Yan Victoria C, Muller Florian L
Department of Cancer Systems Imaging, University of Texas MD Anderson Cancer Center, Houston, Texas 77054, United States.
ACS Med Chem Lett. 2020 Jun 23;11(7):1361-1366. doi: 10.1021/acsmedchemlett.0c00316. eCollection 2020 Jul 9.
While remdesivir has garnered much hope for its moderate anti-Covid-19 effects, its parent nucleoside, GS-441524, has been overlooked. Pharmacokinetic analysis of remdesivir evidences premature serum hydrolysis to GS-441524; GS-441524 is the predominant metabolite reaching the lungs. With its synthetic simplicity and efficacy in the veterinary setting, we contend that GS-441524 is superior to remdesivir for Covid-19 treatment.
虽然瑞德西韦因其对新冠病毒的适度疗效而带来了诸多希望,但其母体核苷GS-441524却被忽视了。瑞德西韦的药代动力学分析表明,血清过早水解为GS-441524;GS-441524是到达肺部的主要代谢产物。鉴于其合成简单且在兽医领域有效,我们认为GS-441524在治疗新冠病毒方面优于瑞德西韦。