司美格鲁肽

化合物

司美格鲁肽(英語:Semaglutide),以品牌名OzempicWegovyRybelsus销售,是由诺和诺德于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。它是一种侧链被修改的与胰高血糖素样肽-1类似的。可皮下注射也可口服。

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]

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[17] 司美格鲁肽也有可能引发胃轻瘫综合征(又称胃麻痹)。[18]

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 [2021-06-06]. (原始内容存档 (PDF)于2021-06-07).  已忽略未知参数|orig-date= (帮助)
  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. ^ Cunha JP (编). Side Effects of Wegovy (Semaglutide Injection), Warnings, Uses. RxList (part of the WebMD network). 18 January 2023 [9 March 2023]. (原始内容存档于9 March 2023). 
  18. ^ Ozempic linked to stomach paralysis, other gastrointestinal issues: UBC study | Globalnews.ca. Global News. [2023-10-05]. (原始内容存档于2023-10-05) (美国英语).