贝尼磷布韦

贝尼磷布韦
临床资料
其他名称	AT-527、AT-511
法律规范状态
法律规范	美：Investigational New Drug;
识别信息
	IUPAC命名法 Propan-2-yl (2S)-2-[[[(2R,3R,4R,5R)-5-[2-amino-6-(methylamino)purin-9-yl]-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate; ;
CAS号	1998705-64-8（; 2241337-84-6 (hemisulfate)）
PubChem CID	122527455;
ChemSpider	112747221;
UNII	7UM3SQL968;
KEGG	D12255;
化学信息
化学式	C24H33FN7O7P
摩尔质量	581.54 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES C[C@@H](C(=O)OC(C)C)NP(=O)(OC[C@@H]1[C@H]([C@@]([C@@H](O1)N2C=NC3=C(N=C(N=C32)N)NC)(C)F)O)OC4=CC=CC=C4;
	InChI InChI=1S/C24H33FN7O7P/c1-13(2)37-21(34)14(3)31-40(35,39-15-9-7-6-8-10-15)36-11-16-18(33)24(4,25)22(38-16)32-12-28-17-19(27-5)29-23(26)30-20(17)32/h6-10,12-14,16,18,22,33H,11H2,1-5H3,(H,31,35)(H3,26,27,29,30)/t14-,16+,18+,22+,24+,40?/m0/s1; Key:OISLSHLAXHALQZ-HEOQURLSSA-N;

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（英语：Nucleoside analogue）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]

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.

[2] 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.

[3] 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  .

[4] 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.

[5] 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)

[6] Fidler B, Gardner J. Atea, Roche change plans for oral COVID-19 drug after trial setback.. Biopharmadive.com. 19 October 2021.

[pmid37928891-7] 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.

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