Research

Hormonal

PPARα agonists (fibrates) lower serum triglycerides and raise HDL cholesterol by directly binding to the PPARα receptor, thereby inducing genes involved in fatty acid oxidation and peroxisome proliferation.

Fibrates are a class of drugs that work by directly activating the PPARα receptor to lower triglycerides and raise HDL. They are most effective when prescribed for specific lipid profiles, though they require higher doses than newer agents and are less selective than PPARγ agonists.

GoodSupportsHIGH confidence
These data provided strong evidence that PPARα mediates the hypolipidemic effects of fibrates and other peroxisome proliferators... These data provide strong evidence that the fibrates and other hypolipidemic agents mediate their therapeutic effects by direct binding to PPARα.
Steven A. Kliewer · Recent Progress in Hormone Research · 2001

Why this rating

Strong in vitro and in vivo correlation between binding potency and clinical effect, though human physiological response differs from rodents.

Source

Peroxisome Proliferator-Activated Receptors: From Genes to Physiology

Steven A. Kliewer · Recent Progress in Hormone Research · 2001

DOI 10.1210/rp.56.1.239

narrative_reviewCited 426×
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DOI resolved against Crossref · corpus check 2026-06-10

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