evolocumab

REMS

Primary hyperlipidemia (including heterozygous familial hypercholesterolemia [HeFH]) in adults (as an adjunct to diet as monotherapy or in combination with other low-density lipoprotein cholesterol [LDL-C]-lowering therapies).
Homozygous familial hypercholesterolemia (in combination with other LDL-C lowering therapies).
HeFH in pediatric patients ≥10 yr (as an adjunct to diet in combination with other LDL-C-lowering therapies).
To reduce the risk of MI, stroke, and coronary revascularization in patients with cardiovascular disease.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

Severe renal impairment;
Severe hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Children <10 yr (safety and effectiveness not established);
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

Local: injection site reactions

MS: back pain

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Solution for injection (needle cover contains latex derivative) (prefilled syringes and autoinjectors): 140 mg/mL

Route/Dosage ⬆ ⬇

Established Cardiovascular Disease or Primary Hyperlipidemia

SC (Adults ): 140 mg every 2 wk or 420 mg once monthly.

Heterozygous Familial Hypercholesterolemia

SC (Children ≥10 yr): 140 mg every 2 wk or 420 mg once monthly.

Homozygous Familial Hypercholesterolemia

SC (Adults and Children ≥10 yr): 420 mg once monthly; if inadequate response after 12 wk, may ↑ to 420 mg every 2 wk. Patients on lipid apheresis: 420 mg every 2 wk (administered after apheresis session completed).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

A human monoclonal immunoglobulin 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-C from blood.

Therapeutic effects:

Reduction in LDL-C.
Reduction in the risk of MI, stroke, and coronary revascularization.

Classifications ⬆ ⬇

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: proprotein convertase subtilisin kexin type-9 pcsk-9 inhibitors, monoclonal antibodies

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed (72%) following SUBQ administration.

Distribution: Minimally distributed to tissues.

Metabolism/Excretion: Eliminated by binding to PCSK9 and by proteolytic degradation.

Half-Life: 11–17 days.

Time/Action Profile ⬆ ⬇

(effect on circulating unbound PCSK9)

ROUTE	ONSET	PEAK	DURATION
SUBQ	rapid	4 hr	2–4 wk

Patient/Family Teaching ⬆ ⬇

Instruct patient in correct technique for self-injection and 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.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Inform pregnant patients of pregnancy safety study that monitors pregnancy outcomes in women exposed to evolocumab during pregnancy. Enroll patient by contacting Amgen at 1-800-77-AMGEN (1-800-772-6436).

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Indications ⬇