贝拉布韦

贝拉布韦
臨床資料
其他名稱	BMS-791325
法律規範狀態
法律規範	美：IND;
识别信息
	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号	958002-33-0
PubChem CID	56934415;
ChemSpider	27289076;
UNII	MYW1X5CO9S;
KEGG	D10610 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID701026084 ;
化学信息
化学式	C36H45N5O5S
摩尔质量	659.85 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	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;

贝拉布韦（INN：Beclabuvir；开发代号：BMS-791325）是一种用于治疗丙型肝炎病毒（HCV）感染的抗病毒药物，已在临床试验中进行研究。2017年2月，百时美施贵宝开始赞助一项后市场试验，将贝拉布韦与阿舒瑞韦和达拉他韦联合使用，以研究该组合在肝功能方面的安全性。^[1]2014年2月至2016年11月，对同时感染HIV和HCV的患者进行了阿舒瑞韦/达拉他韦/贝拉布韦复方药的II期临床试验。^[2]此外，最近对六项已发表的临床试验进行的元分析显示，无论是否使用利巴韦林、先前是否采用干扰素为基础的治疗、对非肝硬化患者的限制、IL28B基因型或基线耐药相关变异，使用达拉他韦、阿舒瑞韦和贝拉布韦治疗的HCV基因型1感染患者均显示出高响应率。^[3]

药理学

贝拉布韦充当NS5B（RNA聚合酶）抑制剂。^[4]

参考资料

^ 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.

[1]

[2]

[3]

[4]