An investigation into statins, PCSK9 inhibitors, and other current cholesterol treatments
Kiley, Mark E.
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Hypercholesterolemia is one of the most prevalent, yet underdiagnosed diseases faced by the medical community today. Its prevalence can largely be attributed to diet, lack of exercise, and lifestyle choices such as smoking or drinking, but there is also a genetic component. Familial Hypercholesterolemia is the genetic disorder in which a person is unable to properly eliminate levels of low-density lipoprotein, mostly due to an ineffective receptor in the liver. Hypercholesterolemia has been positively correlated with the prevalence of cardiovascular disease, and patients with the severe homozygous familial hypercholesterolemia typically have abbreviated lifespans. In these situations, and also those less acutely dire, it’s necessary to rely on medication to help maintain one’s cholesterol levels to within low risk ranges. High does statin therapy has been shown to be the most effective therapy for maintaining LDL cholesterol. It has become the standard regardless of the cause of hypercholesterolemia because of its few side effects, its high tolerability, its ease of administration, its safety, and most of all because of its immense efficacy. This has not, however, prevented the exploration into other types of cholesterol therapies that may work in concurrence with statins. Drug classes such as PCSK9 inhibitors, ApoB inhibitors, MTP inhibitors, and thyromimetics have all been explored with varying success. Each of these potential therapies has a separate mechanism of action, allowing for modulation in conjunction with statins. PCSK9 inhibitors and ApoB inhibitors appear to provide the most upside by virtue of LDL lowering capabilities, followed by a drug known as ezetimibe that reduces dietary cholesterol uptake in the gut. MTP inhibitors have been shown to be effective therapies for homozygous familial hypercholesterolemia specifically due to their function of lowering LDL particle creation rather than LDL receptor number or function as statins and PCSK9 inhibitors do. Thyromimetics have yet to yield an effective therapy for cholesterol treatment, but the hope remains alive that this could come to fruition in the future.