Class: Interleukin Antagonists
- Antiasthmatic Agents
Chemical Name: Disulfide with human-mouse monoclonal SB-240563 κ-chain, anti-(human interleukin 5) (human-mouse monoclonal SB-240563 γ1-chain) immunoglobulin G1, dimer
Molecular Formula: C6476H10084N1732O2028S46
CAS Number: 196078-29-2
Medically reviewed by Drugs.com. Last updated on Sep 21, 2020.
Uses for Mepolizumab
Eosinophilic phenotype (i.e., eosinophilic asthma) is generally characterized by blood and sputum eosinophilia, eosinophilic inflammation, recurrent asthma exacerbations, and frequently, responsiveness to corticosteroids.6 8 9 11
Not indicated for treatment of other eosinophilic conditions.1
Not indicated for relief of acute bronchospasm or status asthmaticus.1
Mepolizumab Dosage and Administration
Administer by sub-Q injection into the upper arm, thigh, or abdomen every 4 weeks by a clinician.1
Reconstitute vial containing 100 mg of mepolizumab lyophilized powder with 1.2 mL of sterile water for injection (using a 2- or 3-mL syringe with 21-gauge needle) to provide a solution containing 100 mg/mL.1
Direct the stream of sterile water diluent onto the lyophilized powder.1 Swirl vial gently for 10 seconds approximately every 15 seconds until completely dissolved (typically ≤5 minutes).1 Do not shake.1
Mechanical reconstitution device may be used to swirl the vial at 450 rpm for ≤10 minutes or at 1000 rpm for ≤5 minutes.1
Reconstituted solution is clear to opalescent, colorless to pale yellow or pale brown, and essentially free from particulates (small air bubbles acceptable).1
Adolescents ≥12 years of age: 100 mg every 4 weeks.1
100 mg every 4 weeks.1
No special population dosage recommendations at this time.1
Cautions for Mepolizumab
History of hypersensitivity to the drug or any ingredient in the formulation.1
Hypersensitivity reactions (e.g., angioedema, bronchospasm, hypotension, urticaria, rash) reported, generally occurring within hours or possibly days following administration.1 If hypersensitivity reaction occurs, discontinue mepolizumab.1 (See Contraindications under Cautions.)
Deterioration of Disease and Acute Episodes
Not indicated for treatment of acute asthma symptoms or exacerbations, acute bronchospasm, or status asthmaticus.1 (See Advice to Patients.)
Herpes Zoster Infection
Immune response against some parasitic (helminth) infections may be altered.1 Not studied in patients with known parasitic infections.1 Treat patients with preexisting parasitic (helminth) infections before initiating mepolizumab.1 If parasitic infection occurs and does not respond to anthelmintic treatment, interrupt mepolizumab therapy until infection resolves.1
Reduction of Corticosteroid Dosage
Do not abruptly discontinue systemic or inhaled corticosteroid therapy upon initiation of mepolizumab therapy.1 If appropriate, reduce corticosteroid dosage gradually and supervise such reduction carefully.1
Antibodies to mepolizumab detected in 6% of patients and associated with approximately 20% increased drug clearance.1 No apparent correlation between anti-mepolizumab antibody titers and change in eosinophil concentrations.1 Clinical importance of such antibodies not known.1
Weigh potential risks to infants against clinical need and known benefits of breast-feeding.1
Safety and efficacy not established in children <12 years of age.1
Pharmacokinetics not studied in patients with hepatic impairment.1
Pharmacokinetics not studied in patients with renal impairment.1
Common Adverse Effects
Interactions for Mepolizumab
No formal drug interaction studies to date.1
Absolute bioavailability following sub-Q injection approximately 80%.1
Maximum plasma concentrations occurred from 4–8 days following sub-Q administration.12
Dose-proportional pharmacokinetics over a sub-Q dosage range of 12.5–250 mg.1
Following drug discontinuance, blood and sputum eosinophil counts increase within 3 months, blood eosinophil counts return to baseline over 6 months, and rate of severe asthma exacerbations increases over 3–6 months.10 Exacerbation rate no different than that with placebo after 12 months.10
Adolescents 12–17 years of age: Mean apparent clearance 35% less than that of adults.1
Powder for Injection
Recombinant DNA-derived humanized interleukin-5 (IL-5) receptor antagonist monoclonal antibody and IgG1 kappa immunoglobulin.1
Advice to Patients
Risk of hypersensitivity reactions.1 Importance of patients informing clinicians if hypersensitivity reactions (e.g., angioedema, bronchospasm, hypotension, urticaria, rash) occur.1 (See Sensitivity Reactions under Cautions.)
Importance of informing patients that mepolizumab does not relieve acute asthma symptoms or exacerbations.1 Advise patients to contact their clinician if asthma remains uncontrolled or worsens after treatment initiation.1
Importance of informing patients with asthma receiving inhaled or systemic corticosteroids not to discontinue or reduce corticosteroid dosage since withdrawal symptoms or worsening of asthma may occur; change corticosteroid dosage only under direct supervision of a clinician.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 Importance of clinicians informing women about the manufacturer's pregnancy registry and encouraging patient enrollment.1 (See Pregnancy under Cautions.)
Importance of informing patients of other important precautionary information.1 (See Cautions.)
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.
For injection, for subcutaneous use only
AHFS DI Essentials™. © Copyright 2021, Selected Revisions September 30, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. GlaxoSmithKline. Nucala (mepolizumab) for injection, for subcutaneous use prescribing information. Research Triangle Park, NC; 2015 Nov.
2. Pavord ID, Korn S, Howarth P et al. Mepolizumab for severe eosinophilic asthma (DREAM): a multicentre, double-blind, placebo-controlled trial. Lancet. 2012; 380:651-9. http://www.ncbi.nlm.nih.gov/pubmed/22901886?dopt=AbstractPlus
3. Ortega HG, Liu MC, Pavord ID et al. Mepolizumab treatment in patients with severe eosinophilic asthma. N Engl J Med. 2014; 371:1198-207. http://www.ncbi.nlm.nih.gov/pubmed/25199059?dopt=AbstractPlus
4. Bel EH, Wenzel SE, Thompson PJ et al. Oral glucocorticoid-sparing effect of mepolizumab in eosinophilic asthma. N Engl J Med. 2014; 371:1189-97. http://www.ncbi.nlm.nih.gov/pubmed/25199060?dopt=AbstractPlus
5. Katz LE, Gleich GJ, Hartley BF et al. Blood eosinophil count is a useful biomarker to identify patients with severe eosinophilic asthma. Ann Am Thorac Soc. 2014; 11:531-6. http://www.ncbi.nlm.nih.gov/pubmed/24606022?dopt=AbstractPlus
6. Walford HH, Doherty TA. Diagnosis and management of eosinophilic asthma: a US perspective. J Asthma Allergy. 2014; 7:53-65. http://www.ncbi.nlm.nih.gov/pubmed/24748808?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=3990389&blobtype=pdf
7. Pouliquen IJ, Kornmann O, Barton SV et al. Characterization of the relationship between dose and blood eosinophil response following subcutaneous administration of mepolizumab. Int J Clin Pharmacol Ther. 2015; 53:1015-27. http://www.ncbi.nlm.nih.gov/pubmed/26445140?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=4647865&blobtype=pdf
8. George L, Brightling CE. Eosinophilic airway inflammation: role in asthma and chronic obstructive pulmonary disease. Ther Adv Chronic Dis. 2016; 7:34-51. http://www.ncbi.nlm.nih.gov/pubmed/26770668?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=4707428&blobtype=pdf
9. Chung KF, Wenzel SE, Brozek JL et al. International ERS/ATS guidelines on definition, evaluation and treatment of severe asthma. Eur Respir J. 2014; 43:343-73. http://www.ncbi.nlm.nih.gov/pubmed/24337046?dopt=AbstractPlus
10. Haldar P, Brightling CE, Singapuri A et al. Outcomes after cessation of mepolizumab therapy in severe eosinophilic asthma: a 12-month follow-up analysis. J Allergy Clin Immunol. 2014; 133:921-3. http://www.ncbi.nlm.nih.gov/pubmed/24418480?dopt=AbstractPlus
11. Menzella F, Lusuardi M, Galeone C et al. Profile of anti-IL-5 mAb mepolizumab in the treatment of severe refractory asthma and hypereosinophilic diseases. J Asthma Allergy. 2015; 8:105-14. http://www.ncbi.nlm.nih.gov/pubmed/26504401?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=4603708&blobtype=pdf
12. GlaxoSmithKline. Nucala (mepolizumab) for injection, for subcutaneous use product monograph. Research Triangle Park, NC; 2015 Dec.
13. GlaxoSmithKline. Research Triangle Park, NC: Personal communication.
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