proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor antibodies
Lowering of low density lipoprotein cholesterol (LDL-C) as an adjunct to diet and maximally tolerated statin (HMG CoA reductase inhibitor) therapy in patients with heterozygous familial hypercholesterolemia (HeFH) or cardiovascular disease who require supplemental agents.
A human monoclonal immunoglobulin (IgG1) produced in genetically engineered Chinese hamster ovary cells that binds to PCSK9 inhibiting its binding to the low density lipoprotein receptor (LDLR) resulting in ↑ number of LDLRs available to clear LDL from blood.
Absorption: Well absorbed (85%) following subcut administration.
Distribution: Mostly distributed in the circulatory system; crosses the placenta.
Metabolism and Excretion: Eliminated by binding to PCSK9 and by proteolytic degradation.
Half-life: 17–20 days.
TIME/ACTION PROFILE (effect circulating unbound PCSK9)
|subcut||rapid||4–8 hr||2 wk|
- History of serious hypersensitivity to alirocumab.
Use Cautiously in:
- Severe renal/hepatic impairment;
- Geri: Elderly patients may be more sensitive to drug effects;
- OB: Crosses the placenta, consider fetal risks
- Lactation: Consider benefits of breast feeding against possible risk to infant
- Pedi: Safe and effective use in children has not been established.
Adverse Reactions/Side Effects
Local: injection site reactions
Misc: serious allergic reactions including vasculitis
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
SC: (Adults) 75 mg every 2 wk; if desired LDL-C has not been achieved, dose may be ↑ to 150 mg every 2 wk. If less frequent dosing desired, may initiate therapy with 300 mg every 4 wk; if desired LDL-C has not been achieved, may adjust dose to 150 mg every 2 wk.
Solution for subcutaneous injection: 75 mg/mL (in prefilled pen or prefilled syringe), 150 mg/mL (in prefilled pen or prefilled syringe)
- Obtain a diet history, especially with regard to fat consumption.
- Monitor for signs and symptoms of hypersensitivity reactions (pruritus, rash, urticaria, hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization) during therapy. If severe symptoms occur, discontinue alirocumab.
Lab Test Considerations:
Assess LDL-C levels within 4 to 8 wk of initiating or titrating alirocumab, to assess response and adjust dose, if needed.
- Noncompliance, related to diet and medication regimen (Patient/Family/Teaching)
- SC: Administer every 2 wks. Allow solution to warm to room temperature for 30–40 min before injecting. May be kept at room temperature for up to 30 days. Solution is clear and colorless to pale yellow; do not administer solutions that are cloudy or contain particulate matter. Do not shake. Inject into thigh, abdomen, or upper arm. Rotate sites with each injection. Do not inject into areas with skin disease or injury (sunburns, rashes, inflammation, skin infections). Do not reuse pre-filled pen or syringe. Do not administer other injectable drugs at same site. Store in refrigerator; keep in original container, protect from light. Do not freeze.
- Administer 300 mg dose as two 150 mg injections in 2 different sites.
- Instruct patient in correct technique for self-injection, care and disposal of equipment. Administer missed doses within 7 days, then resume original schedule. If not administered within 7 days, wait until next dose on original schedule. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
- Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
- Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
- Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.
↓ LDL-C levels.
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