Computational determination of toxicity risks associated with a selection of approved drugs having demonstrated activity against COVID-19

BMC Pharmacol Toxicol. 2021 Oct 21;22(1):61. doi: 10.1186/s40360-021-00519-5.

Abstract

Background: The emergence and rapid spread of SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) in thelate 2019 has caused a devastating global pandemic of the severe pneumonia-like disease coronavirus disease 2019 (COVID-19). Although vaccines have been and are being developed, they are not accessible to everyone and not everyone can receive these vaccines. Also, it typically takes more than 10 years until a new therapeutic agent is approved for usage. Therefore, repurposing of known drugs can lend itself well as a key approach for significantly expediting the development of new therapies for COVID-19.

Methods: We have incorporated machine learning-based computational tools and in silico models into the drug discovery process to predict Adsorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) profiles of 90 potential drugs for COVID-19 treatment identified from two independent studies mainly with the purpose of mitigating late-phase failures because of inferior pharmacokinetics and toxicity.

Results: Here, we summarize the cardiotoxicity and general toxicity profiles of 90 potential drugs for COVID-19 treatment and outline the risks of repurposing and propose a stratification of patients accordingly. We shortlist a total of five compounds based on their non-toxic properties.

Conclusion: In summary, this manuscript aims to provide a potentially useful source of essential knowledge on toxicity assessment of 90 compounds for healthcare practitioners and researchers to find off-label alternatives for the treatment for COVID-19. The majority of the molecules discussed in this manuscript have already moved into clinical trials and thus their known pharmacological and human safety profiles are expected to facilitate a fast track preclinical and clinical assessment for treating COVID-19.

Keywords: COVID-19; Repurposing drugs, hERG); Toxicity.

MeSH terms

  • Animals
  • Antiviral Agents / adverse effects
  • Antiviral Agents / toxicity*
  • COVID-19 Drug Treatment*
  • Captopril / therapeutic use
  • Cardiotoxins / toxicity
  • Catechols / therapeutic use
  • Computational Biology
  • Cytochrome P-450 Enzyme System / metabolism
  • Drug Discovery* / methods
  • Drug Repositioning*
  • Humans
  • Indomethacin / therapeutic use
  • Linezolid / therapeutic use
  • Liver / drug effects
  • Mice
  • Models, Biological
  • Nitriles / therapeutic use
  • Rats
  • Reproduction / drug effects
  • Software
  • Valproic Acid / therapeutic use

Substances

  • Antiviral Agents
  • Cardiotoxins
  • Catechols
  • Nitriles
  • entacapone
  • Valproic Acid
  • Cytochrome P-450 Enzyme System
  • Captopril
  • Linezolid
  • Indomethacin