卢夫特韦
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识别信息 | |
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CAS号 | 2468015-78-1 |
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CompTox Dashboard (EPA) | |
化学信息 | |
化学式 | C24H33N4O9P |
摩尔质量 | 552.52 g·mol−1 |
3D模型(JSmol) | |
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卢夫特韦(英语:Lufotrelvir、PF-07304814)是辉瑞公司开发的一种抗病毒药物,可作为3CL蛋白酶抑制剂。[1]它是一种前体药物,其磷酸基团在体内被裂解以产生活性剂PF-00835231。[2]卢夫特韦正在用于治疗COVID-19的人体临床试验中,并显示出对COVID-19的良好活性,包括几种变异株,但与相关药物奈玛特韦不同,它没有口服活性,必须通过静脉注射给药,因此一直总体而言,临床开发中不太受欢迎的候选者。[3][4][5]
参见
参考文献
- ^ Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, et al. Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. Journal of Medicinal Chemistry. November 2020, 63 (21): 12725–12747. PMC 7571312
. PMID 33054210. doi:10.1021/acs.jmedchem.0c01063.
- ^ Boras, Britton; Jones, Rhys M.; Anson, Brandon J.; Arenson, Dan; Aschenbrenner, Lisa; Bakowski, Malina A.; Beutler, Nathan; Binder, Joseph; Chen, Emily; Eng, Heather; Hammond, Holly. Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19. Nature Communications. 2021-10-18, 12 (1): 6055. Bibcode:2021NatCo..12.6055B. ISSN 2041-1723. PMC 8523698
. PMID 34663813. doi:10.1038/s41467-021-26239-2 (英语).
- ^ de Vries M, Mohamed AS, Prescott RA, Valero-Jimenez AM, Desvignes L, O'Connor R, et al. A comparative analysis of SARS-CoV-2 antivirals characterizes 3CLpro inhibitor PF-00835231 as a potential new treatment for COVID-19. Journal of Virology. February 2021, 95 (10). PMC 8139662
. PMID 33622961. doi:10.1128/JVI.01819-20.
- ^ Baig MH, Sharma T, Ahmad I, Abohashrh M, Alam MM, Dong JJ. Is PF-00835231 a Pan-SARS-CoV-2 Mpro Inhibitor? A Comparative Study. Molecules. March 2021, 26 (6): 1678. PMC 8002701
. PMID 33802860. doi:10.3390/molecules26061678
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- ^ Vandyck K, Deval J. Considerations for the discovery and development of 3-chymotrypsin-like cysteine protease inhibitors targeting SARS-CoV-2 infection. Current Opinion in Virology. August 2021, 49: 36–40. PMC 8075814
. PMID 34029993. doi:10.1016/j.coviro.2021.04.006.
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