Gemfibrozil is a lipid regulator that is used in the reduction of serum triglyceride levels in high-risk patients with hyperlipidemia. Gemfibrozil is a fibric acid agent, similar to clofibrate, used to treat Type IIb, IV, and V hyperlipidemias.
- Mechanism
- Curator reviewed · 14 references
Gemfibrozil activates peroxisome proliferator-activated receptor-α (PPARα), which alters lipid metabolism. This activation leads to increased HDL, apo AI, apo AII, lipoprotein lipase (LPL), inhibition of apo B synthesis, peripheral lipolysis, decreased removal of free fatty acids by the liver, and increased clearance of apoB.
Upregulated LPL reduces plasma triglyceride levels. Decreased hepatic removal of fatty acids decreases the production of triglycerides. The effects on apoB synthesis and clearance decrease VLDL production which also reduce plasma triglyceride levels.
Gemfibrozil's glucuronide metabolite is also an inhibitor of CYP2C8.
- Primary indication
- Gemfibrozil is indicated to treat patients with Types IV and V hyperlipidemia who have elevated serum triglycerides (usually above 2000mg/dL), elevated VLDL cholesterol, fasting chylomicrons, are at risk of developing pancreatitis, and do not adequately...Curator reviewed · 3 structured indications
- Formula / weight
- C15H22O3 · 250.3334 g/mol (avg)
- First approval
- Canada, 1996 · United States, 1993
- Code names
- CI-719
- Brand names
Resolves to
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Which drugs share a target with Gemfibrozil, and which of those have an active Phase 3 trial?
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