19640223. doi:10.1080/14756360802610761. 
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二肽基肽酶-4抑制剂
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