PCSK9 inhibitors

PCSK9 inhibitors are medicines that reduce PCSK9 activity, allowing more LDL receptors to return to the liver-cell surface and lowering LDL cholesterol in blood.

PCSK9: PCSK9 is a protein that promotes the breakdown of LDL receptors in liver cells. These medicines lower LDL cholesterol by blocking this protein’s action.
Familial hypercholesterolemia: Familial hypercholesterolemia is an inherited disorder that causes very high LDL cholesterol from birth. PCSK9 inhibitors can help lower LDL when inherited disease leaves levels difficult to control.
Alirocumab: Alirocumab is a monoclonal antibody medicine that binds PCSK9. It is a second widely used antibody option alongside evolocumab.
FOURIER trial: FOURIER was a randomized trial testing evolocumab in patients with established atherosclerotic cardiovascular disease. It showed that adding evolocumab to statin therapy reduced cardiovascular events.
LDL receptor: The LDL receptor is a cell-surface protein that removes low-density lipoprotein particles from blood. Inhibiting PCSK9 lets more receptors recycle to the surface and clear LDL.
Atherosclerotic cardiovascular disease: Atherosclerotic cardiovascular disease is illness caused by plaque buildup in arteries, including coronary and cerebrovascular disease. Patients with established disease may receive these drugs to reduce LDL and future event risk.
Monoclonal antibody: A monoclonal antibody is a laboratory-produced antibody designed to bind a specific molecular target. Most established PCSK9 inhibitors are antibodies that bind the protein outside cells.
ODYSSEY OUTCOMES: ODYSSEY OUTCOMES was a randomized trial of alirocumab after acute coronary syndrome. It tested whether PCSK9 inhibition benefits patients soon after a major coronary event.
Evolocumab: Evolocumab is a monoclonal antibody medicine that binds PCSK9. It is one of the injectable antibodies used to inhibit PCSK9.
Statin: Statins are medicines that lower cholesterol by inhibiting hepatic cholesterol synthesis and increasing LDL-receptor expression. They are usually foundational therapy, while PCSK9 inhibitors are added when LDL remains above target.

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