Introduction

The experimental drug movalaplin, in its first human trial, reduced the number of cholesterol transporters that block blood vessels at an impressive rate.

Breakthrough in Lowering Lipoprotein Levels

The study, funded by drug developer Eli Lilly, promises a major breakthrough in finding ways to lower lipoprotein levels associated with cardiovascular disease, the leading cause of death worldwide.

The Importance of Cholesterol

Lipoproteins carry cholesterol around our body through the blood. Our cells need cholesterol to perform many vital tasks, including building cell walls, making vitamin D, and making hormones.

The Sticky Molecule: Lp(a)

But lipoprotein(a), or Lp(a) for short, is the most sticky of these molecules and has a bad tendency to clog blood vessels if it aggregates with too many of them. Recent studies have linked this molecule to heart disease. It is also involved in poor circulation and strokes.

The Difficulty in Lowering Lp(a)

Once Lp(a) is established, it is difficult to lower it, and changes in diet and increased exercise have little effect. Attempts to lower lipoprotein levels with drugs have not been very successful.

A New Approach

Using a new approach, drug developers now primarily focus on the ability of Lp(a) to form.

The First Oral Drug Specifically Designed for Lp(a) Levels

“Movaplin is the first oral drug specifically designed to lower lipoprotein(a) levels by interfering with its production,” Stephen Nicholls, MD, cardiologist at Monash Health, and colleagues explained in their article.

The Clinical Trial

In a randomized pharmaceutical trial, Nichols and his team tested Movaplin on 114 volunteers of different gender, race, and age (from 18 to 69 years old).

Promising Results

The initial part of the safety study included 55 healthy participants who received only one dose of movaplapine ranging from 1 to 800 mg or placebo.

A second group of 59 healthy participants with plasma Lp(a) levels above normal received placebo, oral doses of 30 mg, or doses up to 800 mg.

As early as 24 hours after the first dose, the level of Lp(a) in the blood plasma decreased. The degree of reduction depends on the dose and reaches up to 65% in some patients during the study.

The decrease in Lp(a) levels also persisted for 50 days after the last drug was taken. The best part is that it did not change other fat levels and was well tolerated by everyone who took it.

Safety Evaluation

Determining whether a new substance is safe for human use is the main goal of phase one clinical trials like this one, so all potential side effects have been carefully evaluated.

A total of 175 side effects were reported during the study, including headache, back pain, fatigue, nausea, and diarrhea. None of these cases were observed to any extent at this dose level, and all were mild and resolved without any long-term effects.

Further Research

Nichols and his team concluded, “These preliminary Phase I clinical data demonstrate that movaplapine is effective in lowering Lp(a) levels without any major side effects.”

Since this is a small preliminary study, there is not yet enough evidence to determine the overall effectiveness of the drug.

Movalaplin is currently in Phase 2 clinical trials, which includes a much larger group of researchers. This will test the efficacy of the drug with much greater statistical power before long-term risks can be assessed over several years.

Funding and Publication

This study was funded by pharmaceutical company Eli Lilly and published in JAMA.

Source

Source: Science Alert