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PCSK9 Inhibitor for Lipid Disorders

What is PCSK9?

PCSK9 stands for proprotein convertase subtilisin kexin 9. It is a serine protease, a type of enzyme, mostly produced in the liver.

What does PCSK9 do?

It helps break down low density lipoprotein (LDL) receptors in the liver, which in turn increases LDL-C (low density lipoprotein cholesterol or “bad cholesterol”) levels.

Why would PCSK9 inhibitors work?

By blocking the action of the PCSK9 enzyme, LDL-C levels can be decreased.

What types are out there?

evolocumab from Amgen

alirocumab from Regeneron Pharmaceuticals and Sanofi

bococizumab from Pfizer

All of these PCSK9 inhibitors are monoclonal antibodies to PCSK9 that are given as a subcutaneous injection.

Where are PCSK9 inhibitors in the drug development process?

They have not yet been approved for use. However, many studies have shown statistically significant reductions in LDL-C!

The Further Cardiovascular Outcomes Research with PCSK9 Inhibition in Subjects with Elevated Risk (FOURIER) study includes 22,500 patients. The full results will not be available until 2018 at the earliest.

Completed and ongoing studies include:

DESCARTES, LAPLACE-2, GAUSS-2, MENDEL-2, and RUTHERFORD-2 with evolocumab

studies for alirocumab and bococizumab are currently running

SPIRE-1 and SPIRE-2 with bococizumab for 22,000 patients started in October 2013

What side effects have been seen so far during the clinical studies?

Nasopharyngitis

Upper respiratory tract infection

Influenza

Muscle-related issues

Sources:

O’Riordan, M. (2014, March 30). Strong results from early studies with PCSK9 inhibitors generating big buzz. Medscape. Retrieved from http://www.medscape.com/viewarticle/822814

Rosenson, R.S., de Ferranti, S.D., Durrington, P. (2014, November 14). Treatment of drug-resistant hypercholesterolemia. UpToDate. Retrieved from http://www.uptodate.com/contents/treatment-of-drug-resistant-hypercholesterolemia

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