FDA Approves Evolocumab

to treat Certain Patients with High

CholesterolDr. P.Naina Mohamed PhD

Pharmacologist

On 27th Aug 2015, the U.S. Food and Drug Administration approved Evolocumab injection to treat adult patients with…

Heterozygous familial hypercholesterolemia (HeFH)Homozygous familial hypercholesterolemia (HoFH)

or Clinical atherosclerotic cardiovascular disease

(Stroke, Heart Attack) Evolocumab is approved to be used along with diet and

maximally tolerated statin therapy, in those patients who require additional lowering of LDL cholesterol.

Introduction

Evolocumab is the second PCSK9 (Proprotein Convertase Subtilisin Kexin type9) inhibitor.

Evolocumab is a monoclonal antibody and it is administered by subcutaneous injection.

The recommended dose of Evolocumab for adults is 140 mg every two weeks or 420 mg once a month.

For adults with HoFH, the recommended dose is 420 mg once a month.

Evolocumab

Mechanism of Action

Evolocumab(Repatha)

Binds to Proprotein Convertase Subtilisin Kexin type 9 (PCSK9)

Inhibition of binding of PCSK9 to low density lipoprotein receptors (LDLR) at the

surface of hepatocytesIncreased number of LDLR available to

clear LDL particles

Lowering of LDL cholesterol

Adverse Drug Reactions (ADRs)

The most common side effects of Evolocumab (Repatha) include…

Nasopharyngitis Upper respiratory tract infectionFlu like symptomsBack painRedness, pain, or bruising at the injection site.Allergic reactions (Rash and hives)Patients should stop using Evolocumab

(Repatha) and get medical help if they experience symptoms of a serious allergic reaction.

http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm460082.htm?source=govdelivery&utm_medium=email&utm_source=govdelivery

http://www.nejm.org/doi/full/10.1056/NEJMoa1500858#t=articleTop

http://content.onlinejacc.org/article.aspx?articleid=1853981

http://circres.ahajournals.org/content/early/2015/07/30/CIRCRESAHA.115.307071.abstract

http://www.nejm.org/doi/full/10.1056/NEJMoa1316222#t=articleTop

References