Fenofibrate
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Fenofibrate
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| Systematic (IUPAC) name | |
| 1-methylethyl2-[4-(4-chlorobenzoyl) phenoxy]- 2-methyl-propanoate | |
| Identifiers | |
| CAS number | |
| ATC code | C10 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C20H21ClO4 |
| Mol. mass | 360.831 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 99% |
| Metabolism | ? |
| Half life | 20 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
C (US) |
| Legal status | |
| Routes | Oral |
Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease. Like other fibrates, it reduces both low-density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels, as well as increasing high-density liporotein (HDL) levels. It also appears to have a beneficial effect on the insulin resistance featured by the metabolic syndrome[citation needed]. It is used alone or in conjunction with statins in the treatment of hypercholesterolemia and hypertriglyceridemia. Fenofibrate is sold under the brand name TriCor® by Abbott Laboratories.
The pharmaceutical form and the strength may change from one country from another. In the United States, TriCor was reformulated in 2005 and is available in tablets of 48 and 145 mg. This reformulation is controversial and is the subject of anti-trust litigation by generic drug manufacturer Teva.[1] In Europe, it is available in coated tablet but also in capsule, the strength range include 67, 145, 160 and 200 mg. The differences in strength belong is due to altered bioavailability (the fraction absorbed by the body) due to particle size. For example: 200 mg can be replaced by 160 mg because its fenofibrate is micronised. The 145 mg strength is a new strength appeared in 2005-2006 which also replaces 200 or 160 mg as the fenofibrate is nanonised (ie the particle size is below 400 nm).
Like the other fibrates, fenofibrate acts on PPARα to reduce cholesterol levels.
A large study in 2005 of fenofibrate in patients with diabetes showed no change in total mortality or coronary artery events, but did show a significant change in overall cardiovascular events, as well as improving some microvascular complications of diabetes.[2]
Like most fibrates, fenofibrate can cause stomach upsets and myopathy (muscle pain) and very rarely rhabdomyolysis. This risk is increased when used together with statins. However, the Fenofibrate Intervention and Event Lowering in Diabetes (FIELD) study provides important information that long-term treatment with fenofibrate therapy appears to have a favorable safety profile in patients with type 2 diabetes, even when nonstudy lipid-lowering medications were added. In FIELD, there were no cases of rhabdomyolysis reported in patients on combination therapy with fenofibrate and a statin. Thus, there is an increasing body of evidence that fenofibrate/statin combination therapy is safe and effective at managing dyslipidemia in patients with type 2 diabetes who are at risk for cardiovascular events.
[edit] Reference
- ^ Abbott's request to dismiss antitrust charge over Tricor rejected. FDANews, Drug Daily Bulletin, (June 1, 2006) [1]
- ^ The FIELD study investigators. Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study): randomised controlled trial. Lancet 2005;366:1849-1861. PMID 16310551.
