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Erenumab-aooe

Class: Calcitonin Gene-related Peptide (CGRP) Antagonists
- Anti-Calcitonin Gene-related Peptide Monoclonal Antibodies
- Anti-CGRP Monoclonal Antibodies
- Calcitonin Gene-related Peptide Receptor Antagonists
- CGRP Antagonists
- CGRP Receptor Antagonists
Chemical Name: Disulfide with human monoclonal light chain, anti-(human calcitonin gene-related peptide receptor) (human monoclonal heavy chain) immunoglobulin G, dimer
Molecular Formula: C6472H9964N1728O2018S50
CAS Number: 1582205-90-0
Brands: Aimovig

Medically reviewed by Drugs.com on Mar 25, 2022. Written by ASHP.

Introduction

Antimigraine agent; recombinant fully human IgG2 monoclonal antibody that targets calcitonin gene-related peptide (CGRP) receptor.

Uses for Erenumab-aooe

Preventive Treatment of Migraine

Preventive treatment of migraine in adults.

Substantially reduces monthly migraine days and acute antimigraine agent-use days in patients with episodic or chronic migraine (with or without aura) when compared with placebo.

The American Headache Society (AHS) states that erenumab and other anti-CGRP monoclonal antibodies offer a number of advantages over some oral migraine preventive therapies, including no need for dosage escalation, rapid onset of therapeutic activity, minimal risk of adverse drug reactions, favorable overall tolerability profiles, and demonstrated efficacy after failure of prior preventive treatments or in combination with oral preventive treatments. However, the potential benefit of using newer therapies such as the anti-CGRP monoclonal antibodies over established therapies should be considered on an individual basis.

AHS has established a criteria for initiating treatment with anti-CGRP monoclonal antibodies based on a balance of cost-effective considerations and access to care; according to this criteria, use of anti-CGRP monoclonal antibodies may be appropriate when patients with migraine are unable to tolerate and/or have an inadequate response to an 8-week trial of at least 2 oral preventive therapies (e.g., topiramate, valproate, β-adrenergic blocking agents, tricyclic antidepressants, selective serotonin- and norepinephrine-reuptake inhibitors).

Erenumab-aooe Dosage and Administration

General

Patient Monitoring

  • Monitor patients for hypersensitivity reactions.

  • Monitor patients for severe constipation.

  • Monitor patients for new-onset or worsening hypertension.

Dispensing and Administration Precautions

  • Some packaging components of erenumab-aooe contain dry natural rubber, which may cause allergic reactions in individuals sensitive to latex.

Administration

Administer by sub-Q injection once monthly.

Commercially available in single-dose prefilled auto-injectors (i.e., injection pens) and single-dose prefilled syringes containing 70 or 140 mg of the drug; intended for patient self-administration.

Sub-Q Administration

Administer by sub-Q injection into the abdomen, thigh, or outer area of upper arm; avoid injections within 2 inches of the navel. Use upper arm only if someone other than the patient (e.g., caregiver, healthcare professional) is administering the injection. Avoid injection into areas where the skin is tender, bruised, erythematous, or indurated.

Prior to use, provide patients and/or caregivers with proper training on how to prepare and administer erenumab-aooe sub-Q using the prefilled auto-injectors or syringes, including aseptic technique. Consult manufacturer's labeling for detailed instructions.

Prior to sub-Q administration, remove prefilled auto-injector or syringe from carton and allow to sit at room temperature for ≥30 minutes; avoid exposure to direct sunlight. Do not warm auto-injectors and syringes using a heat source (e.g., microwave, hot water). Do not use if the solution is cloudy or discolored or contains flakes or particles.

Prefilled auto-injectors and syringes are intended for single-use only; discard any unused portions.

Dosage

Adults

Migraine
Preventive Treatment
Sub-Q

70 mg once monthly. May consider 140 mg once monthly in some patients. Gradual dosage titration not necessary; may initiate therapy with either the 70- or 140-mg dose.

If a dose is missed, administer the missed dose as soon as possible. May then schedule subsequent doses once monthly from the date of the last administered dose.

When initiating therapy with erenumab or another anti-CGRP monoclonal antibody in patients already receiving a preventive treatment for migraine, the American Headache Society (AHS) recommends adding the anti-CGRP monoclonal antibody to the existing antimigraine regimen. Consider onset and magnitude of effect with the anti-CGRP monoclonal antibody when deciding whether to discontinue the existing therapy.

Assess clinical efficacy after 3 months of treatment; continue therapy only if treatment benefits have been observed by that time.

Special Populations

Hepatic Impairment

No specific dosage recommendations.

Renal Impairment

No specific dosage recommendations.

Geriatric Patients

Select dosage carefully, usually starting at the low end of the dosage range.

Cautions for Erenumab-aooe

Contraindications

  • Serious hypersensitivity to erenumab-aooe or any excipients in the formulation.

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions, including rash, angioedema, and anaphylaxis, reported during postmarketing experience. Most hypersensitivity reactions were not serious and occurred within hours of administration; however, some reactions occurred >1 week following administration.

If a serious or severe hypersensitivity reaction occurs, discontinue administration of the drug and initiate appropriate therapy.

Latex Sensitivity

Some packaging components (e.g., needle shield within cap of the prefilled auto-injector, needle cap of the prefilled syringe) of erenumab-aooe contain natural rubber (a latex derivative), which may cause allergic reactions in individuals sensitive to latex.

Constipation with Serious Complications

Constipation with serious complications, in some cases requiring hospitalization or surgery, reported. Concomitant use of drugs associated with decreased GI motility may increase risk. Onset of constipation generally reported following first dose, but may occur at any time during therapy.

Monitor for severe constipation and manage as clinically appropriate.

Hypertension

New-onset hypertension and worsening of preexisting hypertension, in some cases requiring treatment or hospitalization, reported. Many patients had preexisting hypertension or risk factors for hypertension. Hypertension generally reported within 7 days of dose administration and, in the majority of cases, occurred after the first dose, but may occur at any time.

Monitor for new-onset or worsening hypertension. If hypertension occurs, consider discontinuance of erenumab therapy if alternative etiology cannot be identified.

Immunogenicity

Potential for immunogenicity. Antibodies to erenumab, including neutralizing antibodies to the drug, reported. Available data do not demonstrate an effect of anti-erenumab antibody development on efficacy or safety of the drug; however, data are too limited to make definitive conclusions.

Specific Populations

Pregnancy

No adequate data on the developmental risk associated with use of erenumab in pregnant women. No adverse effects on offspring observed when pregnant monkeys received the drug sub-Q at dosages resulting in systemic exposures approximately 20 times the exposure from the maximum recommended human dosage.

Possible increased risk of preeclampsia during pregnancy in women with migraine.

Lactation

Not known whether distributed into human milk. Effects on the breast-fed infant or on milk production also unknown. Consider developmental and health benefits of breast-feeding, mother's clinical need for erenumab, and potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Pediatric Use

Manufacturer states that safety and efficacy not established in pediatric patients <18 years of age.

Pending further clinical experience with anti-CGRP monoclonal antibodies in pediatric patients, the American Headache Society (AHS) recommends limiting use of anti-CGRP monoclonal antibodies mainly to postpubertal adolescents with relatively frequent migraines (i.e., ≥8 headache days per month) who have moderate to severe disability associated with migraine (e.g., PedMIDAS score ≥30) and in whom ≥2 preventive therapies have failed. For younger pediatric patients with severe chronic migraine that is refractory to multiple preventive therapies, consider anti-CGRP monoclonal antibodies only in carefully selected patients with close monitoring (e.g., pubertal status, bone health, linear growth, weight, body mass index [BMI], infectious complications).

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.

Select dosage with caution, usually starting at the low end of the dosage range. Consider the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy when selecting dosage in geriatric patients.

Hepatic Impairment

Hepatic impairment not expected to affect pharmacokinetics.

Renal Impairment

Renal impairment not expected to affect pharmacokinetics.

Common Adverse Effects

Common adverse effects (≥3%): Injection site reactions, constipation.

Interactions for Erenumab-aooe

Not metabolized by CYP isoenzymes. Unlikely to affect drug-metabolizing enzymes or drug transporters.

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Inhibitors or inducers of CYP isoenzymes: Pharmacokinetic interactions unlikely.

Substrates of major CYP isoenzymes: Pharmacokinetic interactions unlikely.

Drugs Affected by Drug Transport Systems

Substrates of various drug transport systems: Pharmacokinetic interactions unlikely.

Drugs Associated with Decreased GI Motility

Possible increased risk of severe constipation and constipation-related complications.

Specific Drugs

Drug

Interaction

Contraceptives, oral (ethinyl estradiol with norgestimate)

Pharmacokinetics of the oral contraceptive not affected

Sumatriptan

Pharmacokinetics of sumatriptan not affected

Concomitant administration of erenumab-aooe (single 140-mg IV dose) and sub-Q sumatriptan (given as two 6-mg sub-Q doses 1 hour apart) in healthy individuals did not result in increased mean arterial pressure and resting BP compared with sumatriptan administered alone

Concomitant administration is well tolerated

Erenumab-aooe Pharmacokinetics

Absorption

Bioavailability

Following single-dose, sub-Q administration, estimated absolute bioavailability is 82%.

Peak concentrations achieved in approximately 6 days following a single sub-Q dose.

Steady-state trough concentrations approached in 3 months following once-monthly sub-Q administration; systemic accumulation is less than twofold.

Exhibits nonlinear pharmacokinetics due to binding to the CGRP receptor; however, at clinically relevant dosages, pharmacokinetics following once-monthly sub-Q administration are predominantly linear because of saturation of binding to the CGRP receptor.

Onset

Antimigraine effects usually evident following 1–3 monthly sub-Q injections in responding patients.

Special Populations

Renal or hepatic impairment not expected to affect pharmacokinetics.

Age, sex, race, or subtype of migraine spectrum (e.g., episodic or chronic migraine) does not affect pharmacokinetics.

Distribution

Extent

Due to large molecule size, unlikely to cross the blood-brain barrier.

Not known whether distributed into human milk.

Elimination

Elimination Route

At low concentrations, predominantly eliminated through saturable binding to the CGRP receptor; at higher concentrations, predominantly eliminated through a nonspecific, nonsaturable proteolytic pathway.

Half-life

Effective half-life: 28 days.

Stability

Storage

Parenteral

Injection

2–8°C in original carton to protect from light until time of use; do not freeze. Do not shake.

If removed from the refrigerator, store at room temperature (≤25°C) in the original carton; use within 7 days. Discard if stored at room temperature for >7 days.

Actions

  • A fully human IgG2 immunoglobulin that binds to the CGRP receptor and antagonizes CGRP receptor function. Produced using recombinant DNA technology in Chinese hamster ovary cells.

  • CGRP is a potent vasodilator and pain-signaling neuropeptide associated with migraine pathophysiology. CGRP and its receptors are located at sites that are relevant to migraine development (e.g., trigeminal neurons); they also are widely distributed throughout the central and peripheral nervous systems as well as in non-neuronal tissues throughout the body.

  • Increased serum CGRP concentrations observed in individuals during acute migraine attacks (with or without aura). IV infusion of CGRP induces migraines in patients with a history of migraines.

  • Potently and selectively binds to the extracellular binding site of the CGRP receptor and competitively blocks its interaction with CGRP.

  • Because of its large molecular size, unlikely to cross the blood-brain barrier; probably antagonizes CGRP receptor function peripherally rather than centrally within the nervous system.

Advice to Patients

  • Importance of advising patients to read the manufacturer's patient information and instructions for use.

  • Importance of providing guidance to patients and/or caregivers on proper sub-Q administration of erenumab-aooe, including the use of aseptic technique, and use of the single-dose auto-injectors or syringes. Importance of instructing patients and/or caregivers to read and follow the instructions for use each time they use erenumab-aooe.

  • If a dose is missed, administer the missed dose as soon as possible. Schedule subsequent doses monthly from the date of the last administered dose.

  • Some packaging components of erenumab-aooe (e.g., needle shield within cap of the prefilled auto-injector, needle cap of the prefilled syringe) contain dry natural rubber (a derivative of latex), which may cause allergic reactions in individuals sensitive to latex. Importance of alerting clinician if allergy to rubber or latex exists.

  • Importance of advising patients to seek immediate medical attention if they experience any symptoms of serious or severe hypersensitivity reactions.

  • Risk of constipation with serious complications, including the need for hospitalization or surgery. Importance of advising patients to contact their clinician if they experience severe constipation.

  • Risk of developing hypertension or worsening of pre-existing hypertension. Importance of advising patients to contact their clinician if they experience elevation in their blood pressure.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses (e.g., hypertension).

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Erenumab-aooe

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for subcutaneous use only

70 mg/1 mL

Aimovig (available as single-dose prefilled auto-injectors [SureClick] and single-dose prefilled syringes)

Amgen , (comarketed with Novartis)

140 mg/1 mL

Aimovig (available as single-dose prefilled auto-injectors [SureClick] and single-dose prefilled syringes)

Amgen , (comarketed with Novartis)

AHFS DI Essentials™. © Copyright 2022, Selected Revisions March 25, 2022. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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