What to Know About PCSK9 Inhibitors for High Cholesterol
Key takeaways:
PCSK9 inhibitors can lower LDL cholesterol when lifestyle changes and other cholesterol-lowering medications (like statins) haven’t worked.
PCSK9 inhibitors are injectable medications given subcutaneously (under the skin) 1 or 2 times a month.
For people with known heart disease, PCSK9 inhibitors can lower the risk of certain heart-related complications, such as heart attacks and strokes.
Statin medications are generally the first-choice therapy for lowering LDL (“bad”) cholesterol. They work by stopping cholesterol production in the liver. But they also have side effects that can be a limiting factor for people taking them. And sometimes they may not do enough to lower your cholesterol.
What happens if you’re not able to tolerate statins or they’re not doing enough to help you reach your LDL target? Luckily, there are other types of medications available, one of which is PCSK9 inhibitors. Read on to learn more about this unique class of medications and if they could be a good treatment option for you.
What are PCSK9 inhibitors?
PCSK9 inhibitors are monoclonal antibodies. They’re also considered biologics. This means they’re made from living organisms and mimic specific antibodies in the human body to treat certain health conditions.
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Currently, there are only two PCSK9 inhibitors available in the U.S.: Repatha (evolocumab) and Praluent (alirocumab). They can be used alone or in combination with lifestyle changes and other cholesterol-lowering medications.
PCSK9 inhibitors can lower the risk of heart attack, stroke, and other heart-related problems for adults with known heart disease.
They can also lower LDL cholesterol in people who have heterozygous familial hypercholesterolemia (HeFH) and homozygous familial hypercholesterolemia (HoFH). These are inherited (passed down from your parents) conditions that prevent your body from getting rid of cholesterol efficiently.
Repatha can be used to lower LDL cholesterol in adults and children as young as 10 with HeFH or HoFH. Praluent is only approved for use in adults.
PCSK9 inhibitors are generally reserved for people who haven’t had success with — or are unable to tolerate — statins or other cholesterol-lowering medications. Healthcare providers may want to try more conservative treatments first. That’s because Repatha and Praluent are very expensive and require injections.
How do they work for high cholesterol?
The liver plays an important role in controlling how much cholesterol stays in your body. It has certain LDL receptors (chemical binding sites) that clear LDL cholesterol from your bloodstream. A protein called PCSK9 binds to these LDL receptors and lowers the number of receptors that can help get rid of LDL cholesterol. This causes more LDL cholesterol to remain in your blood.
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Repatha and Praluent work by preventing PCSK9 from attaching to the LDL receptors in the liver. This allows more LDL receptors to be available so they can remove excess cholesterol from the blood.
How are PCSK9 inhibitors given when treating high cholesterol?
Repatha and Praluent are injectable medications that are administered subcutaneously (under the skin) every 2 or 4 weeks. Injection sites include the abdomen, thigh, and upper arm. It’s recommended to change where you inject each time to prevent skin irritation in one particular area.
Both medications can be self-administered at home. But this is only after your healthcare provider has shown you how to correctly give yourself a shot.
Praluent is available in a single-dose prefilled pen. Repatha is available in a single-dose prefilled syringe, prefilled autoinjector, and Pushtronex system (a hands-free device that infuses Repatha into your body for about 5 minutes).
What are the potential side effects?
Side effects can vary slightly between PCSK9 inhibitors. They can also vary depending on the condition being treated.
Common side effects
Common side effects of Praluent include:
Common cold or flu
Injection site reactions (such as pain, swelling and redness)
Muscle pain
Diarrhea
Muscle spasms
Chest pain (not heart-related)
Common side effects of Repatha include:
Common cold or flu
Back pain
Injection site reactions
High blood sugar levels
Serious side effects
PCSK9 inhibitors can cause severe allergic reactions that may require hospitalization. It’s also important to note that the needle cover of Repatha’s prefilled syringe and autoinjector contains a latex derivative. This could cause an allergic reaction if you’re allergic to latex.
Call 911 or seek emergency medical care if you experience trouble breathing, swelling of your face, throat, or tongue, or severe rash or hives.
How effective are PCSK9 inhibitors when treating high cholesterol?
Studies have shown that PCSK9 inhibitors can lower LDL cholesterol by 45% to 70%. They can also lower your triglycerides (fat in your blood) and raise your HDL (“good”) cholesterol. By comparison, doses of certain statins can lower LDL by 50% or more.
Another advantage of PCSK9 inhibitors is that they can significantly lower the risk for certain heart-related complications, such as heart attacks and strokes.
How much do PCSK9 inhibitors cost?
PCSK9 inhibitors are expensive medications. Their list prices are a little under $6,000 per year. But how much you pay for them will depend on your insurance plan. And step therapy or a prior authorization may be required before the medication is covered.
If you have commercial insurance coverage, you may qualify for copay cards to help with the cost of your prescription. With these cards, you may be able to pay as little as $5 per month for Repatha or $25 per month for Praluent.
If you don’t have insurance, or if you have Medicare Part D, you may qualify for the MyPraluent Patient Assistance Program. In this case, you may be able to access Praluent at no charge. Amgen also offers a similar program where you may be able to access Repatha at no charge.
What are some alternatives to PCSK9 inhibitors?
Currently, there aren’t other medications available that work exactly the same way as PCSK9 inhibitors. But there are a few alternatives that your healthcare provider might consider to help you reach your LDL target.
Besides statins, other examples include:
Ezetimibe (Zetia)
Bile acid sequestrants, such as cholestyramine (Prevalite)
Fibrates, such as fenofibrate (Tricor)
Bempedoic acid (Nexletol)
In late 2021, the FDA also approved Leqvio (inclisiran). Leqvio is a first-in-class medication that can lower LDL cholesterol when diet and other medications haven’t worked. It’s an injectable small interfering RNA (siRNA) therapy. Leqvio works by interfering with the genes used to form PCSK9 proteins.
The bottom line
PCSK9 inhibitors can help lower LDL cholesterol when diet and other medications haven’t worked for you. They can also lower the risk for certain heart-related complications, such as heart attacks and strokes. If you’re struggling to reach your LDL goal, PCSK9 inhibitors may be a good option for you.
Keep in mind that this class of medications can be very expensive and may not be covered by your insurance plan. They also require self-injections. So, they may not be an ideal choice if you don’t like needles.
If you’re interested in trying a PCSK9 inhibitor, talk to your healthcare provider. Together, you can discuss if it would be an appropriate option for you.
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References
American Cancer Society. (2019). Monoclonal antibody side effects.
American Heart Association. (2020). Familial hypercholesterolemia (FH).
American Heart Association. (2020). Cholesterol medications.
American Heart Association. (2020). HDL (good), LDL (bad) cholesterol and triglycerides.
Amgen. (n.d.). Check eligibility requirements | Amgen Safety Net Foundation.
Amgen. (n.d.). Repatha (evolocumab) cost & copay information.
Amgen. (n.d.). Repatha (evolocumab) injection & dosing guide.
Amgen. (2021). Repatha [package insert].
Centers for Disease Control and Prevention. (2020). Conditions that increase risk for stroke.
Grundy, S. M., et al. (2018). 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol: a report of the american college of cardiology/american heart association task force on clinical practice guidelines. American Heart Association Journal.
Novartis. (2021). FDA approves Novartis Leqvio (inclisiran), first-in-class siRNA to lower cholesterol and keep it low with two doses a year.
Peterson, A. S., et al. (2008). PCSK9 function and physiology. Journal of Lipid Research.
Pokhrel, B., et al. (2021). PCSK9 inhibitors. StatPearls.
Regeneron. (N.d.). Starting and paying for Praluent.
Regeneron. (2021). Praluent [package insert].
Reuters. (2019). Sanofi and Regeneron cut list price of cholesterol drug by 60 percent.
