贝尼磷布韦
贝尼磷布韦(INN:bemnifosbuvir;开发代号:AT-527、RO7496998)是一种抗病毒药物,由Atea制药发明并授权罗氏进行临床开发。它也是一种新型核苷酸类似物前药,最初开发用于治疗丙型肝炎。[1][2]贝尼磷布韦可充当RNA聚合酶抑制剂,从而干扰病毒复制。因此,它已被研究用于治疗冠状病毒疾病,例如SARS-CoV-2引起的疾病。[3]该药物在早期临床试验中展现出良好的结果,但在后期却出现了不一致的结果。[4][5]贝尼磷布韦的III期研究因为未能达到缓解症状的主要终点,也没有降低病毒载量,所以提前结束了。然而,该药物的耐受性良好,相对住院风险降低了71%。[6]
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其他名稱 | AT-527、AT-511 |
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CAS号 | 1998705-64-8( 2241337-84-6 (hemisulfate)) ![]() |
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化学信息 | |
化学式 | C24H33FN7O7P |
摩尔质量 | 581.54 g·mol−1 |
3D模型(JSmol) | |
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参见
参考资料
- ^ Berliba E, Bogus M, Vanhoutte F, Berghmans PJ, Good SS, Moussa A, et al. Safety, pharmacokinetics and antiviral activity of AT-527, a novel purine nucleotide prodrug, in HCV-infected subjects with and without cirrhosis. Antimicrobial Agents and Chemotherapy. September 2019, 63 (12). PMC 6879261 . PMID 31570394. doi:10.1128/AAC.01201-19.
- ^ Good SS, Moussa A, Zhou XJ, Pietropaolo K, Sommadossi JP. Preclinical evaluation of AT-527, a novel guanosine nucleotide prodrug with potent, pan-genotypic activity against hepatitis C virus. PLOS ONE. 2020, 15 (1): e0227104. Bibcode:2020PLoSO..1527104G. PMC 6949113 . PMID 31914458. doi:10.1371/journal.pone.0227104 .
- ^ Good SS, Westover J, Jung KH, Zhou XJ, Moussa A, La Colla P, et al. AT-527, a Double Prodrug of a Guanosine Nucleotide Analog, Is a Potent Inhibitor of SARS-CoV-2 In Vitro and a Promising Oral Antiviral for Treatment of COVID-19. Antimicrobial Agents and Chemotherapy. March 2021, 65 (4). PMC 8097421 . PMID 33558299. doi:10.1128/AAC.02479-20.
- ^ Lowe D. AT-527 Fails a Phase II. In the Pipeline. Science.org. 19 October 2021. 温哥华格式错误 (帮助)
- ^ Fidler B, Gardner J. Atea, Roche change plans for oral COVID-19 drug after trial setback.. Biopharmadive.com. 19 October 2021.
- ^ Horga A, Saenz R, Yilmaz G, Simón-Campos A, Pietropaolo K, Stubbings WJ, Collinson N, Ishak L, Zrinscak B, Belanger B, Granier C, Lin K, C Hurt A, Zhou XJ, Wildum S, Hammond J. Oral bemnifosbuvir (AT-527) vs placebo in patients with mild-to-moderate COVID-19 in an outpatient setting (MORNINGSKY). Future Virology. November 2023, 18 (13). PMC 10621114 . PMID 37928891. doi:10.2217/fvl-2023-0115.