盧夫特韋
![]() | |
法律規範狀態 | |
---|---|
法律規範 |
|
識別資訊 | |
| |
CAS號 | 2468015-78-1 |
PubChem CID | |
DrugBank | |
UNII | |
KEGG | |
ChEBI | |
CompTox Dashboard (EPA) | |
化學資訊 | |
化學式 | C24H33N4O9P |
摩爾質量 | 552.52 g·mol−1 |
3D模型(JSmol) | |
| |
|
盧夫特韋(英語:Lufotrelvir、PF-07304814)是輝瑞公司開發的一種抗病毒藥物,可作為3CL蛋白酶抑制劑。[1]它是一種前體藥物,其磷酸基團在體內被裂解以產生活性劑PF-00835231。[2]盧夫特韋正在用於治療COVID-19的人體臨床試驗中,並顯示出對COVID-19的良好活性,包括幾種變異株,但與相關藥物奈瑪特韋不同,它沒有口服活性,必須通過靜脈注射給藥,因此一直總體而言,臨床開發中不太受歡迎的候選者。[3][4][5]
參見
參考文獻
- ^ 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 (英語).
- ^ 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
.
- ^ 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.
|
|