阿舒瑞韋INN:Asunaprevir;開發代號:BMS-650032),在日本和俄羅斯的商品名為Sunvepra,[2]是一種治療C型肝炎的實驗性候選藥物,由百時美施貴寶公司開發,已於2013年完成III期臨床試驗。[3]

阿舒瑞韋
IUPAC名
3-Methyl-N[(2-methyl-2-propanyl)oxy]carbonylL-valyl-(4R)-4-[(7-chloro-4-methoxy-1-isoquinolinyl)oxy]-N(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-vinylcyclopropylL-prolinamide
系統名
tert-Butyl {(2S)-1-[(32S,34R,61R,62S)-17-chloro-62-ethenyl-14-methoxy-4,7,9,9-tetraoxo-2-oxa-9λ6-thia-5,8-diaza-1(1)-isoquinolina-3(4,2)-pyrrolidina-6(1,1),10(1)-dicyclopropadecaphan-31-yl]-3,3-dimethyl-1-oxobutan-2-yl}carbamate
別名 BMS-650032
識別
CAS號 630420-16-5  checkY
PubChem 16076883
ChemSpider 17235944
SMILES
 
  • O=C(N5[C@H](C(=O)N[C@@]2(C(=O)NS(=O)(=O)C1CC1)[C@H](\C=C)C2)C[C@@H](Oc3ncc(OC)c4c3cc(Cl)cc4)C5)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C
InChI
 
  • 1/C35H46ClN5O9S/c1-9-19-16-35(19,31(44)40-51(46,47)22-11-12-22)39-28(42)25-15-21(49-29-24-14-20(36)10-13-23(24)26(48-8)17-37-29)18-41(25)30(43)27(33(2,3)4)38-32(45)50-34(5,6)7/h9-10,13-14,17,19,21-22,25,27H,1,11-12,15-16,18H2,2-8H3,(H,38,45)(H,39,42)(H,40,44)/t19-,21-,25+,27-,35-/m1/s1
InChIKey XRWSZZJLZRKHHD-WVWIJVSJBJ
ChEBI 134723
DrugBank DB11586
KEGG D10093
IUPHAR配體 10882
性質
化學式 C35H46ClN5O9S
摩爾質量 748.29 g·mol−1
藥理學
ATC代碼 J05AP06J05
藥品分級
若非註明,所有數據均出自標準狀態(25 ℃,100 kPa)下。

阿舒瑞韋是C型肝炎病毒絲氨酸蛋白酶NS3抑制劑[4]阿舒瑞韋與聚乙二醇干擾素利巴韋林的藥物組合正在進行測試,以及與其他直接作用抗病毒藥物(包括達拉他韋)在無干擾素方案中的聯合測試。[5][6][7]

參考資料

編輯
  1. ^ Prescription medicines: registration of new chemical entities in Australia, 2015. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023]. (原始內容存檔於2023-04-10). 
  2. ^ Sunvepra (asunaprevir) soft gelatin capsules 100 mg. Registration certificate. State Register of Medicines. [26 August 2015]. (原始內容存檔於2016-03-04) (Russian). 
  3. ^ A Phase 3 Study in Combination With BMS-790052 and BMS-650032 in Japanese Hepatitis C Virus (HCV) Patients. ClinicalTrials.gov. 23 September 2015 [2024-03-03]. (原始內容存檔於2014-07-14). 
  4. ^ C. Reviriego. Asunaprevir. HCV serine protein NS3 inhibitor, Treatment of hepatitis C virus. Drugs of the Future. 2012, 37 (4): 247–254 [2024-03-03]. doi:10.1358/dof.2012.037.04.1789350. (原始內容存檔於2018-06-03). 
  5. ^ Lok AS, Gardiner DF, Lawitz E, Martorell C, Everson GT, Ghalib R, Reindollar R, Rustgi V, McPhee F, Wind-Rotolo M, Persson A, Zhu K, Dimitrova DI, Eley T, Guo T, Grasela DM, Pasquinelli C. Preliminary study of two antiviral agents for hepatitis C genotype 1. The New England Journal of Medicine. January 2012, 366 (3): 216–24. PMID 22256805. doi:10.1056/NEJMoa1104430 . 
  6. ^ Bristol-Myers' Daclatasvir, Asunaprevir Cured 77%: Study. Bloomberg. Apr 19, 2012 [2024-03-03]. (原始內容存檔於2014-01-18). 
  7. ^ AASLD: Daclatasvir plus Asunaprevir Rapidly Suppresses HCV in Prior Null Responders 網際網路檔案館存檔,存檔日期2015-02-08.. Highleyman, L. HIVandHepatitis.com. 8 November 2011.