erenumab (Rx)

1-10%

Injection site pain (5-6%)

Constipation (1-3%)

Cramps, muscle spasms (<3%)

Postmarketing Reports

Immune system disorders: Rash, angioedema, anaphylaxis, hypersensitivity

Gastrointestinal disorders: Oral mucosal ulceration, constipation with serious complications

Vascular disorders: Hypertension

Contraindications

Hypersensitivity to drug or excipients

Cautions

Hypersensitivity reactions (eg, rash, angioedema, anaphylaxis) reported; may occur within hours or one week following administration; discontinue administration and initiate appropriate therapy if serious reaction occurs

Hypertension

• Development of hypertension and worsening of pre-existing hypertension reported
• Pre-existing hypertension or of risk factors increases risk
• Pharmacological treatment may be necessary
• May occur at anytime but most frequently within seven days of dose administration
• Onset or worsening of hypertension usually reported after first dose
• Monitor for new onset or worsening of pre-existing hypertension and consider whether discontinuation of therapy warranted if no alternate etiology found

Constipation

• Constipation with serious complications reported in the postmarketing setting; cases that required hospitalization, including cases where surgery was necessary reported
• In majority cases, onset of constipation was reported after first dose; however, patients have also presented with constipation later on in treatment
• Monitor patients for severe constipation and manage as clinically appropriate
• Concurrent use of medications associated with decreased gastrointestinal motility may increase risk for more severe constipation and potential for constipation-related complications

Pregnancy

Data are not available regarding fetal risk if used in pregnant women

Animal studies

• No adverse effects on offspring were observed when pregnant monkeys were administered erenumab-aooe throughout gestation

Clinical considerations

• Data suggest that women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy

Lactation

Data are not available on the presence in human milk, the effects on the breastfed infant, or the effects on milk production

Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Human monoclonal antibody; binds to the calcitonin gene-related peptide (CGRP) receptor, which is thought to be causally involved in migraine pathophysiology

Absorption

Absolute bioavailability: 82%

Peak plasma time: ~6 days

Peak plasma concentration: 6.1 mcg/mL (70 mg); 15.8 mcg/mL (140 mg)

AUC: 159 day·mcg/mL (70 mg); 505 day·mcg/mL (140 mg)

Bioavailability: 82%

Distribution

Vd: 3.86 L

Elimination

Half-life: 28 days

2 elimination phases observed

• Low concentrations: Predominantly through saturable binding to target (CGRP receptor)
• Higher concentrations: Largely through a nonspecific, nonsaturable proteolytic pathway

SC Administration

For SC use only

Needle shield within cap of prefilled autoinjector and cap of prefilled syringe contain dry natural rubber (a derivative of latex) may cause allergic reactions in latex-sensitive individuals

Intended for self-administration; properly train on preparation and administration, including aseptic technique

Before SC administration, allow syringe or autoinjector to sit at room temperature for at least 30 minutes protected from direct sunlight

Do not warm by using a heat source (eg, hot water, microwave)

Do not shake product

Visually inspect for particulate matter and discoloration; do not use if solution is cloudy or discolored or contains particles

Administer SC in the abdomen, thigh, or upper arm; do not inject into areas where skin is tender, bruised, red, or hard

Prefilled autoinjector and syringe are single-dose and deliver entire contents

Missed dose

• Administer as soon as possible: reschedule monthly dose from date of last dose

Storage

Refrigerate at 2-8ºC (36-46ºF) in original carton to protect from light

If removed from refrigerator, store at room temperature (up to 25ºC [77ºF]) in original carton for up to 7 days; discard if left at room temperature for >7 days

Do not freeze

Do not shake