Department of Biology, University of Rome Tor Vergata, Rome, Italy; Institute of Translational Pharmacology, CNR, Rome, Italy.
Venetian Institute of Molecular Medicine, University of Padova, Italy.
Biochem Biophys Res Commun. 2021 Jan 29;538:145-150. doi: 10.1016/j.bbrc.2020.11.043. Epub 2020 Nov 19.
Human coronaviruses (HCoV) were discovered in the 1960s and were originally thought to cause only mild upper respiratory tract diseases in immunocompetent hosts. This view changed since the beginning of this century, with the 2002 SARS (severe acute respiratory syndrome) epidemic and the 2012 MERS (Middle East respiratory syndrome) outbreak, two zoonotic infections that resulted in mortality rates of approximately 10% and 35%, respectively. Despite the importance of these pathogens, no approved antiviral drugs for the treatment of human coronavirus infections became available. However, remdesivir, a nucleotide analogue prodrug originally developed for the treatment of Ebola virus, was found to inhibit the replication of a wide range of human and animal coronaviruses in vitro and in preclinical studies. It is therefore not surprising that when the highly pathogenic SARS-CoV-2 coronavirus emerged in late 2019 in China, causing global health concern due to the virus strong human-to-human transmission ability, remdesivir was one of the first clinical candidates that received attention. After in vitro studies had shown its antiviral activity against SARS-CoV-2, and a first patient was successfully treated with the drug in the USA, a number of trials on remdesivir were initiated. Several had encouraging results, particularly the ACTT-1 double blind, randomized, and placebo controlled trial that has shown shortening of the time to recovery in hospitalized patients treated with remdesivir. The results of other trials were instead negative. Here, we provide an overview of remdesivir discovery, molecular mechanism of action, and initial and current clinical studies on its efficacy.
人类冠状病毒(HCoV)于 20 世纪 60 年代被发现,最初被认为只会导致免疫功能正常宿主的轻度上呼吸道疾病。自本世纪初以来,这种观点发生了变化,出现了 2002 年严重急性呼吸综合征(SARS)和 2012 年中东呼吸综合征(MERS)疫情,这两种人畜共患感染的死亡率分别约为 10%和 35%。尽管这些病原体很重要,但目前还没有批准用于治疗人类冠状病毒感染的抗病毒药物。然而,瑞德西韦是一种核苷酸类似物前药,最初是为治疗埃博拉病毒而开发的,在体外和临床前研究中发现它可以抑制广泛的人类和动物冠状病毒的复制。因此,当高致病性的 SARS-CoV-2 冠状病毒于 2019 年底在中国出现,由于该病毒具有很强的人际传播能力而引起全球健康关注时,瑞德西韦是首批受到关注的临床候选药物之一也就不足为奇了。在体外研究表明其对 SARS-CoV-2 具有抗病毒活性之后,并且在美国首例患者成功用该药物治疗后,启动了多项瑞德西韦临床试验。其中一些试验结果令人鼓舞,特别是 ACTT-1 双盲、随机、安慰剂对照试验表明,用瑞德西韦治疗的住院患者康复时间缩短了。其他试验的结果则相反。在这里,我们对瑞德西韦的发现、作用机制以及最初和当前关于其疗效的临床研究进行了综述。