CPHI China 2023- Oral drug PCSK9 inhibitor reduces cholesterol

MK-0616, one of the first oral PCSK9 inhibitors to be tested in clinical trials, was published in the Journal of the American College of Cardiology (JACC), where patients showed significant improvement in symptoms after receiving the drug in Phase II testing. PCSK9 inhibitors reduce the risk of heart disease by lowering LDL cholesterol levels. MK-0616 was developed by Merck, and PCSK9 inhibitors currently on the market are administered by subcutaneous injection and taken together with statins.

PCSK9 inhibitors in pill form can reduce costs, and once the safety and efficacy of the drug are established, more patients can receive the corresponding treatment.

Dr. Christie M. Ballantyne, director of the Center for Metabolic Disease Prevention at Baylor College of Medicine in Houston, said that MK-0616, coupled with the aid of other drugs, can be a good treatment for many types of heart disease patients, and MK-0616 opens up a new way of thinking about treatment options.

Phase II study of oral PCSK9 inhibitors

The researchers recruited 381 adults with a history of heart disease or high LDL cholesterol levels who were at risk for heart disease.

During the trial, participants continued to take a placebo or MK-0616 for eight weeks, and at the eighth week, those taking MK-0616 had significantly lower LDL cholesterol markers compared to those taking a placebo.

Among them, the dose of 60mg, the indicator dropped by more than 30%, and the test dose of 55mg, the indicator also dropped by more than 12%.

In addition, patients also had significant reductions in non-high-density lipoprotein (non-HDL) cholesterol and apolipoprotein B (ApoB).

The researchers said that the current experiment time is short and the sample group is not large enough, so there are not enough data samples to support the conclusion, but at present, the experiment has not found serious side effects, and the degree of side effects has not been found to be positively correlated with the drug dose, and the phase III clinical trial plan is also under way.