Oral PCSK9-inhibitor is highly effective in decreasing the levels of LDL cholesterol, research shows

Two early clinical studies indicate that the first oral PCSK9 inhibitor cholesterol-lowering medicine was well tolerated and highly efficient in reducing high levels of LDL cholesterol, as per late-breaking research presented today at the American Heart Association’s Scientific Sessions 2021. The conference is entirely virtual, from Saturday 13th November through Monday, November 15, 2021 and is a major global exchange of the most recent discoveries in research, scientific advances and evidence-based clinical practice developments in cardiovascular science to improve health care worldwide.

PCSK9 inhibitors block the liver protein that helps destroy LDL cholesterol receptors. These receptors are responsible for helping remove cholesterol from the blood stream. More LDL is removed from the blood stream if there are more active receptors. Currently, PCSK9 inhibitors are only available via injection. This study is the first human study on the brand-new medication known as MK-0616. It is an oral version of the PCSK9 inhibitor.

Despite the difficulties of developing oral PCSK9 inhibitors in the past, our aim is to create an easy oral medication that will help patients reduce their bad cholesterol. We used novel technology and medicinal chemistry to identify the molecule MK-0616 that can be administered orally to block the PCSK9 protein, in turn helping to lower bad LDL cholesterol that can build up in arteries.”

Douglas Johns, Ph.D., FAHA, lead study author clinical director of translational medicine/clinical pharmacy, Merck Research Laboratories

MK-0616 lowered LDL cholesterol, but without creating death or serious adverse side effects when administered orally for up to 300 mgs a day in healthy men.

Johns said that “I believe this is the first report of oral absorption of a synthesized circular peptide, such as MK-0616” in humans. “We were happy that it was absorbed consistently and absorbed into the patients’ blood and also helped to lower cholesterol levels.”

The first study on MK-0616 included 60 healthy male volunteers aged between 18 and 50. Fifty-one participants in the study that were randomized received single doses of MK-0616 that ranged from 10 to 300 milligrams. Twenty-three participants received at least one dose of a placebo. The study was one of a “cross-over” design, so some participants received MK-0616 during one time, and then “crossed over” to placebo in a subsequent period. In each time 75 percent of participants received MK0616 and 25% received placebo. Researchers discovered that MK0616 significantly reduced PCSK9 levels that can cause high LDL cholesterol levels by more than 90% compared to baseline in all single-dose levels.

The second study of MK-0616 included 40 female and male volunteers aged between 18 and 65, who had already been taking statin medication to manage their cholesterol levels for at minimum three months. In this study, 75 percent (31) participants received a daily dose of 10 milligrams or 20 milligrams of MK-0616, whereas 25% (9) received a placebo – both groups receiving them in addition to their current statin therapy. After 14 days, participants were able to lower their blood cholesterol by 65% when they used MK-0616. Patients who received placebo showed less than 5% decrease in cholesterol levels compared to baseline.

“The initial results are encouraging; however, more clinical studies are required to confirm these findings, given limited clinical experience with the MK-0616 molecule,” said Johns.

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Gemma Wilson

Gemma is a journalism graduate with keen interest in covering business news – specifically startups. She has as a keen eye for technologies and has predicted quite a few successful startups over the last couple of years.

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