Pharmacology · Class
Fibrates !
PPAR-alpha agonists that mainly lower triglycerides. Used for very high triglycerides, especially to reduce the risk of pancreatitis.
Updated 2026-11-01
What they are
Fibric acid derivatives (fenofibrate, gemfibrozil, bezafibrate, ciprofibrate) that act on the nuclear receptor PPARα. Their main use is severe hypertriglyceridemia.
Mechanism of action
Fibrates activate PPARα in the liver, muscle and other tissues. This increases fatty acid oxidation, raises lipoprotein lipase activity and lowers apolipoprotein C-III (an inhibitor of the lipase), so triglyceride-rich particles are cleared faster and the liver makes less VLDL. PPARα also raises apo A-I and A-II, which modestly increases HDL.
Target: PPARα (peroxisome proliferator-activated receptor alpha), a nuclear receptor
Drugs in this class
- FenofibrateA fibrate that lowers triglycerides by activating PPAR-alpha. The fibrate usually chosen when one is needed together…PPARα (nuclear receptor)
- GemfibrozilA fibrate that lowers triglycerides. Famous for interactions: it raises statin and repaglinide levels and must not be…PPARα (nuclear receptor)
Others in the class
- bezafibrate
- ciprofibrate
- pemafibrate (selective PPARα modulator)
Test yourself
Think of the answer, then tap the question to see it.
Through which receptor do fibrates lower triglycerides?
PPARα, a nuclear receptor that switches on fatty acid oxidation and lipoprotein lipase activity and lowers apo C-III.
Which fibrate must not be combined with simvastatin, and why?
Gemfibrozil: it blocks hepatic uptake (OATP1B1) and glucuronidation of statins, raising statin levels and the risk of rhabdomyolysis.
Which gallbladder adverse effect is shared by fibrates?
Gallstones: they increase cholesterol excretion into the bile.
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - FENOFIBRATE tablet (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 37 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.