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Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH).
Expert Opin Investig Drugs. 2020 Feb; 29(2):117-123.EO

Abstract

Introduction: Nonalcoholic fatty liver disease (NAFLD) encompasses a progressive disease phenotype starting from simple steatosis, which can progress to nonalcoholic steatohepatitis (NASH). It is component of the metabolic syndrome with a large impact on mortality in these patients. Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that regulate lipid and insulin metabolism, two key components in pathophysiology of NAFLD and NASH. Elafibranor acts as an agonist of PPAR-α and PPAR-δ and is currently under development for the treatment of NAFLD.Areas covered: This review summarizes the pharmacological aspects, the preclinical and clinical effectivity, and safety data of elafibranor for the treatment of nonalcoholic steatohepatitis and fibrosis.Expert opinion: Current data support an effect of elafibranor on the resolution on NASH and the improvement of two key drivers of NASH progression - insulin resistance and serum lipid normalization. The safety profile is favorable, though reversible serum creatinine elevations occur with use, potentially limiting its use in patients with concurrent renal disease. The modest effect sizes in different NAFLD disease stages of elafibranor and other drugs in development for NASH, will likely lead to pursuing of drug combinations personalized to each stage of the NAFLD disease spectrum.

Authors+Show Affiliations

Department of Gastroenterology and Hepatology, Radboud University Medical Center, Nijmegen, The Netherlands.Department of Gastroenterology and Hepatology, Radboud University Medical Center, Nijmegen, The Netherlands.Department of Gastroenterology and Hepatology, Radboud University Medical Center, Nijmegen, The Netherlands.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

31523999

Citation

Westerouen Van Meeteren, Menso J., et al. "Elafibranor: a Potential Drug for the Treatment of Nonalcoholic Steatohepatitis (NASH)." Expert Opinion On Investigational Drugs, vol. 29, no. 2, 2020, pp. 117-123.
Westerouen Van Meeteren MJ, Drenth JPH, Tjwa ETTL. Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH). Expert Opin Investig Drugs. 2020;29(2):117-123.
Westerouen Van Meeteren, M. J., Drenth, J. P. H., & Tjwa, E. T. T. L. (2020). Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH). Expert Opinion On Investigational Drugs, 29(2), 117-123. https://doi.org/10.1080/13543784.2020.1668375
Westerouen Van Meeteren MJ, Drenth JPH, Tjwa ETTL. Elafibranor: a Potential Drug for the Treatment of Nonalcoholic Steatohepatitis (NASH). Expert Opin Investig Drugs. 2020;29(2):117-123. PubMed PMID: 31523999.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH). AU - Westerouen Van Meeteren,Menso J, AU - Drenth,Joost P H, AU - Tjwa,Eric T T L, Y1 - 2019/09/25/ PY - 2019/9/17/pubmed PY - 2020/2/15/medline PY - 2019/9/17/entrez KW - Elafibranor KW - PPAR-α KW - PPAR-δ KW - nonalcoholic fatty liver disease KW - nonalcoholic steatohepatitis SP - 117 EP - 123 JF - Expert opinion on investigational drugs JO - Expert Opin Investig Drugs VL - 29 IS - 2 N2 - Introduction: Nonalcoholic fatty liver disease (NAFLD) encompasses a progressive disease phenotype starting from simple steatosis, which can progress to nonalcoholic steatohepatitis (NASH). It is component of the metabolic syndrome with a large impact on mortality in these patients. Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that regulate lipid and insulin metabolism, two key components in pathophysiology of NAFLD and NASH. Elafibranor acts as an agonist of PPAR-α and PPAR-δ and is currently under development for the treatment of NAFLD.Areas covered: This review summarizes the pharmacological aspects, the preclinical and clinical effectivity, and safety data of elafibranor for the treatment of nonalcoholic steatohepatitis and fibrosis.Expert opinion: Current data support an effect of elafibranor on the resolution on NASH and the improvement of two key drivers of NASH progression - insulin resistance and serum lipid normalization. The safety profile is favorable, though reversible serum creatinine elevations occur with use, potentially limiting its use in patients with concurrent renal disease. The modest effect sizes in different NAFLD disease stages of elafibranor and other drugs in development for NASH, will likely lead to pursuing of drug combinations personalized to each stage of the NAFLD disease spectrum. SN - 1744-7658 UR - https://www.unboundmedicine.com/medline/citation/31523999/Elafibranor:_a_potential_drug_for_the_treatment_of_nonalcoholic_steatohepatitis__NASH__ L2 - http://www.tandfonline.com/doi/full/10.1080/13543784.2020.1668375 DB - PRIME DP - Unbound Medicine ER -