Statin medicines are the most common medicines prescribed for high cholesterol. However, statins and healthy lifestyle habits are not always enough to lower cholesterol levels in some people. A newer group of cholesterol-lowering medicines, known as PCSK9 inhibitors, can help lower cholesterol in people who can’t reach their target cholesterol levels with statins and other cholesterol medicines or who can’t tolerate those medicines. Lerochol (lerodalcibep-liga) is a PCSK9 inhibitor used to lower cholesterol levels in adults.
How Does Lerochol Lower My Cholesterol Levels?
Cholesterol is a fatty substance that naturally occurs in human blood. There are two major forms of cholesterol: low-density lipoprotein (LDL), also known as “bad” cholesterol, and high-density lipoprotein (HDL), also called “good” cholesterol. LDL is the main source of artery-clogging plaque. Lerochol works in your liver and binds to PCSK9, an enzyme in your body. PCSK9 destroys receptors in the liver that help your body get rid of bad cholesterol (LDL) from the blood. By binding to the PCSK9 enzyme, Lerochol prevents the breakdown of the receptors in the liver. This helps remove bad cholesterol from your blood.
How Do I Use Lerochol?
Lerochol is a liquid injected under the skin (subcutaneously) once a month. Lerochol comes as a single dose in a prefilled syringe or autoinjector. Your health care provider should show you how to use the prefilled syringe or autoinjector before you inject Lerochol at home. Follow the instructions that come with your specific device to give the injection correctly. Some of the steps differ for the prefilled syringe versus the autoinjector.
You or a caregiver can inject Lerochol into the thighs or stomach area. A caregiver or health care professional may also inject the medicine into the back of your upper arm. Do not inject into areas of the skin that are tender, bruised, red, or hard, or that have moles or scars. Do not inject within 2 inches of your belly button.
The medicine is stored in the refrigerator, or it can be kept at room temperature for up to 3 months. To make the injection more comfortable, the drugmaker recommends letting the medicine sit at room temperature for 30 minutes before using it. Ask your pharmacist or other health care provider if you are unsure how to use Lerochol.
How Was Lerochol Studied for High Cholesterol?
Two clinical studies compared Lerochol to a placebo (containing no medicine) over a 52-week period in people with high cholesterol levels. In a third study, Lerochol was compared to a placebo over 24 weeks for high cholesterol levels in people with heterozygous familial hypercholesterolemia (HeFH). HeFH is a hereditary condition that causes very high cholesterol levels. People enrolled in the studies had to be on a stable diet and have high LDL cholesterol levels (“bad” cholesterol) despite already receiving other medicines to lower cholesterol levels, such as statins, ezetimibe, fenofibrate, or bile-acid sequestrants. In all of the studies, people received either 300 mg of Lerochol injection or a placebo injection once every four weeks. Neither the study participants nor the investigators knew who was receiving the medicine or a placebo.
There were a total of 1,844 adults in the two 52-week studies. People enrolled in the studies had to have either atherosclerotic cardiovascular disease (ASCVD) — plaque buildup in arteries leading to complications like heart attacks or strokes — or be at an increased risk for ASCVD. People had LDL levels of 70 mg/dL or higher and triglyceride levels of up to 400 mg/dL.
There were 478 adults with HeFH in the 24-week study that compared Lerochol to a placebo. People were enrolled in the study if they had a genetic diagnosis of HeFH, an LDL level of at least 70 mg/dL if they had ASCVD, or an LDL level of over 100 mg/dL without ASCVD and triglyceride levels of less than 400 mg/dL.
Characteristics of the study participants in all studies are described in the table below.
Participant Characteristics | Trial 1 (52 weeks) | Trial 2 (52 weeks) | Trial 3 (24 weeks) |
|---|---|---|---|
Average age | 64 years (49% ≥ 65 years) | 65 years (54% ≥ 65 years) | 53 years (19% ≥ 65 years) |
Sex | 30% female, 70% male | 45% female, 55% male | 52% female, 48% male |
Race/ethnicity | 80% White 17% Black or African American 3% Asian 1.1% Hispanic or Latino | 78% White 18% Black or African American 4% Asian 13% Hispanic or Latino | 87% White 8% Black or African American 5% Asian 1% Hispanic or Latino |
Diabetes | 34% | 43% | 45% |
Average LDL cholesterol | 102 mg/dL | 116 mg/dL | 150 mg/dL |
On statin therapy | 87% | 83% |
89% |
On high-intensity statin therapy | 53% | 39% |
67% |
What Benefits Were Seen With Lerochol?
In all three studies, people who used Lerochol saw significant drops in their “bad” LDL cholesterol compared to those using a placebo. The specific LDL reductions are provided in the table below. Note that your results may differ from what was seen in clinical studies.
Changes in LDL Levels
Trial 1 (52 weeks) | Trial 2 (52 weeks) | Trial 3 (24 weeks) | |
|---|---|---|---|
| Placebo | 0.1% decrease | 0.3% increase | 8% increase |
| Lerochol | 55% decrease | 49% decrease | 51% decrease |
| Difference from placebo | 55% decrease | 50% decrease | 59% decrease |
What Are Common Side Effects and How Can I Manage Them?
Some common side effects seen with Lerochol are injection site reactions, nasopharyngitis (common cold), diarrhea (frequent, loose, or watery stools), nausea, and peripheral edema (swelling in the arms, hands, legs, or feet).
The Lerochol injection can cause reactions in the part of the body where you get the shot. These reactions are usually mild and include rash, swelling, redness, itching, and warmth. If you have a reaction, apply a warm or cool compress to the area for 15 to 20 minutes. Your health care provider may suggest an over-the-counter (OTC) pain reliever such as ibuprofen or an OTC antihistamine like diphenhydramine for itching. To limit injection site reactions, make sure to inject the medicine into a different part of the body each time, which is called “rotating” the injection site.
If you develop severe diarrhea while using Lerochol, contact your health care provider. They will recommend ways to manage your diarrhea.
If you get nausea when using Lerochol, limit your diet to clear liquids in frequent, small amounts until you can tolerate solid foods. Keeping food portions small and avoiding sweet, fried, spicy, or greasy food is also helpful. If nausea persists and home remedies do not help, contact your health care provider.
Peripheral edema can be managed with lifestyle changes like lowering salt intake, keeping the affected limb raised, and wearing compression stockings or sleeves. If peripheral edema is persistent or bothersome, contact your health care provider.
How Long Does It Take Lerochol to Work?
In studies, improvements in LDL cholesterol levels were seen 4 weeks after starting the medicine. Even though improvements can be seen following one dose of the medicine, you should continue taking the medicine in order to keep your cholesterol levels down. Keep all your lab appointments so that you and your health care provider can track your cholesterol response and adjust your treatment plan if needed.
