The search for clinically effective antivirals against the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is ongoing. Repurposing of drugs licensed for non–coronavirus disease 2019 (COVID-19) indications has been extensively investigated in laboratory models and in clinical studies with mixed results. Nafamostat mesylate (nafamostat) is a drug licensed in Japan and Korea for indications including acute pancreatitis and disseminated intravascular coagulation. It is available only for continuous intravenous infusion. In vitro human lung cell line studies with nafamostat demonstrate high antiviral potency against SARS-CoV-2 (half maximal inhibitory concentration [IC50] of 0.0022 µM [compared to remdesivir 1.3 µM]), ostensibly via inhibition of the cellular enzyme transmembrane protease serine 2 (TMPRSS2) preventing viral entry into human cells. In addition, the established antithrombotic activity is hypothesised to be advantageous given thrombosis-associated sequelae of COVID-19. Clinical reports to date are limited, but indicate a potential benefit of nafamostat in patients with moderate to severe COVID-19. In this review, we will explore the pre-clinical, pharmacokinetic and clinical outcome data presently available for nafamostat as a treatment for COVID-19. The recruitment to ongoing clinical trials is a priority to provide more robust data on the safety and efficacy of nafamostat as a treatment for COVID-19.

针对严重急性呼吸综合征冠状病毒-2 (SARS-CoV-2) 的临床有效抗病毒药物的研究正在进行中。已在实验室模型和临床研究中对已获许可用于非 2019 年冠状病毒病 (COVID-19) 适应症的药物的重新利用进行了广泛的研究，结果好坏参半。甲磺酸萘莫司他（nafamostat）是一种在日本和韩国获得许可的药物，用于治疗急性胰腺炎和弥散性血管内凝血等适应症。只能用于连续静脉输注。体外人肺细胞系研究表明，nafamostat 对 SARS-CoV-2 具有高抗病毒效力（半数最大抑制浓度 [IC50] 为 0.0022 µM [与瑞德西韦 1.3 µM 相比]），表面上是通过抑制细胞酶跨膜蛋白酶丝氨酸 2 （TMPRSS2）阻止病毒进入人体细胞。此外，鉴于 COVID-19 的血栓相关后遗症，假设已确定的抗血栓活性是有利的。迄今为止的临床报告有限，但表明 nafamostat 对中度至重度 COVID-19 患者具有潜在益处。在本次综述中，我们将探讨目前可用的 nafamostat 用于治疗 COVID-19 的临床前、药代动力学和临床结果数据。招募正在进行的临床试验是一个优先事项，以便提供关于 nafamostat 作为 COVID-19 治疗的安全性和有效性的更可靠的数据。