Definition
A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Description
A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic and gastrointestinal: rapid de-esterification occurs in the gastrointestinal tract and/or on first-pass metabolism to produce the active form, clofibric acid (chlorophenoxy isobutyric acid [CPIB]). Half Life: Half-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.
- Uses/Sources: For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.
- Route of Exposure: Completely but slowly absorbed from the intestine. Between 95% and 99% of an oral dose of clofibrate is excreted in the urine as free and conjugated clofibric acid; thus, the absorption of clofibrate is virtually complete.
Toxicity
- Carcinogenicity: 3, not classifiable as to its carcinogenicity to humans. (L135)
- Toxicity: Oral, mouse: LD<sub>50</sub> = 1220 mg/kg; Oral, rabbit: LD<sub>50</sub> = 1370 mg/kg; Oral, rat: LD<sub>50</sub> = 940 mg/kg.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Estrogen receptor Peroxisome proliferator-activated receptor alpha |
10753628 10922459 10951268 20671072 10454501 10787442 23611293 20637823 |