Monoclonal antibody targeting PCSK9

Marketed as Repatha.

A monoclonal antibody designed for the treatment of hyperlipidemia.

Evolocumab inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9).

PCSK9 is a protein that targets LDL receptors for degradation.

An antibody that targets the PCSK9 protein. which reduces the number of receptors on the liver that remove LDL-cholesterol from the blood.

Enhances the removal of circulating LDL cholesterol.

It reduces the liver’s ability to remove LDL-C from the blood.

Evolocumab binds to PCSK9, a natural protein produced by the liver.

Designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface.

In the absence of PCSK9, there are more LDL receptors on the surface of the liver to remove LDL-C from the blood.

Approved for use with diet and maximally tolerated statin therapy in adults with the heterozygous familial hypercholesterolemia, homozygous familial hypercholesterolemia, or clinical atherosclerotic cardiovascular disease such as myocardial infarction a stroke who need to lower their LDL-cholesterol.

The Phase 3 GAUSS-2 (Goal Achievement After Utilizing an Anti-PCSK9 Antibody in Statin Intolerant Subjects-2) trial evaluating evolocumab in patients with high cholesterol who cannot tolerate statins met its co-primary endpoints, with a reduction from baseline in low-density lipoprotein cholesterol (LDL-C) at week 12 and the mean percent reduction from baseline in LDL-C at weeks 10 and 12.

Evolocumab plus standard therapy reduced the LDL cholesterol levels by 61% from the median of 120 mg/dL to 48 mg/L compared with standard therapy during approximately one year of therapy(Sabatine MS et al).

In the above study Evolocumab reduced cardiovascular events after one year of therapy.

GAUSS-3 trial-year-enrolled patients with elevated LDL levels unable to tolerate effective doses of statins: evolocumab compared with ezetimbe resulted in a significantly greater reduction in LDL-C levels at 24 weeks.

Pediatric patients with familial hypercholesterolemia have a reduced LDL cholesterol levels and other variables with evolocumab.

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