Cholesterol: Nexletol may help lower LDL levels without the need for statins

  • A major study finds that the drug Nexletol, often used as a supplement for low-density lipoprotein (LDL)-lowering statins, is effective—to a degree—in its own right.
  • While the effect of bempedoic acid—the main ingredient in Nexletol— is less strong than statins, the study validates the drug as a therapeutic option for people who are intolerant of statins.
  • Bempedoic acid is most likely to be prescribed in combination with ezetimibe, another supplemental LDL-lowering drug, that will strengthen its effect.

For people with high LDL cholesterol, statins are considered the first medication of choice. When statins alone do not adequately lower LDL levels, they may be supplemented with other drugs. It is also the case that some people do not tolerate, or are wary of, statins.

A large new study investigates the value of one of the supplementary LDL-lowering drugs, bempedoic acid, when used on its own without statins.

While bempedoic acid alone is not as effective as statins, it does significantly reduce the incidence of heart attacks and other events, offering patients a non-statin therapeutic alternative.

The double-blind, randomized, placebo-controlled trial was conducted in 32 countries at 1,250 sites. It involved 13,970 people who were unable or unwilling to take statins due to adverse effects, or who were at high risk of cardiovascular disease.

Participants were randomly assigned to one of two groups. The first received Nexletol, a pill form of bempedoic acid (N=6992), and the second a placebo (N=6978). The participants were followed for approximately 3.5 years.

Compared to those who received a placebo, participants who received bempedoic acid had a 13% lower risk of major cardiac events.

They were also 23% less likely to have heart attacks and 19% fewer surgical interventions for unclogging arteries. Bempedoic acid had no significant effects on the incidence of death from any cause, which is unexplained.

The efficacy of bempedoic acid was not compared in the study to that of statins, which are considered the most-effective LDL-lowering drugs.

The study is published in the New England Journal of Medicine, and the findings were presented Saturday at a meeting of the American College of Cardiology.

The study was also funded by Esperion Therapeutics, Inc.. the manufacturer of Nexletol.

Why LDL cholesterol is ‘bad’

One of the study’s authors, Dr. A. Michael Lincoff, a cardiovascular doctor from the Cleveland Clinic, explained to Medical News Today why LDL cholesterol levels are important in assessing health.

“LDL is the bad cholesterol — that’s the cholesterol that we really care about. LDL’ stands for ‘low-density liver’ cholesterol, fatty acids linked to proteins. It’s transported into the walls of arteries,” said Dr. Lincoff.

“It becomes oxidized and inflamed, and contributes to the formation of the plaques on the wall of the arteries that cause heart attacks and cause obstruction,” he added.

The plaques can weaken artery cell walls and rough their surface, making it easier for clots to form. It is one of the primary drivers of atherosclerosis.

While heredity can play a role in high LDL cholesterol levels, it can often be managed by adhering to a heart-healthy diet.

A solution for statin intolerance

Dr. Lincoff said the study “specifically assessed a group of patients that were felt to be statin-intolerant.”

“That means that they couldn’t, for a variety of perceived symptoms, they couldn’t or wouldn’t take statins at the dose is required to get their LDL cholesterol to the level that is the target LDL for their cardiovascular risk,” he elaborated.

The most common symptom of statin intolerance is muscle aching or weakness. Dr. Lincoff said some people also report gastrointestinal, neurologic, and cognitive issues when taking them.

“I’m being a little vague on what these [other symptoms] are because the entity of statin intolerance is very hard to define. In fact, the FDA says they don’t have a definition,” he added.

Pointing out that numerous studies have failed to confirm some reported adverse effects of statins compared to placebos, Dr. Lincoff suggested they may be attributable to the nocebo effect. He also wondered whether an aversion to statins may be a reaction to internet conjecture.

Hope for people who can’t take statins

“A trial like this gives us some hope that for the many people who are intolerant of statins that there are alternatives, which at the moment are not quite as good as statins but have benefits, potential benefits.”
— Dr. Jennifer Wong, cardiologist, who was not involved in the study, speaking to MNT.

For such people, Dr. Wong said the options were limited.

“[W]e are stuck using a non-statin-based medication even though that particular medication may not have shown any benefit on its own,” she said.

“What’s impressive is bempedoic acid showed some benefit on its own, not as impressive as statins, but showed some benefit on its own,” she added.

Dr. Wong said that since so much more confirming research has been done with statins, the first-line of treatment, based on “the current level of data that we have,” would be to try statins first.

A change of label

The purpose of this trial was to investigate and prove bempedoic acids’ value for reducing cardiovascular events.

“Most classes of [LDL-lowering] drugs that reduce LDL reduce heart disease, but you have to prove it. So, that’s why the FDA will give you a label — which they did for bempedoic acid for LDL reduction — but not for cardiovascular event reduction,” said Dr. Lincoff.

Bempedoic acid, plus

Bempedoic acid is currently available on its own as a monotherapy, and also in a form combined with another drug commonly prescribed alongside statins, ezetimibe.

The stand-alone efficacy of ezetimibe has been investigated in at least one large trial. It is less effective than bempedoic acid, reducing cardiovascular events by just 7%.

However, ezetimibe’s effect is additive, so when combined with bempedoic acid, the combined medication could lower overall cardiovascular risk by 26%.

According to Dr. Lincoff, ezetimibe is free to patients, so it does not add to bempedoic acid’s price.

“We expect in practice, [bempedoic acid and ezetimibe will] be a combination drug. There’s no reason not to. It’s not going to be more expensive,” he said.

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