Statins are typically the first line of treatment used for treating high cholesterol. However, in recent years, injectable alternatives such as PCSK9 Inhibitors have been introduced to help reduce cholesterol levels.

High cholesterol can increase your risk of developing heart disease, which is the leading cause of death for both men and women in the United States. Since high cholesterol is such a widespread problem, new medications have been in the works to help control and manage the condition.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are among the newest line of drugs that have been developed to help reduce the prevalence of heart disease. These injectable medications work by increasing your liver’s ability to remove “bad” LDL cholesterol from your blood and decrease your risk of heart attack.

Keep reading to learn more about PCSK9 inhibitors and how they could potentially benefit you.

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The Food and Drug Administration (FDA) has approved the first cholesterol-lowering injection treatments in the new class of PCSK9 inhibitors.

There are currently 2 types available:

These drugs are antibodies that target a protein in the body called PCSK9. By inhibiting PCSK9’s ability to work, these antibodies are able to get rid of LDL cholesterol from the blood and decrease overall levels.

Benefits

Alirocumab and evolocumab can be beneficial for adults with heterozygous familial hypercholesterolemia (HeFH), an inherited condition that causes high levels of LDL cholesterol in the blood, and those with clinical cardiovascular disease.

When PCSK9 inhibitors are used in conjunction with a statin drug, they can help reduce LDL cholesterol by as much as 60%.

These antibodies are able to get rid of LDL cholesterol from the blood and decrease overall levels.

This class of drugs can be a reasonable option for someone who is not able to tolerate the side effects caused by statins or is not getting effective results from statin use.

Side effects

The most commonly reported side effects of evolocumab were:

  • upper respiratory tract infection
  • nasopharyngitis (inflammation of the nasal passages)
  • back pain
  • flu
  • and bruising, redness, or pain at the injection site

Allergic reactions, including hives and rash, were also observed.

Side effects from Praluent use were similar to Repatha, including:

  • pain and bruising at the injection site
  • flu-like symptoms
  • nasopharyngitis
  • allergic reactions, such as hypersensitivity vasculitis (a severe reaction to a darug)

Dosage

The recommended starting doses of PCSK9 inhibitors are as follows:

  • alirocumab, 75 milligrams (mg) should be injected once every 2 weeks, or 300 mg once every 4 weeks subcutaneously (under the skin)
  • evolocumab, 140 mg should be injected every 2 weeks or 420 mg once a month, delivered subcutaneously

Your dosage may be increased if a doctor feels your LDL levels aren’t responding adequately to the smaller dose.

Trials and research have shown positive results for both alirocumab and evolocumab. Recent studies have found that PCSK9 inhibitors may be able to significantly reduce cholesterol levels without any safety concerns for up to 24 weeks.

Other trials using alirocumab have also shown favorable results. In 2018, a landmark study called the Odyssey Outcomes Trial took place. It found that when alirocumab was used every other week, there was a significant reduction in ischemic events (where the heart does not get enough blood and oxygen). Ischemic events can lead to coronary heart and artery disease. PCSK9 inhibitors may be able to decrease this risk.

Cost

As is the case with most pharmaceutical advancements, these new injection drugs come with a hefty price tag. While the cost for consumers will depend on their insurance plan, wholesale costs start at $5000 per year.

In comparison, brand-name statin drugs, which are oral tablets, cost around $500 to $700 per year, and those figures drop considerably if purchasing the generic statin form.

Experiments are still ongoing as to the effectiveness of these injection drugs. Some health experts worry the new drugs pose a risk of neurocognitive dysfunction, particularly among older adults.

The effectiveness and safety of PCSK9 Inhibitors on the immune system are also still being investigated, and further extensive clinical studies are needed.

Until then experts urge caution since the trials conducted thus far have been short-term, making it uncertain whether PCSK9 inhibitors can actually reduce the risk of heart disease and extend lives.

For people with high cholesterol, statins are typically the first line of treatment suggested. However, in recent years, injectable alternatives such as PCSK9 Inhibitors are becoming widely available. The medication can help to significantly reduce LDL cholesterol levels.

There are currently 2 types available: alirocumab (Praluent) and evolocumab (Repatha).

However, further research is still needed to understand the long-term effectiveness and safety of these drugs.