貝拉布韋

貝拉布韋
臨床資料
其他名稱	BMS-791325
法律規範狀態
法律規範	美：IND;
識別資訊
	IUPAC命名法 (1aR,12bS)-8-Cyclohexyl-N-(dimethylsulfamoyl)-11-methoxy-1a[(1R,5S)-3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl]carbonyl1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a] [2]benzazepine-5-carboxamide; ;
CAS號	958002-33-0
PubChem CID	56934415;
ChemSpider	27289076;
UNII	MYW1X5CO9S;
KEGG	D10610 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID701026084 ;
化學資訊
化學式	C36H45N5O5S
摩爾質量	659.85 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES CN1C[C@H]2CC[C@@H](C1)N2C(=O)[C@]34C[C@H]3c5cc(ccc5-c6c(c7ccc(cc7n6C4)C(=O)NS(=O)(=O)N(C)C)C8CCCCC8)OC;
	InChI InChI=1S/C36H45N5O5S/c1-38(2)47(44,45)37-34(42)23-10-14-28-31(16-23)40-21-36(35(43)41-24-11-12-25(41)20-39(3)19-24)18-30(36)29-17-26(46-4)13-15-27(29)33(40)32(28)22-8-6-5-7-9-22/h10,13-17,22,24-25,30H,5-9,11-12,18-21H2,1-4H3,(H,37,42)/t24-,25+,30-,36-/m0/s1; Key:ZTTKEBYSXUCBSE-QDFUAKMASA-N;

貝拉布韋（INN：Beclabuvir；開發代號：BMS-791325）是一種用於治療丙型肝炎病毒（HCV）感染的抗病毒藥物，已在臨床試驗中進行研究。2017年2月，百時美施貴寶開始贊助一項後市場試驗，將貝拉布韋與阿舒瑞韋和達拉他韋聯合使用，以研究該組合在肝功能方面的安全性。^[1]2014年2月至2016年11月，對同時感染HIV和HCV的患者進行了阿舒瑞韋/達拉他韋/貝拉布韋複方藥的II期臨床試驗。^[2]此外，最近對六項已發表的臨床試驗進行的元分析顯示，無論是否使用利巴韋林、先前是否採用干擾素為基礎的治療、對非肝硬化患者的限制、IL28B基因型或基線耐藥相關變異，使用達拉他韋、阿舒瑞韋和貝拉布韋治療的HCV基因型1感染患者均顯示出高響應率。^[3]

藥理學

貝拉布韋充當NS5B（RNA聚合酶）抑制劑。^[4]

參考資料

^ Clinical trial number NCT03071133 for "Asunaprevir/Daclatasvir/Beclabuvir Fixed-Dose Combination Safety Surveillance in Japanese Patients With Chronic Hepatitis C (HCV) or Japanese Patients With Compensated Cirrhosis" at ClinicalTrials.gov
^ Clinical trial number NCT02124044 for "Safety, Tolerability, and Efficacy of Asunaprevir and Daclatasvir in Subjects Coinfected With HIV-HCV" at ClinicalTrials.gov
^ Ahmed AM, Doheim MF, Mattar OM, Sherif NA, Truong DH, Hoa PT, et al. Beclabuvir in combination with asunaprevir and daclatasvir for hepatitis C virus genotype 1 infection: A systematic review and meta-analysis. Journal of Medical Virology. May 2018, 90 (5): 907–918. PMID 28892235. S2CID 3829214. doi:10.1002/jmv.24947.
^ Tatum H, Thuluvath PJ, Lawitz E, Martorell C, DeMicco M, Cohen S, et al. A randomized, placebo-controlled study of the NS5B inhibitor beclabuvir with peginterferon/ribavirin for HCV genotype 1. Journal of Viral Hepatitis. August 2015, 22 (8): 658–64. PMID 25496007. doi:10.1111/jvh.12372.

[Japanese_Hepatic_Trio_Trial-1] Clinical trial number NCT03071133 for "Asunaprevir/Daclatasvir/Beclabuvir Fixed-Dose Combination Safety Surveillance in Japanese Patients With Chronic Hepatitis C (HCV) or Japanese Patients With Compensated Cirrhosis" at ClinicalTrials.gov

[HIV-HCV_Coinfx_Trial-2] Clinical trial number NCT02124044 for "Safety, Tolerability, and Efficacy of Asunaprevir and Daclatasvir in Subjects Coinfected With HIV-HCV" at ClinicalTrials.gov

[3] Ahmed AM, Doheim MF, Mattar OM, Sherif NA, Truong DH, Hoa PT, et al. Beclabuvir in combination with asunaprevir and daclatasvir for hepatitis C virus genotype 1 infection: A systematic review and meta-analysis. Journal of Medical Virology. May 2018, 90 (5): 907–918. PMID 28892235. S2CID 3829214. doi:10.1002/jmv.24947.

[4] Tatum H, Thuluvath PJ, Lawitz E, Martorell C, DeMicco M, Cohen S, et al. A randomized, placebo-controlled study of the NS5B inhibitor beclabuvir with peginterferon/ribavirin for HCV genotype 1. Journal of Viral Hepatitis. August 2015, 22 (8): 658–64. PMID 25496007. doi:10.1111/jvh.12372.

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