Фенофибрат: Холестерин деңгейін төмендетуге арналған дәрі

Drug of the fibrate class, mainly used to reduce cholesterol levels

Fenofibrate (sold under the brand names Tricor, Fenobrat etc. ), is an oral medication of the fibrate class used to treat abnormal blood lipid levels. Its use is recommended together with dietary changes. It works by multiple mechanisms. It was patented in 1969, and came into medical use in 1975. It is available as a generic medication.

Fenofibrate is mainly used for primary hypercholesterolemia or mixed dyslipidemia. Fenofibrate may slow the progression of diabetic retinopathy and the need for invasive treatment such as laser therapy in patients with type 2 diabetes with pre existing retinopathy. It was initially indicated for diabetic retinopathy in patients with type 2 diabetes and diabetic retinopathy in Australia. The large scale, international FIELD and ACCORD Eye trials found that fenofibrate therapy reduced required laser treatment for diabetic retinopathy by 1.5% over 5 years, as well as reducing progression by 3.7% over 4 years. Further studies looking at the role of fenofibrate in the progression of diabetic retinopathy as the primary outcome is warranted to understand its role in this condition. Although no statistically significant cardiovascular risk benefits were identified in these trials, benefits may accrue to add on therapy to patients with high triglyceride dyslipidaemia currently taking statin medications. Fenofibrate appears to reduce the risk of below ankle amputations in patients with Type 2 diabetes without microvascular disease. The FIELD study reported that fenofibrate at doses of 200 mg daily, reduced the risk for any amputation by 37% independent of glycaemic control, presence or absence of dyslipidaemia and its lipid lowering mechanism of action. However, the cohort of participants who underwent amputations were more likely to have had previous cardiovascular disease (e. g. angina, myocardial infarction), longer duration of diabetes and had baseline neuropathy. It is used in addition to diet to reduce elevated low density lipoprotein cholesterol (LDL), total cholesterol, triglycerides (TG), and apolipoprotein B (apo B), and to increase high density lipoprotein cholesterol (HDL) in adults with primary hypercholesterolemia or mixed dyslipidemia.

It is used in tandem with diet for treatment of adults with severe hypertriglyceridemia. Improving glycemic control in diabetics showing fasting chylomicronemia usually reduces the need for pharmacologic intervention. Additionally, in 2016, the FDA filed "Withdrawal of Approval of Indications Related to the Coadministration With Statins in Applications for Niacin Extended Release Tablets and Fenofibric Acid Delayed Release Capsules" noting "the Agency has concluded that the totality of the scientific evidence no longer supports the conclusion that a drug induced reduction in triglyceride levels and/or increase in HDL cholesterol levels in statin treated patients results in a reduction in the risk of cardiovascular events. Consistent with this conclusion, FDA has determined that the benefits of niacin ER tablets and fenofibric acid DR capsules for coadministration with statins no longer outweigh the risks, and the approvals for this indication should be withdrawn."

"In summary, enhanced catabolism of triglyceride rich particles and reduced secretion of VLDL underlie the hypotriglyceridemic effect of fibrates, whereas their effect on HDL metabolism is associated with changes in HDL apolipoprotein expression." PPARα also increases apoproteins AI and AII, reduces VLDL and LDL containing apoprotein B, and increases HDL containing apoprotein AI and AII.

Fenofibric acid was one of the 12 compounds identified in sludge samples taken from 12 wastewater treatment plants in California that were associated with estrogenic activity in in vitro.

Fenofibrate was first synthesized in 1974, as a derivative of clofibrate, and was initially offered in France. It was initially known as procetofen, and was later renamed fenofibrate' to comply with World Health Organization International Nonproprietary Name guidelines. Fenofibrate was developed by Groupe Fournier SA of France.

In the United States, Tricor was reformulated in 2005. This reformulation was controversial, seen as an attempt to stifle competition from generic equivalents, and was the subject of antitrust litigation by Teva.