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.
- Additional lowering of low density lipoprotein cholesterol (LDL-C) as an adjunct to diet and maximally tolerated statin and other drug therapies in patients with homozygous familial hypercholesterolemia (HoFH).
A human monoclonal immunoglobulin (IgG2) produced in genetically engineered Chinese hamster ovary cells that binds to PSCSK9 inhibiting its binding to the low density lipoprotein receptor (LDLR) resulting in ↑ number of LDLRs available to clear LDL from blood.
Absorption: Well absorbed (72%) following subcut administration.
Distribution: Crosses the placenta.
Metabolism and Excretion: Eliminated by binding to PCSK9 and by proteolytic degradation.
Half-life: 11–17 days.
TIME/ACTION PROFILE (effect circulating unbound PCSK9)
|subcut||rapid||4 hr||2–4 wk|
- History of serious hypersensitivity to evolocumab.
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 <13 yr has not been established.
Adverse Reactions/Side Effects
Local: injection site reactions
MS: back pain
Misc: allergic reactions (including urticaria and rash), flu-like symptoms
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
SC: (Adults) Primary hyperlipidemia with established CVD/HeFH– 140 mg every two wk or 420 mg monthly; HoFH– 420 mg monthly.
Solution for subcutaneous injection (needle cover contains latex derivative): 120 mg/mL (in Pushtronex system), 140 mg/mL (in prefilled syringes and autoinjector)
- Obtain a diet history, especially with regard to fat consumption.
- Monitor for signs and symptoms of hypersensitivity reactions (rash, urticaria) during therapy. If symptoms occur, discontinue therapy.
- Assess for latex allergy. Needle cover of the glass prefilled syringe and the autoinjector contain dry natural rubber (a derivative of latex); may cause allergic reactions.
Lab Test Considerations:
Assess LDL-C levels within 4 to 8 wk of initiating; response to therapy depends on degree of LDL-receptor function.
- Noncompliance, related to diet and medication regimen (Patient/Family/Teaching)
- SC: Administer 140 mg every 2 wks or 420 mg once monthly. To administer the 420 mg dose, give 3 injections, using 3 separate pens/syringes in 3 separate sites, consecutively within 30 minutes. When switching dose regimens, administer first dose of new regimen on next scheduled date of prior regimen. If stored in refrigerator allow solution to warm to room temperature for at least 30 min before injecting. May also be stored at room temperature, but only stable for 30 days. Solution is clear to opalescent 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 that are tender, bruised, red, or indurated. Do not re-use pre-filled pen or syringe. Do not administer other injectable drugs at same site.
- Pushtronex on-body infusor system: Remove on-body infusor and prefilled cartridge from refrigerator 45 min prior to use to allow to reach room temperature; do not use other sources of warming. Prepare injection site with little hair (may trim) and firm and flat skin surface by cleaning with alcohol and allowing to dry. May use thigh, abdomen (except 2 inches from umbilicus) or outer area of upper arm if not self-administered. Avoid areas that are tender, bruised, red, or hard, or areas with wrinkles, skin folds, scars, stretch marks, moles and excessive hair. Solution in cartridge should be clear and colorless to slightly yellow; do not administer solutions that are discolored or contain particular matter. Clean bottom of cartridge with alcohol and load into on-body infusor; press firmly on top of unit to secure. Swing door close until it snaps. Peel away both green pull tabs to show adhesive. When blue light flashes, infusor is on. If using abdomen, stretch skin prior to applying; do not stretch skin for thigh placement. Apply infusor to skin making sure blue light is visible and firmly press start button. Flashing green light and click indicates infusion has begun; may beep and patient may feel a pinch. When green light changes to solid, infusion is complete. Remove from skin and check medicine window for green light to be off. Dispose of on-body infusor in a sharps container.
- Instruct patient in correct technique for self-injection or on-body infusor, 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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