Role of pirfenidone in TGF-β pathways and other inflammatory pathways in acute respiratory syndrome coronavirus 2 (SARS-Cov-2) infection: a theoretical perspective

Pharmacol Rep. 2021 Jun;73(3):712-727. doi: 10.1007/s43440-021-00255-x. Epub 2021 Apr 21.

Abstract

Background: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes pulmonary injury or multiple-organ injury by various pathological pathways. Transforming growth factor-beta (TGF-β) is a key factor that is released during SARS-CoV-2 infection. TGF-β, by internalization of the epithelial sodium channel (ENaC), suppresses the anti-oxidant system, downregulates the cystic fibrosis transmembrane conductance regulator (CFTR), and activates the plasminogen activator inhibitor 1 (PAI-1) and nuclear factor-kappa-light-chain-enhancer of activated B cells (NF-kB). These changes cause inflammation and lung injury along with coagulopathy. Moreover, reactive oxygen species play a significant role in lung injury, which levels up during SARS-CoV-2 infection.

Drug suggestion: Pirfenidone is an anti-fibrotic drug with an anti-oxidant activity that can prevent lung injury during SARS-CoV-2 infection by blocking the maturation process of transforming growth factor-beta (TGF-β) and enhancing the protective role of peroxisome proliferator-activated receptors (PPARs). Pirfenidone is a safe drug for patients with hypertension or diabetes and its side effect tolerated well.

Conclusion: The drug as a theoretical perspective may be an effective and safe choice for suppressing the inflammatory response during COVID-19. The recommendation would be a combination of pirfenidone and N-acetylcysteine to achieve maximum benefit during SARS-CoV-2 treatment.

Keywords: COVID-19 therapy; Pathology of COVID-19; Pirfenidone mechanism of action; SARS-CoV-2 mechanism; TGF-β signaling.

Publication types

  • Review

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • COVID-19 / metabolism*
  • COVID-19 / virology
  • COVID-19 Drug Treatment*
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / metabolism
  • Lung Injury / metabolism*
  • Lung Injury / virology
  • Pyridones / therapeutic use*
  • SARS-CoV-2 / pathogenicity
  • Signal Transduction / drug effects*
  • Transforming Growth Factor beta / metabolism*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Pyridones
  • Transforming Growth Factor beta
  • pirfenidone