貝尼磷布韋

貝尼磷布韋
臨床資料
其他名稱	AT-527、AT-511
法律規範狀態
法律規範	美：Investigational New Drug;
識別資訊
	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號	1998705-64-8（; 2241337-84-6 (hemisulfate)）
PubChem CID	122527455;
ChemSpider	112747221;
UNII	7UM3SQL968;
KEGG	D12255;
化學資訊
化學式	C24H33FN7O7P
摩爾質量	581.54 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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;

貝尼磷布韋（INN：bemnifosbuvir；開發代號：AT-527、RO7496998）是一種抗病毒藥物，由Atea製藥發明並授權羅氏進行臨床開發。它也是一種新型核苷酸類似物（英語：Nucleoside analogue）前藥，最初開發用於治療丙型肝炎。^[1]^[2]貝尼磷布韋可充當RNA聚合酶抑制劑，從而干擾病毒複製。因此，它已被研究用於治療冠狀病毒疾病，例如SARS-CoV-2引起的疾病。^[3]該藥物在早期臨床試驗中展現出良好的結果，但在後期卻出現了不一致的結果。^[4]^[5]貝尼磷布韋的III期研究因為未能達到緩解症狀的主要終點，也沒有降低病毒載量，所以提前結束了。然而，該藥物的耐受性良好，相對住院風險降低了71%。^[6]

參見

參考資料

^ 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. 溫哥華格式錯誤 (幫助)
^ 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. 溫哥華格式錯誤 (幫助)

[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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