Scientists have discovered an orally delivered medication that reduces cholesterol levels in animal models by 70%. As per The Indian Express, the finding, which was published in Cell Reports, reveals a hitherto unrecognized technique for cholesterol management and may possibly have implications for cancer therapy.
PCSK9 inhibitors are the second-leading family of drugs for cholesterol management, following statins, according to researchers. These very effective drugs assist the body in removing excess cholesterol from the blood, but unlike statins, which are available as oral agents, PCSK9 inhibitors can only be provided via injection, presenting barriers to their use, as stated by the researchers.
In the most recent study, scientists from University Hospitals (UH) and Case Western Reserve University School of Medicine, United States, created an orally administered small-molecule medication that reduces PCSK9 levels and cholesterol levels in animal models 70%.
“Lowering cholesterol is one of the most important medications we have to prolong life and protect patients from heart disease, which is still the leading cause of morbidity and mortality in the Western world,” said UH and Case Western Reserve School of Medicine Professor Jonathan S. Stamler.
“Statins reduce cholesterol to a limited extent. Stamler stated that this medication family represents a novel approach to lowering cholesterol by targeting PCSK9. PCSK9 in the bloodstream regulates the quantity of LDL receptors by degrading them. Inhibitors of PCSK9, therefore, increase the amount of LDL receptors that remove cholesterol.
By dilating blood arteries, nitric oxide is known to prevent heart attacks, according to the study. Stamler and colleagues demonstrate in a recent study that nitric oxide can also target and inhibit PCSK9, hence lowering cholesterol levels.
They identified a small-molecule medication that increases PCSK9 inactivation by nitric oxide. The medication decreases LDL “bad” cholesterol by 70% in mice treated with it.
In addition to having an impact on the field of cholesterol metabolism, the findings may have implications for cancer patients, as increasing data suggest that targeting PCSK9 can enhance the efficacy of cancer immunotherapies, according to the researchers.
Stamler stated, “PCSK9 not only targets LDL receptors for degradation, but it also facilitates the degradation of MHC 1 on lymphocytes, which is used to recognize cancer cells.”
Effectively, PCSK9 prevents lymphocytes from recognizing cancer cells. Therefore, inhibiting PCSK9 can enhance the body’s cancer surveillance. “One day, it may be possible to apply these new medications to this requirement,” he continued.