跳转到内容

司美格鲁肽

维基百科,自由的百科全书
(重定向自C187H291N45O59
司美格鲁肽
臨床資料
商品名英语Drug nomenclatureOzempic, Rybelsus, Wegovy, others
AHFS/Drugs.comMonograph
MedlinePlusa618008
核准狀況
懷孕分級
给药途径皮下注射, 口服给药
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度89%
药物代谢蛋白酶解
生物半衰期7 days
作用時間63.6 h
排泄途徑Urine and feces
识别信息
CAS号910463-68-2
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ECHA InfoCard100.219.541 編輯維基數據鏈接
化学信息
化学式C187H291N45O59
摩尔质量4,113.64 g·mol−1
3D模型(JSmol英语JSmol
  • CCC(C)C(C(=O)NC(C)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCNC(=N)N)C(=O)NCC(=O)NC(CCCNC(=N)N)C(=O)NCC(=O)O)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CCC(=O)O)NC(=O)C(CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(C(C)C)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(C)(C)NC(=O)C(CC6=CN=CN6)N
  • InChI=1S/C187H291N45O59/c1-18-105(10)154(180(282)208-108(13)159(261)216-133(86-114-89-200-119-50-40-39-49-117(114)119)170(272)218-129(82-102(4)5)171(273)228-152(103(6)7)178(280)215-121(53-44-72-199-186(192)193)162(264)201-91-141(242)209-120(52-43-71-198-185(190)191)161(263)204-94-151(257)258)230-172(274)131(83-111-45-33-31-34-46-111)219-167(269)126(64-69-149(253)254)214-166(268)122(51-41-42-70-195-144(245)98-290-79-78-289-76-74-197-145(246)99-291-80-77-288-75-73-196-139(240)66-61-127(183(285)286)211-140(241)54-37-29-27-25-23-21-19-20-22-24-26-28-30-38-55-146(247)248)212-158(260)107(12)206-157(259)106(11)207-165(267)125(60-65-138(189)239)210-142(243)92-202-163(265)123(62-67-147(249)250)213-168(270)128(81-101(2)3)217-169(271)130(85-113-56-58-116(238)59-57-113)220-175(277)135(95-233)223-177(279)137(97-235)224-179(281)153(104(8)9)229-174(276)134(88-150(255)256)221-176(278)136(96-234)225-182(284)156(110(15)237)231-173(275)132(84-112-47-35-32-36-48-112)222-181(283)155(109(14)236)227-143(244)93-203-164(266)124(63-68-148(251)252)226-184(287)187(16,17)232-160(262)118(188)87-115-90-194-100-205-115/h31-36,39-40,45-50,56-59,89-90,100-110,118,120-137,152-156,200,233-238H,18-30,37-38,41-44,51-55,60-88,91-99,188H2,1-17H3,(H2,189,239)(H,194,205)(H,195,245)(H,196,240)(H,197,246)(H,201,264)(H,202,265)(H,203,266)(H,204,263)(H,206,259)(H,207,267)(H,208,282)(H,209,242)(H,210,243)(H,211,241)(H,212,260)(H,213,270)(H,214,268)(H,215,280)(H,216,261)(H,217,271)(H,218,272)(H,219,269)(H,220,277)(H,221,278)(H,222,283)(H,223,279)(H,224,281)(H,225,284)(H,226,287)(H,227,244)(H,228,273)(H,229,276)(H,230,274)(H,231,275)(H,232,262)(H,247,248)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,285,286)(H4,190,191,198)(H4,192,193,199)/t105-,106-,107-,108-,109+,110+,118-,120-,121-,122-,123-,124-,125-,126-,127+,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,152-,153-,154-,155-,156-/m0/s1
  • Key:DLSWIYLPEUIQAV-CCUURXOWSA-N checkY[pubchem]
一只于中国大陆出售的诺和泰®司美格鲁肽

司美格鲁肽INN:semaglutide)常见商品名有OzempicWegovyRybelsus等,是一种长效的胰高糖素样肽-1受体激动剂(GLP-1RA)类药物[17],由诺和诺德于2012年开发的针对2型糖尿病抗糖尿病药和用于长期体重管理的减肥药

司美格鲁肽是一种侧链被修改,且与胰高血糖素样肽-1类似的。可皮下注射也可口服。用于治疗2型糖尿病的为诺和泰(Ozempic),用于减重的则是诺和盈(Wegovy)[18]

好处

[编辑]

司美格鲁肽主要有以下好处:

副作用

[编辑]

可能的副作用包括噁心肚瀉嘔吐便秘腹痛頭痛疲倦消化不良心悸頭暈腹胀打嗝2型糖尿病患者的低血糖放屁肠胃炎胃食管反流病[30] 司美格鲁肽也有可能引发胃轻瘫综合征(又称胃麻痹)。

假药

[编辑]

世界卫生组织於2024年第2期《醫療產品警報》中發出警示:2023年10月到12月,巴西、英國與美國等地共查获三批次司美格鲁肽假药[31]

参考资料

[编辑]
  1. ^ 1.0 1.1 AusPAR: Semaglutide. Therapeutic Goods Administration (TGA). 2020-12-02 [2022-02-23]. (原始内容存档于2022-02-24). 
  2. ^ 2.0 2.1 Rybelsus APMDS. Therapeutic Goods Administration (TGA). 2022-02-22 [2022-02-23]. 
  3. ^ Summary for ARTG Entry:315107 Ozempic 1 mg semaglutide (rys) 1.34 mg/mL solution for injection pre-filled pen. Therapeutic Goods Administration (TGA). [2021-06-06]. (原始内容存档于2022-02-24). 
  4. ^ Summary for ARTG Entry: 346198 Rybelsus semaglutide 3 mg tablet blister pack. Therapeutic Goods Administration (TGA). [2022-02-23]. (原始内容存档于2022-02-24). 
  5. ^ WEGOVY (Novo Nordisk Pharmaceuticals Pty Ltd). Therapeutic Goods Administration (TGA). 2022-10-07 [2023-04-07]. (原始内容存档于2023-04-14). 
  6. ^ Product Monograph Including Patient Medication Information – Ozempic semaglutide injection (PDF) (报告). Novo-Nordisk Canada. 2020-08-21 [Initial approval 4 January 2018] [2021-06-06]. (原始内容存档 (PDF)于2021-06-07). 
  7. ^ Product Monograph Including Patient Medication Information – Rybelsus semaglutide tablets (PDF) (报告). Novo-Nordisk Canada. 2020-03-30 [2021-06-06]. (原始内容存档 (PDF)于2021-12-14). 
  8. ^ Regulatory Decision Summary – Rybelsus. Health Canada. 2014-10-23 [2022-06-04]. (原始内容存档于2022-06-05). 
  9. ^ Ozempic 0.25 mg solution for injection in pre-filled pen – Summary of Product Characteristics (SmPC). (emc). 2021-04-09 [2021-06-06]. (原始内容存档于2021-06-06). 
  10. ^ Rybelsus – Summary of Product Characteristics (SmPC). (emc). 2020-11-25 [2021-06-06]. (原始内容存档于2021-06-06). 
  11. ^ Ozempic- semaglutide injection, solution. DailyMed. [2021-06-05]. (原始内容存档于2021-06-05). 
  12. ^ Rybelsus- oral semaglutide tablet. DailyMed. [2021-06-05]. (原始内容存档于2021-06-05). 
  13. ^ Wegovy- semaglutide injection, solution. DailyMed. 2021-06-04 [2022-03-11]. (原始内容存档于2021-12-14). 
  14. ^ Ozempic EPAR. European Medicines Agency (EMA). 2018-09-17 [2020-09-26]. (原始内容存档于2020-10-25). 
  15. ^ Rybelsus EPAR. European Medicines Agency (EMA). 2020-01-29 [2020-09-26]. (原始内容存档于2020-08-14). 
  16. ^ Wegovy EPAR. European Medicines Agency. 2021-11-11 [2022-03-11]. (原始内容存档于2022-07-02). 
  17. ^ 金岩,林武,郑焱,等. 司美格鲁肽临床应用浅谈[J]. 中华糖尿病杂志,2022,14(Z1):35-37. DOI:10.3760/cma.j.cn115791-20220721-00357
  18. ^ 鸠江区科学技术局(科协). 世界上从来没有“减肥神药”. 鸠江区人民政府. 2024-06-28 [2024-11-18] –通过芜湖市政务公开平台 (中文). [失效連結]
  19. ^ 张文豹. Semaglutide for weight loss you need to know - semaglutide user guide. semaglutide user guide. 2024-04-29. (原始内容存档于2024-05-24) (美国英语).  |url-status=|dead-url=只需其一 (帮助)
  20. ^ Bliddal, Henning; Bays, Harold; Czernichow, Sébastien; Uddén Hemmingsson, Joanna; Hjelmesæth, Jøran; Hoffmann Morville, Thomas; Koroleva, Anna; Skov Neergaard, Jesper; Vélez Sánchez, Patricia; Wharton, Sean; Wizert, Alicja. Once-Weekly Semaglutide in Persons with Obesity and Knee Osteoarthritis. The New England Journal of Medicine. 2024-10-31, 391 (17) [2025-05-12]. ISSN 1533-4406. PMID 39476339. doi:10.1056/NEJMoa2403664. (原始内容存档于2025-03-17). 
  21. ^ Wang, Lindsey; Xu, Rong; Kaelber, David C.; Berger, Nathan A. Glucagon-Like Peptide 1 Receptor Agonists and 13 Obesity-Associated Cancers in Patients With Type 2 Diabetes. JAMA network open. 2024-07-01, 7 (7) [2025-05-12]. ISSN 2574-3805. PMC 11227080可免费查阅. PMID 38967919. doi:10.1001/jamanetworkopen.2024.21305. (原始内容存档于2025-02-20). 
  22. ^ 22.0 22.1 22.2 中国疾病预防控制中心. 华人团队发现,“减肥神药”司美格鲁肽或可显著降低阿尔茨海默病风险. 中国疾病预防控制中心科技文献服务系统. 2024-11-26 [2025-05-12]. (原始内容存档于2024-12-12). 
  23. ^ Wang, William; Volkow, Nora D.; Berger, Nathan A.; Davis, Pamela B.; Kaelber, David C.; Xu, Rong. Associations of semaglutide with incidence and recurrence of alcohol use disorder in real-world population. Nature Communications. 2024-05-28, 15 (1) [2025-05-12]. ISSN 2041-1723. PMC 11133479可免费查阅. PMID 38806481. doi:10.1038/s41467-024-48780-6. (原始内容存档于2025-04-15). 
  24. ^ Wang, William; Volkow, Nora D.; Berger, Nathan A.; Davis, Pamela B.; Kaelber, David C.; Xu, Rong. Association of semaglutide with reduced incidence and relapse of cannabis use disorder in real-world populations: a retrospective cohort study. Molecular Psychiatry. 2024-08, 29 (8) [2025-05-12]. ISSN 1476-5578. PMC 11412894可免费查阅. PMID 38486046. doi:10.1038/s41380-024-02498-5. (原始内容存档于2025-02-23). 
  25. ^ Apperloo, Ellen M.; Gorriz, Jose L.; Soler, Maria Jose; Cigarrán Guldris, Secundino; Cruzado, Josep M.; Puchades, Maria Jesús; López-Martínez, Marina; Waanders, Femke; Laverman, Gozewijn D.; van der Aart-van der Beek, Annemarie; Hoogenberg, Klaas. Semaglutide in patients with overweight or obesity and chronic kidney disease without diabetes: a randomized double-blind placebo-controlled clinical trial. Nature Medicine. 2025-01, 31 (1) [2025-05-12]. ISSN 1546-170X. doi:10.1038/s41591-024-03327-6. (原始内容存档于2025-04-30) (英语). 
  26. ^ Wang, William; Wang, QuangQiu; Qi, Xin; Gurney, Mark; Perry, George; Volkow, Nora D.; Davis, Pamela B.; Kaelber, David C.; Xu, Rong. Associations of semaglutide with first-time diagnosis of Alzheimer's disease in patients with type 2 diabetes: Target trial emulation using nationwide real-world data in the US. Alzheimer's & Dementia: The Journal of the Alzheimer's Association. 2024-12, 20 (12) [2025-05-12]. ISSN 1552-5279. PMC 11667504可免费查阅. PMID 39445596. doi:10.1002/alz.14313. (原始内容存档于2025-05-03). 
  27. ^ Sanyal, Arun J.; Newsome, Philip N.; Kliers, Iris; Østergaard, Laura Harms; Long, Michelle T.; Kjær, Mette Skalshøi; Cali, Anna M. G.; Bugianesi, Elisabetta; Rinella, Mary E.; Roden, Michael; Ratziu, Vlad. Phase 3 Trial of Semaglutide in Metabolic Dysfunction-Associated Steatohepatitis. The New England Journal of Medicine. 2025-04-30 [2025-05-12]. ISSN 1533-4406. PMID 40305708 请检查|pmid=值 (帮助). doi:10.1056/NEJMoa2413258. 
  28. ^ McGuire, Darren K.; Marx, Nikolaus; Mulvagh, Sharon L.; Deanfield, John E.; Inzucchi, Silvio E.; Pop-Busui, Rodica; Mann, Johannes F. E.; Emerson, Scott S.; Poulter, Neil R.; Engelmann, Mads D. M.; Ripa, Maria Sejersten. Oral Semaglutide and Cardiovascular Outcomes in High-Risk Type 2 Diabetes. The New England Journal of Medicine. 2025-03-29 [2025-05-12]. ISSN 1533-4406. PMID 40162642 请检查|pmid=值 (帮助). doi:10.1056/NEJMoa2501006. (原始内容存档于2025-04-04). 
  29. ^ Wang, William; Volkow, Nora D.; Berger, Nathan A.; Davis, Pamela B.; Kaelber, David C.; Xu, Rong. Association of semaglutide with risk of suicidal ideation in a real-world cohort. Nature Medicine. 2024-01, 30 (1) [2025-05-12]. ISSN 1546-170X. PMC 11034947可免费查阅. PMID 38182782. doi:10.1038/s41591-023-02672-2. 
  30. ^ Cunha JP (编). Side Effects of Wegovy (Semaglutide Injection), Warnings, Uses. RxList (part of the WebMD network). 2023-01-18 [2023-03-09]. (原始内容存档于2023-03-09). 
  31. ^ 医疗产品警报2024年第2期. 世界卫生组织. 2024-06-19 [2025-03-17]. (原始内容存档于2024-07-05) (中文). 

https://www.who.int/news/item/20-06-2024-who-issues-warning-on-falsified-medicines-used-for-diabetes-treatment-and-weight-loss页面存档备份,存于互联网档案馆