Pan Ppar Articles

Single, dual and pan-PPAR agonists are under development for the pharmacological treatment of NASH, 📰 read more from our articles.

Emerging drugs targeting specific points in NASH pathogenesis

Authors: Stojsavljevic-Shapeski S, Duvnjak M, Virovic-Jukic L,
et al.
Published in J Clin Transl Hepatol 2021
Extensive research and revelation in the field of pathogenesis of NASH has offered new possibilities of treatment and emerging new drugs that are being tested currently in numerous preclinical and clinical trials. These drugs target almost all steps in the pathogenesis of NASH...
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Pharmacotherapy in NAFLD/NASH

Authors: Attia SL, Softic S, Mouzaki M.
Published in Clin Transl Sci 2021
This review by SL Attia et al. (University of Kentucky College of Medicine, USA) summarises emerging pharmacotherapies for the treatment of adult and paediatric NAFLD. Investigated pharmacotherapies include lanifibranor (IVA337), an indole sulfonamide PPAR agonist that activates....
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PPARs as candidates for the treatment of NAFLD

Authors: Fougerat A, Montagner A, Loiseau N, et al
Published in Cells 202
The prevalence of NAFLD is dramatically increasing in developed countries, but no approved therapy is available. Most of the current pharmacological strategies target comorbidities, such as manifestations of metabolic syndrome. In addition, none of used medications improve fibrosis, which is the strongest indicator of mortality in NAFLD...
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Fibrosis in NASH: targeted therapies

Authors: Huisman TM, Dieterich DT, Friedman SL
Published in J Exp Pharmacol 2021
Progress in uncovering pathogenic determinants of fibrosis in NASH include metabolic dysregulation in hepatocytes that induce inflammation and cytokine secretion leading to cell injury and apoptosis, among others.This review by T. M. Huisman et al. (Division of Liver Diseases, Icahn School of Medicine at Mount Sinai...
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Management of NAFLD: a review

Authors: Petroni ML, Brodosi L, Bugianesi E, et al.
Published in BMJ 2021
As explained in the review by M. L. Petroni et al. (“Alma Mater” University, Bologna, Italy), several drugs are under investigation according to the agreed targets of reduced NASH activity without worsening of fibrosis or improving fibrosis without worsening of NASH. Anti-inflammatory, anti-fibrotic agents and metabolism modulators...
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Pan-PPAR agonist lanifibranor improves portal hypertension and hepatic fibrosis in experimental advanced chronic liver disease

Authors: Boyer-Diaz Z, Aristu-Zabalza P, Andrés-Rozas M, et al.
Published in J Hepatol 2020
Advanced chronic liver disease (ACLD) is a serious public health issue for which a safe and effective treatment is still lacking. It is often associated with portal hypertension and liver fibrosis. Over the recent years, peroxisome proliferator-activated receptors family (PPARs) have been considered as a relevant...
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PPARs and immune responses

Authors: Christofides A, Konstantinidou E, Jani C, et al.
Published in Metabolism 2020
Peroxisome proliferator-activated receptors (PPARs) are fatty acid-activated transcription factors of nuclear hormone receptor superfamily that regulate energy metabolism. Currently, three PPAR subtypes have been identified: PPARα, PPARγ, and PPARβ/δ. PPARα and PPARδ are highly expressed in oxidative tissues and regulate genes involved in substrate delivery...
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Peroxisome proliferator-activated receptors and their novel ligands as candidates for the treatment of non-alcoholic fatty liver disease

Authors: Fougerat A, Montagner A, Loiseau N, et al.
Published in Cells 2020
anifibranor is a moderately potent and well-balanced modulator of the three PPAR isotypes and has a good safety profile. Beneficial effects of lanifibranor on NASH histology, including reduced fibrosis, were confirmed recently in a preclinical model of NASH and fibrosis (choline-deficient amino acid-defined HFD mouse model)...
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Experimental steatohepatitis: lanifibranor early reduces NASH activity and macrophage infiltration.

Authors: Lefere S, Puengel T, Hundertmark J, et al.
Published in J Hepatol 2020
In a CDAA-HFD (choline-deficient, amino acid-defined high-fat diet-induced) model, which induces severe inflammation and liver fibrosis, S. Lefere et al. studied the efficacy of single and pan-PPAR agonists in the treatment of progressive steatohepatitis. To examine the pathophysiological sequence of steatohepatitis...
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Differential effects of selective- and pan-PPAR agonists on experimental steatohepatitis and hepatic macrophages.

Authors: Lefere S, Puengel T, Hundertmark J, et al.
Published in J Hepatol 2020
In an experimental study, S. Lefere et al. investigated the efficacy of single and pan-PPAR agonists in the treatment of progressive steatohepatitis. The authors employed the CDAA-HFD (choline-deficient, amino acid-defined high-fat diet-induced) model, which induces severe inflammation and liver fibrosis...
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Human hepatic in vitro models reveal distinct anti-NASH potencies of PPAR agonists.

Authors: Boeckmans J, Natale A, Rombaut M, et al.
Published in Cell Biol Toxicol 2020
In this study, J. Boeckmans et al. (Faculty of Medicine and Pharmacy, Vrije Universiteit, Brussels, Belgium) reproduced key NASH characteristics in vitro by exposing primary human hepatocytes, human skin stem cell-derived hepatic cells, HepaRG and HepG2 cell lines, as well as LX-2 hepatic stellate cells to multiple factors that play a role in the onset of NASH...
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