Mechanism of action of fibrates

  • derivatives of fibric acid (isobutyric acid)
  • activate Peroxisome Proliferator Activated Receptor alpha (PPAR) – a gene transcription regulating receptor present in liver, fat and muscles

Activation of PPAR alpha results in:

  • increased synthesis of lipoprotein lipase – hydrolyse triglycerides – decrease circulating TG’s
  • increased expression of LDL receptor in liver – mainly with II generation fibrates
  • increased fatty acid oxidation
  • decrease TG synthesis in liver
  •  reduce circulating free fatty acids

Outcome:

  • decrease TG 20-50%
  • decrease LDL 10-15%
  • increase HDL 10-15%