FDA Approves New Pill That Reduces Bad Cholesterol by Nearly 60%
Viviana Cetola
Life News Today
A new option for the treatment of high cholesterol has just marked an important advance in cardiology. The United States Food and Drug Administration (FDA) approved Lipfendra (enlicitide), the first PCSK9 inhibitor that can be taken orally. In clinical studies, the medication achieved reductions in LDL cholesterol of nearly 60%.
Cholesterol is a waxy, fat-like substance found in all the cells of the body. The human body needs some cholesterol to function properly. But if there is too much cholesterol in the blood, it can build up on the walls of the arteries, narrowing or even blocking them. This puts a person at risk for coronary artery disease and other heart diseases.
There are different types of cholesterol. Low-density lipoprotein (LDL) cholesterol is often called "bad" cholesterol because it is the main source of cholesterol buildup and blockage in the arteries. High-density lipoprotein (HDL) cholesterol is known as "good" cholesterol because it helps remove cholesterol from the arteries. Triglycerides are another type of fat found in the blood that can also increase the risk of heart disease. A blood test known as a lipid panel can measure cholesterol and triglyceride levels. The test provides information about total cholesterol, LDL cholesterol, HDL cholesterol, non-HDL cholesterol and triglycerides. Although fasting for nine to 12 hours before a cholesterol test was traditionally recommended, many cholesterol tests can now be performed without fasting. In certain circumstances, a doctor may ask the patient to fast before the test.
There are different treatment options for reducing elevated LDL cholesterol levels, including statins such as rosuvastatin, atorvastatin and simvastatin. These medications primarily reduce the production of cholesterol in the liver. Lipfendra belongs to a different class known as PCSK9 inhibitors, medications that interact with a protein involved in the regulation of LDL cholesterol. Until now, medications in this class were administered by injection, making Lipfendra the first PCSK9 inhibitor available in oral form.
PCSK9 is a protein in the body that helps control the level of bad cholesterol (LDL) in the blood. Its main function is to bind to receptors in the liver that remove this cholesterol and promote their degradation. When the number of these receptors decreases, the liver has less ability to remove LDL cholesterol from the blood. PCSK9 inhibitors block this protein, allowing the liver to have more receptors available and remove a greater amount of LDL cholesterol. Drugs such as evolocumab and alirocumab work through this mechanism but are administered by subcutaneous injection.
Lipfendra is administered as a 20 mg tablet once a day. It must be taken in the morning on an empty stomach and only with water, black coffee or plain tea without any other ingredients. These instructions are important because food can considerably reduce the absorption of the medication. In studies, taking Lipfendra 30 minutes after eating caused the body to absorb approximately 48% to 50% less of the medication than when it was taken on an empty stomach. After taking the medication, the patient must wait at least 30 minutes before consuming food or other beverages. The FDA approved Lipfendra, together with diet and exercise, to reduce LDL cholesterol in adults with hypercholesterolemia, including people with heterozygous familial hypercholesterolemia, a genetic condition that causes elevated cholesterol levels from an early age.
The efficacy and safety of Lipfendra were evaluated in two randomized, double-blind, placebo-controlled clinical trials that included a total of 3,207 adults. After 24 weeks of treatment, the medication produced an average reduction in LDL cholesterol of approximately 56% compared with placebo among patients with atherosclerotic cardiovascular disease or at high cardiovascular risk. In another study involving people with heterozygous familial hypercholesterolemia, the average reduction compared with placebo was approximately 59% after 24 weeks. In one of the main studies, the overall frequency of adverse reactions was similar among those who received Lipfendra and those who received placebo. In the study involving patients with heterozygous familial hypercholesterolemia, diarrhea and dizziness were observed more frequently among patients treated with Lipfendra than among those who received placebo.
Statins continue to be widely used medications for reducing LDL cholesterol and protecting the heart. In addition to lowering LDL, they can reduce triglycerides and produce a modest increase in HDL cholesterol. They also help stabilize fatty plaques in the arteries and have been shown to reduce the risk of heart attack and stroke. Possible side effects include muscle pain or weakness, increases in liver enzymes and a small increase in blood glucose and the risk of developing type 2 diabetes, especially in people who already have risk factors.
Reducing LDL cholesterol is one of the main factors in lowering the risk of serious health complications, such as heart attacks and strokes, which are responsible for millions of deaths each year worldwide. Although Lipfendra has been shown to considerably reduce LDL levels, its approval is based on this effect on cholesterol and not on a long-term cardiovascular outcomes study that has specifically demonstrated that the medication reduces the risk of these complications. The cardiovascular benefits of lowering LDL have been established with other treatments, including statins and injectable PCSK9 inhibitors. For now, Lipfendra is authorized by the FDA in the United States. If it is later approved in other countries, this innovation could become a more practical alternative for many patients who need to keep their cholesterol under control on an ongoing basis.
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