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Review
. 2022 Sep 20:9:751499.
doi: 10.3389/fcvm.2022.751499. eCollection 2022.

Pharmacological basis of the antifibrotic effects of pirfenidone: Mechanistic insights from cardiac in-vitro and in-vivo models

Laura Sartiani  1 , Gianluca Bartolucci  2 , Marco Pallecchi  2 , Valentina Spinelli  1 , Elisabetta Cerbai  1
Affiliations
Review

Pharmacological basis of the antifibrotic effects of pirfenidone: Mechanistic insights from cardiac in-vitro and in-vivo models

Laura Sartiani et al. Front Cardiovasc Med. .

Abstract

Pirfenidone is a small drug with marked antifibrotic activity approved for the treatment of Idiopathic pulmonary fibrosis. Recently, its peculiar pharmacological profile has attracted attention for its potential therapeutic benefit for extra-pulmonary disorders characterized by pathological fibrosis, such as kidney, liver, and cardiac failure. A major pitfall of pirfenidone is the lack of consistent understanding of its mechanism of action, regardless of the target. In addition to the increasing attention to the role of inflammation and its mediators in several processes, a better knowledge of the variety of fibroblasts' population, of signals controlling their activation and trans-differentiation, and of crosstalk with other cell resident and non-resident cell types is needed for prevention, treatment and possibly reverse of fibrosis. This review will focus on pirfenidone's pharmacological profile and its effects on cardiac fibroblasts.

Keywords: TGF-β; cardiac fibrosis; hypertrophy; myofibroblasts; pirfenidone.

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Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. The handling editor AA declared a past co-authorship/collaboration doi: 10.1016/j.jacc.2020.08.031 and doi: 10.1016/j.phrs.2020.104694 with the authors EC and GB.

Figures

Figure 1
Figure 1
Signals controlling fibroblast-to-myofibroblast transdifferentiation and favoring cardiac interstitial fibrosis.
Figure 2
Figure 2
Immunocytochemistry of primary culture of fibroblasts isolated from human biopsies of patients undergoing cardiosurgery for obstructive human hypertrophic cardiomyopathy; α-SMA is marked in red; DAPI is marked in blue.
See this image and copyright information in PMC

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References

    1. Agency EM,. Esbriet (pirfenidone) hard capsules: EU summary of product characteristics. (2021). Available online at: http://www.ema.europa.eu
    1. Shi S, Wu J, Chen H, Zeng F. Single- and multiple-dose pharmacokinetics of pirfenidone, an antifibrotic agent, in healthy Chinese volunteers. J Clin Pharmacol. (2007) 47:1268–76. 10.1177/0091270007304104 - DOI - PubMed
    1. Rubino CM, Bhavnani SM, Ambrose PG, Forrest A, Loutit JS. Effect of food and antacids on the pharmacokinetics of pirfenidone in older healthy adults. Pulm. Pharmacol. Ther. (2009) 22:279–85. 10.1016/j.pupt.2009.03.003 - DOI - PubMed
    1. FDA U,. Esbriet (pirfenidone) capsules US prescribing information. (2021). Available online at: https://www.accessdata.fda.gov/scripts/cder/daf/
    1. Macías-Barragán J, Sandoval-Rodríguez A, Navarro-Partida J, Armendáriz-Borunda J. The multifaceted role of pirfenidone and its novel targets. Fibrogenesis Tissue Repair. (2010) 3:1–11. 10.1186/1755-1536-3-16 - DOI - PMC - PubMed

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