Medically reviewed by Drugs.com. Last updated on Jun 3, 2019.
(e voe LOK ue mab)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Auto-injector, Subcutaneous [preservative free]:
Repatha SureClick: 140 mg/mL (1 mL) [contains mouse (murine) and/or hamster protein, polysorbate 80]
Solution Cartridge, Subcutaneous [preservative free]:
Repatha Pushtronex System: 420 mg/3.5 mL (3.5 mL) [contains polysorbate 80]
Solution Prefilled Syringe, Subcutaneous [preservative free]:
Repatha: 140 mg/mL (1 mL) [contains mouse (murine) and/or hamster protein, polysorbate 80]
Brand Names: U.S.
- Repatha Pushtronex System
- Repatha SureClick
- Antilipemic Agent, PCSK9 Inhibitor
- Monoclonal Antibody
Evolocumab is a human monoclonal antibody (IgG2 isotype) that binds to proprotein convertase subtilisin kexin type 9 (PCSK9). PCSK9 binds to the low-density lipoprotein receptors (LDLR) on hepatocyte surfaces to promote LDLR degradation within the liver. LDLR is the primary receptor that clears circulating LDL; therefore, the decrease in LDLR levels by PCSK9 results in higher blood levels of LDL-cholesterol (LDL-C). By inhibiting the binding of PCSK9 to LDLR, evolocumab increases the number of LDLRs available to clear LDL from the blood, thereby lowering LDL-C levels.
IV: Vd: ~3.3 L
Onset of Action
Peak effect: Proprotein convertase subtilisin kexin type 9 (PCSK9) suppression: 4 hours
Time to Peak
SubQ: 3 to 4 days
11 to 17 days
Special Populations: Hepatic Function Impairment
In patients with mild or moderate hepatic impairment, a 20% to 30% lower mean Cmax and 40% to 50% lower mean AUC occurs.
Use: Labeled Indications
Homozygous familial hypercholesterolemia: Adjunct to diet and other LDL-lowering therapies (eg, statins, ezetimibe, LDL apheresis) for the treatment of patients with homozygous familial hypercholesterolemia who require additional lowering of LDL-C
Hyperlipidemia, primary: Adjunct to diet, alone or in combination with other lipid-lowering therapies (eg, maximum tolerated dose of statins), for the treatment of adults with primary hyperlipidemia, including heterozygous familial hyperlipidemia, to reduce LDL-C (Sabatine 2015)
Prevention of cardiovascular events in patients with established cardiovascular disease: To reduce the risk of MI, stroke, and coronary revascularization in adults with established cardiovascular disease. Note: Use in combination with an optimized regimen of lipid-lowering therapy (eg, high-intensity statin) (Sabatine 2017).
Serious hypersensitivity to evolocumab or any component of the formulation.
Documentation of allergenic cross-reactivity for PCSK9 inhibitors is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Note: Use may be considered in patients who do not meet cholesterol treatment goals with dietary modification and other lipid-lowering therapies (eg, maximally tolerated statin with or without ezetimibe) (AHA/ACC [Grundy 2018]).
Homozygous familial hypercholesterolemia: SubQ: 420 mg once monthly.
Off-label dosing: 420 mg once every 2 weeks (after 12 weeks, may decrease to 420 mg once a month) in conjunction with lipid apheresis has been studied in a limited number of patients (Bruckert 2014). The European Atherosclerosis Society recommends administration directly after lipid apheresis (EAS [France 2016]).
Hyperlipidemia, primary: SubQ: 140 mg every 2 weeks or 420 mg once monthly.
Prevention of cardiovascular events in patients with established cardiovascular disease: SubQ: 140 mg every 2 weeks or 420 mg once monthly.
Switching regimens: Administer the first dose of the new regimen on the next scheduled day of the prior regimen.
Missed dose: Administer within 7 days from the missed dose and resume original schedule. If an every-2-week dose is not administered within 7 days, wait until the next dose on the original schedule. If a once-monthly dose is not administered within 7 days, administer the dose and start a new schedule based on this date.
Refer to adult dosing.
Homozygous familial hypercholesterolemia: Adolescents 13 to 17 years: SubQ: Refer to adult dosing.
Missed dose: Refer to adult dosing.
For SubQ administration. Do not shake. If refrigerated, allow to stand at room temperature for at least 30 minutes (single-use prefilled autoinjector or single-use prefilled syringe) or at least 45 minutes (single-use on-body infusor with prefilled cartridge) prior to use (do not warm with heat or hot water). Administer into areas of the abdomen (except for the 2-inch area around the navel), thigh, or upper arm; only use areas that are not tender, bruised, red, or indurated. Do not coadminister with other injectable drugs at the same injection site. Rotate the injection site with each injection.
Once-monthly dose (ie, 420 mg): Administer SubQ over 9 minutes using the single-use infusor with prefilled cartridge or give 3 separate SubQ 140 mg injections consecutively within a 30-minute period using the single-use prefilled autoinjector or single-use prefilled syringe.
Store between 2°C to 8°C (36°F to 46°F) in the original carton. May also store at room temperature (at 20°C to 25°C [68°F to 77°F]) in the original carton; however, under these conditions, must use within 30 days (discard if not used within 30 days). Protect from direct light and do not expose to temperatures above 25°C (77°F). Do not freeze.
There are no known significant interactions.
>10%: Respiratory: Nasopharyngitis (6% to 11%)
1% to 10%:
Cardiovascular: Hypertension (3%)
Central nervous system: Dizziness (4%), fatigue (2%)
Dermatologic: Skin rash (1%)
Endocrine & metabolic: Diabetes mellitus (9%)
Gastrointestinal: Gastroenteritis (3% to 6%), nausea (2%)
Genitourinary: Urinary tract infection (5%)
Hematologic & oncologic: Bruise (1%)
Infection: Influenza (8% to 9%)
Local: Injection site reaction (6%)
Neuromuscular & skeletal: Myalgia (4%)
Respiratory: Upper respiratory tract infection (9%), cough (1% to 5%), sinusitis (4%)
<1%, postmarketing, and/or case reports: Angioedema, antibody development, flu-like symptoms, hypersensitivity reaction
Concerns related to adverse effects:
• Hypersensitivity reactions: Hypersensitivity reactions (eg, angioedema, rash, urticaria) have been reported, some requiring discontinuation. Discontinue treatment and initiate supportive treatment in patients who develop signs/symptoms of serious allergic reaction; monitor until symptoms resolve.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Dosage form specific issues:
• Latex: The packaging (needle cap of prefilled syringe and autoinjector) may contain dry natural rubber, which is a derivative of latex.
Lipid profile (fasting or nonfasting) before initiating treatment; fasting lipid profile should be rechecked 4 to 12 weeks after starting therapy and every 3 to 12 months thereafter (AHA/ACC [Grundy 2018]); signs/symptoms of hypersensitivity reactions.
Evolocumab is a humanized monoclonal antibody (IgG2). Potential placental transfer of human IgG is dependent upon the IgG subclass and gestational age, generally increasing as pregnancy progresses. The lowest exposure would be expected during the period of organogenesis (Palmeira 2012; Pentsuk 2009).
Data collection to monitor pregnancy and infant outcomes following exposure to evolocumab is ongoing. Health care providers are encouraged to enroll females exposed to evolocumab during pregnancy in the Pregnancy Registry (1-877-311-8972 or https://mothertobaby.org/ongoing-study/repatha).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience pharyngitis, rhinitis, flu-like symptoms, signs of common cold, back pain, or injection site irritation. Have patient report immediately to prescriber signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, flushing, fast breathing, or breath that smells like fruit) (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer:Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
More about evolocumab
- Side Effects
- During Pregnancy
- Dosage Information
- En Español
- 235 Reviews
- Drug class: PCSK9 inhibitors
Other brands: Repatha