Cholesterol-lowering is one of the most important therapies we have to prolong life and protect people from heart disease, which is still the number one cause of morbidity and mortality in the Western world.
In a study from University Hospitals (UH) and Case Western Reserve University, scientists found a new drug to reduce blood cholesterol levels.
After statins, the next leading class of medications for managing cholesterol are PCSK9 inhibitors.
These highly effective agents help the body pull excess cholesterol from the blood, but unlike statins, which are available as oral agents, PCSK9 inhibitors can only be administered as shots, creating barriers to their use.
In the study, the team found an orally administered small-molecule drug that reduces PCSK9 levels and lowers cholesterol in animal models by 70%.
The findings represent a previously unrecognized strategy for managing cholesterol and may also impact cancer treatments.
Central to cholesterol regulation are LDL receptors, which sit at the surface of liver cells and remove cholesterol from the blood, thereby lowering serum levels.
PCSK9 in the bloodstream controls the number of LDL receptors by marking them for degradation. Therefore, agents that inhibit PCSK9 increase the number of LDL receptors that remove cholesterol.
Nitric oxide is a molecule that is known to prevent heart attacks by dilating blood vessels.
In the new study, the team showed that nitric oxide can also target and inhibit PCSK9, thus lowering cholesterol.
They identify a small molecule drug that functions to increase nitric oxide inactivation of PCSK9. Mice treated with the drug display a 70% reduction in LDL “bad” cholesterol.
In addition to impacting the field of cholesterol metabolism, the findings may impact patients with cancer, as emerging evidence suggests targeting PCSK9 can improve the efficacy of cancer immunotherapies.
If you care about heart health, please read studies about new way to prevent heart attacks, strokes, and common nutrient that is good for your heart rate.
For more information about health, please see recent studies about how oral health may affect your heart, brain and risk of death, and results showing aspirin is linked to increased risk of heart failure.
The study was conducted by Jonathan S. Stamler et al and published in Cell Reports.
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