Revisiting PPAR agonists: novel perspectives in the treatment of primary biliary cholangitis

Expert Opin Pharmacother. 2024 Sep;25(13):1825-1834. doi: 10.1080/14656566.2024.2406268. Epub 2024 Oct 4.

Abstract

Introduction: In primary biliary cholangitis (PBC), approximately 40% of the patients respond incompletely to first-line treatment with ursodeoxycholic acid (UDCA), resulting in a poorer prognosis. Although obeticholic acid (OCA) is approved as a second-line therapy, it is not well-tolerated by patients with significant itching or advanced cirrhosis. Peroxisome proliferator-activated receptor (PPAR) agonists, including fibrates traditionally known as antihyperlipidemic agents, have emerged as potent alternatives for treating PBC patients with an incomplete response to UDCA.

Areas covered: This article provides a detailed overview of the mechanisms of PPAR agonists and evaluates their efficacy and adverse events, focusing on findings from recent phase III clinical trials.

Expert opinion: PPAR agonists are significant alternatives in the treatment of PBC, showing the potential to enhance biochemical responses, reduce mortality, and alleviate pruritus. Long-term outcomes for PBC patients, particularly those with advanced disease, and longitudinal data on the antipruritic effects of PPAR agonists require further investigation. Combining PPAR agonists with other treatments and advancing personalized approaches may enhance therapeutic efficacy and patient outcomes. This study provides future perspectives on the roles of PPAR agonists in PBC management.

Keywords: Primary biliary cholangitis; fibrates; long-term outcomes; peroxisome proliferator-activated receptor agonist; treatment.

Publication types

  • Review

MeSH terms

  • Animals
  • Chenodeoxycholic Acid / analogs & derivatives
  • Chenodeoxycholic Acid / pharmacology
  • Chenodeoxycholic Acid / therapeutic use
  • Cholagogues and Choleretics / therapeutic use
  • Fibric Acids / therapeutic use
  • Humans
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / therapeutic use
  • Liver Cirrhosis, Biliary* / drug therapy
  • Peroxisome Proliferator-Activated Receptors* / agonists
  • Prognosis
  • Pruritus / drug therapy
  • Ursodeoxycholic Acid / therapeutic use

Substances

  • Peroxisome Proliferator-Activated Receptors
  • obeticholic acid
  • Chenodeoxycholic Acid
  • Ursodeoxycholic Acid
  • Hypolipidemic Agents
  • Fibric Acids
  • Cholagogues and Choleretics