Drug Theoretics and Cheminformatics Laboratory, Department of Pharmaceutical Technology, Jadavpur University, 188 Raja S C Mullick Road, Kolkata 700032, India.
Chemometrics and Molecular Modeling Laboratory, Department of Chemistry, Kean University, Union, NJ 07083, USA.
Aquat Toxicol. 2023 Mar;256:106416. doi: 10.1016/j.aquatox.2023.106416. Epub 2023 Feb 4.
To fight COVID-19 with uncountable medications and bioproducts throughout the world has taken us to another challenge of ecotoxicity. The indiscriminate usage followed by improper disposal of unused antibacterials, antivirals, antimalarials, immunomodulators, angiotensin II receptor blockers, corticosteroids, anthelmintics, anticoagulants etc. can lead us to an unimaginable ecotoxicity in the long run. A series of studies already identified active pharmaceutical ingredients (APIs) of the mentioned therapeutic classes and their metabolites in aquatic bodies as well as in wastewater treatment plants. Therefore, an initial ecotoxicity assessment of the majorly used pharmaceuticals is utmost requirement of the present time. The present in silico risk assessment study is focused on the aquatic toxicity prediction of 81 pharmaceuticals where 77 are most-used pharmaceuticals for COVID-19 throughout the world based on the literature along with one drug nirmatrelvir [PF-07321332] approved for emergency use by US-FDA and three other molecules under clinical trial. The ecotoxicity of the studied compounds were predicted based on the three aquatic species fish, algae and crustaceans employing the highest quality QSAR models available from the literature as well as using ECOSAR and QSAR Toolbox. To compare the toxicity thresholds, we have also used 4 control pharmaceuticals based on the worldwide occurrence from river, lake, STP, WWTPs, influent and effluent followed by high reported aquatic toxicity over the years as per the literature. Based on the statistical comparison, we have proposed top 3 pharmaceuticals used for the COVID-19 most toxic to the aquatic environment. The study will provide confident predictions of aquatic ecotoxicity data related to abundant use of COVID-19 drugs. The major aim of the study is to fill up the aquatic ecotoxicity data gap of major medications used for COVID-19.
为了与世界各地不计其数的药物和生物制品一起抗击 COVID-19,我们面临着另一个生态毒性挑战。由于抗菌药、抗病毒药、抗疟药、免疫调节剂、血管紧张素 II 受体阻滞剂、皮质类固醇、驱虫药、抗凝剂等药物的无差别使用和不当处置,从长远来看,我们可能会面临难以想象的生态毒性。一系列研究已经在水生生物和废水处理厂中发现了上述治疗类别中的活性药物成分 (API) 及其代谢物。因此,对主要使用的药物进行初步的生态毒性评估是当前的首要要求。本研究采用计算机模拟方法,对 81 种药物进行了水生毒性预测,其中 77 种是目前全球用于治疗 COVID-19 的最常用药物,依据的是文献中提到的药物以及美国食品药品监督管理局批准的用于紧急使用的药物 nirmatrelvir [PF-07321332] 和三种处于临床试验阶段的其他分子。研究采用来自文献的最高质量的定量构效关系模型,以及 ECOSAR 和 QSAR Toolbox,根据鱼类、藻类和甲壳类动物这三种水生生物对研究化合物的生态毒性进行预测。为了比较毒性阈值,我们还使用了根据全球河流、湖泊、STP、WWTP、进水和出水情况以及多年来文献报道的高报道水生毒性选择的 4 种对照药物。基于统计比较,我们提出了用于治疗 COVID-19 的三种毒性最大的药物。该研究将为与 COVID-19 药物大量使用相关的水生生态毒性数据提供可靠的预测。该研究的主要目的是填补 COVID-19 常用药物的水生生态毒性数据空白。