Elafibranor: a potential drug for the treatment of nonalcoholic steatohepatitis (NASH).

Expert Opin Investig Drugs

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

Published: February 2020

AI Article Synopsis

  • Nonalcoholic fatty liver disease (NAFLD) starts as simple fat accumulation in the liver and can progress to a more severe condition called nonalcoholic steatohepatitis (NASH), which is linked to metabolic syndrome and increased mortality risks.
  • Elafibranor, a drug being developed for treating NAFLD, targets peroxisome proliferator-activated receptors (PPARs) that play a crucial role in managing lipid and insulin metabolism, showing promise in improving conditions associated with NASH like insulin resistance and abnormal lipid levels.
  • Though elafibranor has a generally favorable safety profile, it may cause temporary increases in serum creatinine levels, which could be a concern for those with kidney

Article Abstract

: 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.: This review summarizes the pharmacological aspects, the preclinical and clinical effectivity, and safety data of elafibranor for the treatment of nonalcoholic steatohepatitis and fibrosis.: 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.

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Source
http://dx.doi.org/10.1080/13543784.2020.1668375DOI Listing

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