Tenofovir Disoproxil Fumarate: New Chemical Developments and Encouraging in vitro Biological Results for SARS-CoV-2

The recent emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has led society to live with a serious public health problem. In this sense, repositioning of antiretrovirals has captured the attention of the scientific community. Tenofovir disoproxil fumarate (TDF) is an antiretroviral compound that is used to treat acquired immune deficiency syndrome (AIDS) and hepatitis B. In this short report, we present a scale-up investigation of TDF by in situ infrared spectroscopy monitoring and a forced degradation study to describe a new degradation product. Finally, we have evaluated TDF in vitro for SARS-CoV-2 for the first time foreseeing the using of this medicine in pre-clinical and clinical investigations for the COVID-19 (coronavirus disease 2019) treatment.

严重急性呼吸综合征冠状病毒2（SARS-CoV-2）的暴发，使人类社会面临严峻的公共卫生挑战。在此背景下，抗逆转录病毒药物的重定位研究受到了科学界的广泛关注。富马酸替诺福韦二吡呋酯（TDF）是一种用于治疗获得性免疫缺陷综合征（艾滋病，AIDS）与乙型肝炎的抗逆转录病毒化合物。在本短篇报告中，我们通过原位红外光谱法（in situ infrared spectroscopy）监测对TDF开展了规模放大研究，并结合强制降解试验（forced degradation study）发现了一种全新的降解产物。最后，我们首次在体外评估了TDF对抗SARS-CoV-2的活性，为该药物用于2019冠状病毒病（COVID-19）治疗的临床前与临床研究提供了前瞻性参考。