Millions of Americans take daily medication to keep their cholesterol in check. For many, that means taking a statin, but some of the most effective cholesterol treatments require regular injections.

Several types of medications can lower low-density lipoprotein (LDL), or “bad,” cholesterol, including statins, Zetia (ezetimibe), and injectable PCSK9 inhibitors. Now, a new drug called Lipfendra (enlicitide)—the first oral form of PCSK9 inhibitor—offers another option. The medication can be taken on its own or alongside statins.

How Does Lipfendra Work?

Unlike statins, which reduce the body’s cholesterol production, Lipfendra blocks a protein called PCSK9. This allows the liver to remove more LDL cholesterol from the bloodstream.

Injectable PCSK9 inhibitors, including Repatha and Praluent, have been available for a decade. However, they remain underused, said Allen Taylor, MD, chairman of cardiology at MedStar Washington Hospital Center and MedStar Georgetown University Hospital in Washington, DC.

An oral version could make this type of treatment a more appealing option for some people.

“We always focus on lifestyle, eating right, and exercising for lowering cholesterol, but when it comes to treatment with medications, treating aggressively is the best thing we can do,” Taylor told Verywell. “And, for far too long, we’ve just had statins, and as good as they are, they’ve left levels too high for many people.” 

How Effective Is Lipfendra?

Lipfendra was evaluated in two clinical trials involving more than 3,000 adults who were already taking statins. Researchers looked at how well the drug lowered low-density lipoprotein (LDL), or “bad,” cholesterol compared with a placebo.

The first trial included adults with heart disease caused by plaque buildup in the arteries or those at high risk for it. Participants started with an average LDL cholesterol level of 96 mg/dL. After six months, people taking Lipfendra lowered their LDL cholesterol by an average of 56% more than those taking a placebo.

The second trial enrolled adults with heterozygous familial hypercholesterolemia (HeFH), an inherited condition that causes very high LDL cholesterol. Participants started with an average LDL cholesterol level of 119 mg/dL. People taking Lipfendra lowered their LDL cholesterol by an average of 59% compared to those taking a placebo.

Those reductions could help many patients reach recommended cholesterol goals. Current cholesterol guidelines recommend lowering LDL cholesterol to less than 70 mg/dL for many people at intermediate or high cardiovascular risk and to less than 55 mg/dL for people at very high risk.

The most common side effects reported in the trials included headache, nausea, diarrhea, and dizziness.

Michael D. Shapiro, DO, a professor of preventive cardiology at Wake Forest University, said Repatha and Praluent have been shown to not only reduce LDL cholesterol but also help prevent cardiovascular disease and deaths. It’s likely that Lipfendra achieves that as well, but the trials are not completed yet.

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Who Is Eligible for Lipfendra?

Under the FDA approval, Lipfendra is indicated for adults with high LDL cholesterol or HeFH. It’s most likely to be prescribed for patients whose LDL cholesterol remains high despite taking other medications such as statins, or those who can’t tolerate statins because of side effects like muscle pain.

Taylor said patients who are already taking a statin will likely remain on it even if they start Lipfendra because “statins can do things the PCSK9 drugs cannot.”

Statins not only lower cholesterol by reducing the amount the liver produces, but they also help stabilize plaque in the arteries and reduce inflammation. PCSK9 inhibitors work differently by helping the liver remove LDL cholesterol.

How Much Will Lipfendra Cost?

Lipfendra is expected to be less expensive than the injectable versions on the market. According to the drugmaker Merck, a 30-day supply will cost $315, though people whose insurance covers the drug will pay a much lower copay. By comparison, a 30-day supply of Praluent with an online coupon costs about $550, while Repatha costs about $240.

Merck will also make the drug available at a lower price on TrumpRx, the White House discount drug program for patients whose insurance does not cover certain drugs.