By: Katie Lee, PharmD Candidate c/o 2019
In 2015, FDA approved evolocumab (Repatha ®), a human monoclonal antibody of the PCKSK9 (proprotein convertase subtilisin kexin type 9) inhibitor class.1 Evolocumab is used to treat adult patients with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease who need further lowering of their LDL-C levels, while being on maximum tolerated statin therapy. 1 Evolocumab is also further approved for adult patients with homozygous familial hypercholesterolemia (HoHF), who are not controlled on other LDL-lowering therapies, such as Ezetimibe (Zetia®). PCSK9 is a protein that binds to LDL receptors and is responsible for its degradation2. Since evolocumab is a PCSK9 inhibitor, it blocks the effects of PCSK9 and prevents the degradation of LDL receptors1. This allows for an increase in the availability of LDL receptors to bind to circulating cholesterol, reducing the amount of free cholesterol in the blood.
The route of administration of evolocumab is injection administered subcutaneously; however, there are different dosage directions depending on whether the patient has HeFH and clinical atherosclerotic disease or HoFH1. Up to July 2016, the recommended direction was to administer a dose of 420mg and give three injections consecutively within thirty minutes. The new direction is to administer a dose of 420mg over nine minutes using a single-use-on-body infusor with a prefilled cartridge, or by giving three injections consecutively within thirty minutes using the single-use prefilled autoinjector or single-use prefilled syringe. 1
The common adverse effects of evolocumab include nasopharyngitis, upper respiratory tract infection, influenza, back pain, and injection site reactions that result in redness and itching at where the injection was administered1. If the patient develops signs of an allergic reaction, such as rash and hives, the patient should discontinue the medication and seek medical help immediately1.
Although evolocumab is effective at reducing of LDL-C levels in the blood, its effects on reducing morbidity and mortality are still in question1. Unlike statins, there is no proven benefit with evolocumab in preventing cardiovascular events such as strokes or heart attacks2. Evolocumab still needs to be monitored for its efficacy in patients and their quality of life.
- REPATHA (EVOLOCUMAB) [package insert]. Thousand Oaks, CA; Amgen Inc.; Revised 07/2016.
- Pahon E. FDA approves Repatha to treat certain patients with high cholesterol. FDA. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm460082.htm. Published 08/27/2015.