What are PCSK9 inhibitors?

PCSK9 inhibitors are a type of cholesterol-lowering drug. They reduce your low-density lipoprotein (LDL) cholesterol or “bad” cholesterol. This medication may be especially helpful if you’ve had high cholesterol throughout your life.

What is PCSK9?

Your liver makes a protein called proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 regulates how many LDL receptors you have. Studies have shown that if you have naturally high PCSK9, you are more likely to have high cholesterol.

Who should take PCSK9 inhibitors?

Your provider may prescribe PCSK9 inhibitors if your cholesterol is still high after taking other medications. Lowering your cholesterol can decrease your risk of heart and blood vessel (cardiovascular) problems, including heart attack and stroke.

You may also take a PCSK9 inhibitor if you have a condition called familial hypercholesterolemia. This genetic condition causes high LDL cholesterol.

How do PCSK9 inhibitors work?

PCSK9 breaks down a kind of protein called LDL receptors. LDL receptors are on the outside of cells in your body, especially in your liver. These receptors attach to LDL cholesterol to carry it into your liver. The liver breaks down LDL cholesterol and gets rid of it.

PCSK9 inhibitors block PCSK9 proteins from breaking down your LDL receptors. The result is that more of your LDL receptors work. These active LDL receptors can then reduce your LDL cholesterol more efficiently.

How effective are PCSK9 inhibitors?

PCSK9 inhibitors can be highly effective for some people. Some research has found that these drugs can decrease your LDL cholesterol by up to 70%. They can cut the risk of a heart attack by almost one-third.

What are the types of PCSK9 inhibitors?

The Food and Drug Administration (FDA) has approved two types of PCSK9 inhibitors:

  • Alirocumab (Praluent®).
  • Evolocumab (Repatha®).

How do you take PCSK9 inhibitors?

You take PCSK9 inhibitors as an injection. You get the injection in a hospital or at your provider’s office every three months.

Every few months, you get a blood test so your provider can see how well the medication is working. Your provider may prescribe PCSK9 inhibitors alone or along with a statin, another type of cholesterol-lowering drug.

What are the benefits of PCSK9 inhibitors?

PCSK9 inhibitors can significantly decrease LDL cholesterol. One study found that the medicines lower LDL cholesterol by about 50%. Lowering your LDL cholesterol can reduce your risk of:

What are the side effects of PCSK9 inhibitors?

Many people take PCSK9 inhibitors without severe side effects. For people who have side effects from these medications, the most common ones include:

Less commonly, taking these drugs may increase your risk of:

  • Kidney problems.
  • Liver problems.

Who should not take PCSK9 inhibitors?

Most people who have high cholesterol don’t need to take PCSK9 inhibitors. Usually, providers try other medications before recommending these drugs. If you have severe kidney disease or liver disease, your provider may need to adjust your dose.

Is this medication a standalone treatment?

PCSK9 inhibitors and other cholesterol medications are usually part of an overall treatment plan. You may also improve your heart health by:

How long should you take PCSK9 inhibitors?

When taking PCSK9 inhibitors, you need regular follow-ups with a healthcare provider. If the medicines lower your cholesterol, your provider may prescribe PCSK9 inhibitors long-term. You should continue taking PCSK9 inhibitors for as long as your provider prescribes them.

A note from Cleveland Clinic

PCSK9 inhibitors are a type of medicine to lower cholesterol. They work by reducing your LDL cholesterol. Your provider might recommend a PCSK9 inhibitor if you have tried other treatments and your cholesterol is still high. You take PCSK9 inhibitors as an injection. When taking these medicines, be sure to follow up regularly with a healthcare provider.

Last reviewed by a Cleveland Clinic medical professional on 02/17/2022.

References

  • American Heart Association. Cholesterol Medications. (https://www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia/cholesterol-medications) Accessed 2/17/2022.
  • Gulpen AJW, Claessen RJM, Vanmolkot FHM. PCSK9-remmers [PCSK9 inhibitors; who benefits from these new cholesterol-lowering drugs? (https://pubmed.ncbi.nlm.nih.gov/32186821/) ]. Ned Tijdschr Geneeskd. 2020 Jan 16;164:D4325. Accessed 2/17/2022.
  • Heart UK. PCSK9 inhibitors. (https://www.heartuk.org.uk/getting-treatment/pcsk9-inhibitors) Accessed 2/17/2022.
  • Pokhrel B, Yuet WC, Levine SN. PCSK9 Inhibitors. (https://www.ncbi.nlm.nih.gov/books/NBK448100/) Treasure Island (FL): StatPearls Publishing; 2021 Jan-. Accessed 2/17/2022.

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