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玛仕度肽

维基百科，自由的百科全书
玛仕度肽
臨床資料
其他名稱IBI362; LY3305677
法律規範狀態
法律規範
识别信息
  • 20-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]hexanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[2-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid
CAS号2259884-03-0
PubChem CID
UNII
化学信息
化学式C210H322N46O67
摩尔质量4,563.14 g·mol−1
3D模型（JSmol（英语：JSmol））
  • C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)NCC(=O)N7CCC[C@H]7C(=O)N[C@@H](CO)C(=O)NCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C(C)(C)NC(=O)[C@H](CC8=CNC=N8)N)O
  • InChI=1S/C207H317N45O65/c1-116(2)93-144(189(295)230-138(70-76-168(271)272)179(285)221-107-162(264)219-109-166(268)252-86-46-57-157(252)201(307)245-154(110-253)181(287)220-106-159(213)261)234-190(296)145(94-117(3)4)236-194(300)151(100-127-104-218-133-52-37-36-51-131(127)133)240-188(294)142(73-79-171(277)278)233-202(308)174(119(7)8)249-197(303)149(96-123-47-30-28-31-48-123)238-187(293)141(72-78-170(275)276)231-183(289)135(56-41-45-83-215-164(266)113-316-91-90-315-88-85-217-165(267)114-317-92-89-314-87-84-216-160(262)75-69-143(205(311)312)225-161(263)58-34-26-24-22-20-18-16-14-15-17-19-21-23-25-27-35-59-167(269)270)226-177(283)120(9)224-182(288)134(53-38-42-80-208)227-184(290)136(54-39-43-81-209)228-186(292)140(71-77-169(273)274)232-195(301)152(102-172(279)280)241-191(297)146(95-118(5)6)235-192(298)147(98-125-60-64-129(258)65-61-125)237-185(291)137(55-40-44-82-210)229-199(305)155(111-254)244-193(299)148(99-126-62-66-130(259)67-63-126)239-196(302)153(103-173(281)282)242-200(306)156(112-255)246-204(310)176(122(11)257)250-198(304)150(97-124-49-32-29-33-50-124)243-203(309)175(121(10)256)248-163(265)108-222-180(286)139(68-74-158(212)260)247-206(313)207(12,13)251-178(284)132(211)101-128-105-214-115-223-128/h28-33,36-37,47-52,60-67,104-105,115-122,132,134-157,174-176,218,253-259H,14-27,34-35,38-46,53-59,68-103,106-114,208-211H2,1-13H3,(H2,212,260)(H2,213,261)(H,214,223)(H,215,266)(H,216,262)(H,217,267)(H,219,264)(H,220,287)(H,221,285)(H,222,286)(H,224,288)(H,225,263)(H,226,283)(H,227,290)(H,228,292)(H,229,305)(H,230,295)(H,231,289)(H,232,301)(H,233,308)(H,234,296)(H,235,298)(H,236,300)(H,237,291)(H,238,293)(H,239,302)(H,240,294)(H,241,297)(H,242,306)(H,243,309)(H,244,299)(H,245,307)(H,246,310)(H,247,313)(H,248,265)(H,249,303)(H,250,304)(H,251,284)(H,269,270)(H,271,272)(H,273,274)(H,275,276)(H,277,278)(H,279,280)(H,281,282)(H,311,312)/t120-,121+,122+,132-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,174-,175-,176-/m0/s1
  • Key:XRBYWQZGSZWYEJ-HMQIFOERSA-N

玛仕度肽（英語：Mazdutide，信達生物研发代号：IBI362，礼来制药研发代号：LY3305677）是GLP-1受体（英语：Glucagon-like peptide-1 receptor）和胰高血糖素受体（英语：Glucagon receptor）的双重激动剂。它是胃泌酸调节素（英语：Oxyntomodulin）（OXM）的类似物[1][2][3] 。该药物由信達生物和礼来制药共同开发，正在进行多项III期临床试验[4][5]。2025年5月，一项III期临床试验结果显示，每周一次使用玛仕度肽，对于超重或肥胖的中国成年人获得了具有临床意义的减重效果[6]。

参考来源

[编辑]
  1. ^ Jiang, Hongwei; Pang, Shuguang; Zhang, Yawei; Yu, Ting; Liu, Meng; Deng, Huan; Li, Li; Feng, Liqi; Song, Baili; Han-Zhang, Han; Ma, Qingyang; Qian, Lei; Yang, Wenying. A phase 1b randomised controlled trial of a glucagon-like peptide-1 and glucagon receptor dual agonist IBI362 (LY3305677) in Chinese patients with type 2 diabetes. Nature Communications. 2022-06-24, 13 (1): 3613. Bibcode:2022NatCo..13.3613J. ISSN 2041-1723. PMC 9232612 可免费查阅. PMID 35750681. doi:10.1038/s41467-022-31328-x 可免费查阅 （英语）. 
  2. ^ Ji, Linong; Gao, Leili; Jiang, Hongwei; Yang, Jing; Yu, Lei; Wen, Jie; Cai, Chenghang; Deng, Huan; Feng, Liqi; Song, Baili; Ma, Qingyang; Qian, Lei. Safety and efficacy of a GLP-1 and glucagon receptor dual agonist mazdutide (IBI362) 9 mg and 10 mg in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple-ascending-dose phase 1b trial. eClinicalMedicine. 2022-12, 54: 101691. PMC 9561728 可免费查阅. PMID 36247927. doi:10.1016/j.eclinm.2022.101691 可免费查阅. 
  3. ^ Ji, Linong; Jiang, Hongwei; An, Pei; Deng, Huan; Liu, Meng; Li, Li; Feng, Liqi; Song, Baili; Han-Zhang, Han; Ma, Qingyang; Qian, Lei. IBI362 (LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study. eClinicalMedicine. 2021-09, 39: 101088. PMC 8374649 可免费查阅. PMID 34430840. doi:10.1016/j.eclinm.2021.101088 可免费查阅. 
  4. ^ Deswal, Phalguni. EASD 2024: Innovent shows off mazdutide's efficacy in diabetes and obesity. Clinical Trials Arena. 2024-09-12 [2024-11-10] （美国英语）. 
  5. ^ Next-gen Lilly obesity drug slashes weight in Innovent study—but is it enough to rival Mounjaro?. [2023-11-04]. 
  6. ^ Linong Ji, Hongwei Jiang, Yan Bi, Hua Li, Junhang Tian, Dexue Liu, Yuzhu Zhao, Wei Qiu, Chongbing Huang, Lei Chen, Shao Zhong, Jie Han, Yawei Zhang, Qiufang Lian, Ping Yang, Lingchun Lv, Jieyu Gu, Zihan Liu, Huan Deng, Yanqi Wang, Li Li, Lijuan Pei, Lei Qian. Once-Weekly Mazdutide in Chinese Adults with Obesity or Overweight. New England Journal of Medicine. 2025-05-24. doi:10.1056/NEJMoa2411528. 
检索自“https://zh.wikipedia.org/w/index.php?title=玛仕度肽&oldid=87698452”