2023-08-29 13:38:29
In its first human trial, the experimental drug movalaplin reduced cholesterol transporters that block blood vessels at an impressive rate.
The study, funded by drug developer Eli Lilly, promises a major breakthrough in the search for ways to reduce a form of lipoprotein associated with cardiovascular disease. It is the leading cause of death worldwide.
Lipoproteins carry cholesterol around our bodies through the blood; Our cells need cholesterol to carry out many vital tasks, including building their cell walls, producing vitamin D, and making hormones. But lipoprotein(a), or Lp(a) for short, is the more sticky of these molecules and has a bad tendency to clog blood vessels if it’s crowded with too many of its friends.
Recent studies have linked this molecule to heart disease. It is also involved in poor circulation and strokes; Once Lp(a) has formed, it is difficult to reduce, with changes in diet and increased exercise having little effect. Attempts to lower lipoprotein through medication have also had little success. However, taking a new approach, drug developers are now targeting Lp(a)’s ability to form in the first place.
To further elucidate, Dr Stephen Nicholls, a cardiologist at Monash Health University and colleagues, said in their paper, “Movaplapine is the first oral drug specifically developed to lower levels of lipoprotein A by disrupting its formation.” This is according to what was reported by the scientific “Science Alert” website, according to the prestigious scientific magazine “JAMA”.
In a double-blind, randomized pharmaceutical trial, Nichols and his team tested movaplin with 114 volunteers, who included a mix of genders, ethnicities, and ages (18 to 69 years old). The initial safety-evaluation part of the study involved 55 healthy participants who took only a single dose of movaplapine, ranging from 1 mg to 800 mg, or a placebo. The second group of 59 healthy participants had higher than normal plasma Lp(a) levels; They were given a placebo (oral doses of 30 mg) or doses of up to 800 mg.
Within just 24 hours following the first dose, Lp(a) levels in the blood plasma decreased. The amount of reduction depends on the dose, reaching up to 65% in some patients over the course of the trial. Low Lp(a) levels also persisted for up to 50 days following administration of the final drug. But best of all, it didn’t alter levels of any other fats, and it was well tolerated by everyone who took it.
Determining whether the new substance is safe for human use is the main goal of phase 1 clinical trials like this one, so all potential side effects have been evaluated in meticulous detail.
In this context, 175 adverse events were reported during the trial, including headache, back pain, fatigue, nausea and diarrhea. None of these cases were more or less observed with the dose level, and they were all mild and resolved without any long-term consequences.
To that end, Nichols and his team conclude, “These preliminary phase I clinical results demonstrate that movaplapine effectively lowers Lp(a) without any serious adverse effects.” Since this trial is preliminary and small, there is not yet enough evidence to determine the drug’s overall effectiveness. Therefore, movalaplin is now in its Phase 2 clinical trial, which includes a much larger test group before long-term risks can be assessed over several years.
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