Clofibrate
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| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Protein binding | Variable, 92–97% at therapeutic concentrations |
| Metabolism | Hydrolyzed to clofibric acid; hepatic glucuronidation |
| Elimination half-life | Highly variable; average 18–22 hours. Prolonged in renal failure |
| Excretion | Renal, 95 to 99% |
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| ECHA InfoCard | 100.010.253 |
| Chemical and physical data | |
| Formula | C12H15ClO3 |
| Molar mass | 242.70 g·mol−1 |
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| Boiling point | 148 °C (298 °F) |
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Clofibrate (trade name Atromid-S) is a lipid-lowering agent used for controlling the high cholesterol and triacylglyceride level in the blood. It belongs to the class of fibrates. It increases lipoprotein lipase activity to promote the conversion of VLDL to LDL, and hence reduce the level of VLDL. It can increase the level of HDL as well.
It was patented in 1958 by Imperial Chemical Industries and approved for medical use in 1963.[1] Clofibrate was discontinued in 2002 due to adverse effects. In 2026, it was reported that clofibric acid is a ligand for E3 ligase synoviolin 1 (SYVN1) and was used to construct PROTACs for targeted protein degradation.[2]
Complications and controversies
[edit]It can induce SIADH, syndrome of inappropriate secretion of antidiuretic hormone ADH (vasopressin). Clofibrate can also result in formation of cholesterol stones in the gallbladder.
The World Health Organization Cooperative Trial on Primary Prevention of Ischaemic Heart Disease using clofibrate to lower serum cholesterol observed excess mortality in the clofibrate-treated group despite successful cholesterol lowering (47% more deaths during treatment with clofibrate and 5% after treatment with clofibrate) than the non-treated high cholesterol group. These deaths were due to a wide variety of causes other than heart disease, and remain "unexplained".[3]
References
[edit]- ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 474. ISBN 978-3-527-60749-5.
- ↑ Warren J, Munakala A, Zientek KD, Kim K, Wilmarth PA, Reddy AP, et al. (July 2026). "Identification of Clofibric Acid as a Synoviolin (SYVN1) Ligand for Proteolysis-Targeting Chimera (PROTAC) Development". ACS Medicinal Chemistry Letters. 17 (7): 1430–1439. doi:10.1021/acsmedchemlett.6c00223. PMC 13358943. PMID 42445038.
- ↑ "WHO cooperative trial on primary prevention of ischaemic heart disease with clofibrate to lower serum cholesterol: final mortality follow-up. Report of the Committee of Principal Investigators". Lancet. 2 (8403). London, England: 600–604. September 1984. doi:10.1016/s0140-6736(84)90595-6. PMID 6147641. S2CID 2473318.
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