New pill shows early promise in lowering bad cholesterol

The pill, developed by researchers at Monash University, is called Muvalaplin.
Sejal Sharma
Representational image
Representational image

Ake Ngiamsanguan/iStock 

A study recently published in the journal JAMA claims that researchers at Monash University have developed a pill that can lower bad cholesterol (known as 'lipoprotein a') levels within 24 hours of the first administration.

The effectiveness of the drug, called Muvalaplin, which is the first oral drug ever developed to target lipoprotein(a) or Lp(a), was demonstrated via a trial.

The development targets a significant cardiovascular risk factor, potentially revolutionizing high cholesterol management and aiding in the prevention of heart-related diseases commonly triggered by high bad cholesterol levels.

What is bad vs. good cholesterol?

Lipoproteins are composed of protein and fats and carry cholesterol to the cells via the bloodstream. The two main groups of lipoproteins are called HDL (high-density lipoprotein), also called the ‘good’ cholesterol, and LDL (low-density lipoprotein), which is ‘bad’ cholesterol.

If a person has high levels of LDL particles, cholesterol can build up in their arteries and form blockages called plaques. Lipoprotein(a) is a form of cholesterol that falls in the LDL category — the bad cholesterol. High levels of lipoprotein(a) might mean a high risk of heart disease or stroke.

Muvalaplin is a small molecule that inhibits the formation of Lp(a) by interfering with the binding of apo(a) to apo B100. 

“When it comes to treating high Lp(a), a known risk factor for cardiovascular disease, our clinicians currently have no effective tools in their kit,” said lead author Professor Stephen Nicholls, Director of the Monash Victorian Heart Institute and Victorian Heart Hospital, in a press release.

The drug effectively lowered the levels by up to 65 percent. It works by disrupting the ability of Lp(a) to form in the body.

“This drug is a game-changer in more ways than one. Not only do we have an option for lowering an elusive form of cholesterol, but being able to deliver it in an oral tablet means it will be more accessible for patients,” he added. “Lp(a) is essentially a silent killer with no available treatment, this drug changes that.”

A first-in-human study

The researchers conducted a phase 1 study involving 114 participants. Of these participants, 89 were treated with Muvalaplin, and 25 were treated with placebo. A total of 105 participants completed the study to test Lp(a) lowering and tolerability of Muvalaplin during administration for 14 days.

They found that daily administration of Muvalaplin produced a dose-dependent lowering of Lp(a) by up to 65 percent after two weeks.

In their study, the researchers highlighted several limitations. The first is that the safety of using muvalaplin will require larger and longer clinical trials in more diverse populations.

Second, the study only evaluated the effect of muvalaplin in participants with low and moderate-level Lp(a) but not in persons with greater elevations. Also, they noted that it remains uncertain whether Lp(a) lowering with muvalaplin will reduce cardiovascular risk.

The study was published in JAMA on August 28.

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