Apaydın Çağla Begüm, Çınar Gözde, Cihan-Üstündağ Gökçe
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, 34116, Turkey.
Curr Drug Targets. 2021;22(17):1986-2005. doi: 10.2174/1389450122666210215112150.
The coronavirus disease 2019 (COVID-19) pandemic, due to the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in December 2019 and has rapidly spread globally. As the confirmed number of cases has reached 83 million worldwide, the potential severity and the deadly complications of the disease requires urgent development of effective drugs for prevention and treatment. No proven effective treatment for this virus currently exists. Most of the antiviral discovery efforts are focused on the repurposing of approved or clinical stage drugs. This review highlights the small-molecule repurposed antiviral agents that are currently under investigation in clinical trials for COVID-19. These include viral polymerase and protease inhibitors remdesivir, galidesivir, favipiravir, ribavirin, sofosbuvir, tenofovir/emtricitabine, baloxavir marboxil, EIDD-2801, lopinavir/ritonavir; virus-/host-directed viral entry and fusion inhibitors arbidol chloroquine/hydroxychloroquine, chlorpromazine, camostat mesylate, nafamostat mesylate, bromhexine and agents with diverse/unclear mechanism of actions as oseltamivir, triazavirin, ivermectin, nitazoxanide, niclosamide and BLD-2660. The published preclinical and clinical data to date on these drugs as well as the mechanisms of action are reviewed.
2019年冠状病毒病（COVID-19）大流行由新型严重急性呼吸综合征冠状病毒2（SARS-CoV-2）引起，于2019年12月出现并迅速在全球传播。由于全球确诊病例数已达8300万，该疾病的潜在严重性和致命并发症需要紧急研发有效的预防和治疗药物。目前尚无经证实对该病毒有效的治疗方法。大多数抗病毒药物研发工作都集中在对已批准或处于临床阶段的药物进行重新利用。本综述重点介绍了目前正在进行COVID-19临床试验研究的小分子重新利用抗病毒药物。这些药物包括病毒聚合酶和蛋白酶抑制剂瑞德西韦、加利地韦、法匹拉韦、利巴韦林、索磷布韦、替诺福韦/恩曲他滨、巴洛沙韦酯、EIDD-2801、洛匹那韦/利托那韦；病毒/宿主导向的病毒进入和融合抑制剂阿比多尔、氯喹/羟氯喹、氯丙嗪、甲磺酸卡莫司他、甲磺酸萘莫司他、溴己新以及作用机制多样/不明的药物，如奥司他韦、三氮唑核苷、伊维菌素、硝唑尼特、氯硝柳胺和BLD-2660。本文综述了迄今为止这些药物已发表的临床前和临床数据以及作用机制。
