Clofibrate (BioDeep_00000001936)

描述信息

Clofibrate is only found in individuals that have used or taken this drug. It is a fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia (from Martindale, The Extra Pharmacopoeia, 30th ed, p986). Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Clofibrate also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Also, as a fibrate, clofibrate is an agonist of the PPAR-α receptor[4] in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, increased lipoprotein lipase activity.
C78276 - Agent Affecting Digestive System or Metabolism > C29703 - Antilipidemic Agent > C98150 - Fibrate Antilipidemic Agent
C - Cardiovascular system > C10 - Lipid modifying agents > C10A - Lipid modifying agents, plain > C10AB - Fibrates
D057847 - Lipid Regulating Agents > D000960 - Hypolipidemic Agents > D000924 - Anticholesteremic Agents
D009676 - Noxae > D000963 - Antimetabolites
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ～500 μM for murine PPARα and PPARγ, and 55 μM, ～500 μM for human PPARα and PPARγ, respectively.

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