High cholesterol is a significant risk factor for cardiovascular disease, a leading cause of death. Statins, a class of medications commonly prescribed to lower cholesterol, have been the go-to treatment for many years. However, not everyone achieves their target cholesterol levels with statins alone, and some individuals may experience side effects or have contraindications that make them unable to use statins. This is where PCSK9 inhibitors, a newer class of cholesterol-lowering medications, come into the picture. In this blog post, we’ll explore what PCSK9 inhibitors are, how they work, their benefits, and considerations to keep in mind.
What are PCSK9 Inhibitors?
PCSK9 inhibitors are a type of medication that work by blocking the activity of an enzyme called PCSK9 (proprotein convertase subtilisin/kexin type 9). PCSK9 is responsible for breaking down LDL receptors in the liver, which normally help remove LDL cholesterol (often referred to as “bad” cholesterol) from the bloodstream. By inhibiting PCSK9, these medications increase the number of LDL receptors available in the liver, resulting in increased clearance of LDL cholesterol from the bloodstream and overall lower LDL cholesterol levels.
Currently, there are two FDA-approved PCSK9 inhibitors available on the market: evolocumab (Repatha) and alirocumab (Praluent). These medications are usually prescribed in addition to statins for individuals with familial hypercholesterolemia (a genetic condition causing very high LDL cholesterol levels) or those with clinical atherosclerotic cardiovascular disease (ASCVD) who require further LDL cholesterol reduction despite statin therapy.
How Do PCSK9 Inhibitors Work?
PCSK9 inhibitors are injectable medications that are typically self-administered as a subcutaneous injection (under the skin into the fatty tissue) every two to four weeks, depending on the specific medication and dosage prescribed. They work by specifically targeting PCSK9 and preventing it from breaking down LDL receptors in the liver. This increases the number of LDL receptors available in the liver, leading to increased removal of LDL cholesterol from the bloodstream and ultimately lowering LDL cholesterol levels.
Benefits of PCSK9 Inhibitors
The primary benefit of PCSK9 inhibitors is their ability to significantly lower LDL cholesterol levels, which can help reduce the risk of cardiovascular events such as heart attacks and strokes. Clinical trials have shown that PCSK9 inhibitors, when used in addition to statins or used alone in certain cases, can lower LDL cholesterol levels by 60%. Additionally, PCSK9 inhibitors have been shown to be effective in patients who are unable to tolerate statins or have contraindications to statin use.
Considerations for PCSK9 Inhibitor Use
Despite their benefits, there are some considerations to keep in mind when it comes to PCSK9 inhibitors. One significant consideration is the cost. PCSK9 inhibitors are expensive medications, and their high cost may pose challenges in terms of affordability and insurance coverage for some patients. However, some insurance plans do cover PCSK9 inhibitors, and there may be patient assistance programs available from the manufacturers to help with the cost.
Another consideration is that PCSK9 inhibitors are injectable medications, which may not be suitable for everyone. Some individuals may have concerns about self-administering injections or may have difficulties with the injection process due to various reasons. It’s important to discuss any concerns or challenges with your healthcare provider to determine the best approach for you.
In conclusion, PCSK9 inhibitors are a newer class of cholesterol-lowering medications that can be effective in lowering LDL cholesterol levels in addition to other standard of care therapies.
Resources:
- PRALUENT (alirocumab) [package insert]. Bridgewater, NJ: Sanofi-Aventis U.S. LLC; 2017.
- REPATHA (evolocumab) [package insert]. Thousand Oaks, CA: Amgen Inc.; 2017.
- https://my.clevelandclinic.org/health/drugs/22550-pcsk9-inhibitors#:~:text=PCSK9%20inhibitors%20block%20PCSK9%20proteins,your%20LDL%20cholesterol%20more%20efficiently.
- https://www.health.harvard.edu/blog/are-statins-enough-when-to-consider-pcsk9-inhibitors-2020060819986
