Class: Immunomodulatory Agents
- Immunomodulatory Agents
Chemical Name: l-Glutamic acid polymer with l-alanine, l-lysine, and l-tyrosine, acetate
Molecular Formula: C5H9NO4 • C3H7-5H9NO4 • C3H7NO2 • C6H14N2O2 • C9H11NO3)x • xC2H4O2)
CAS Number: 147245-92-9
Brands: Copaxone, Glatopa
Medically reviewed by Drugs.com. Last updated on Nov 4, 2019.
Uses for Glatiramer Acetate
Multiple Sclerosis (MS)
Glatiramer acetate is one of several disease-modifying therapies used in the management of RRMS.76 77 Although not curative, these therapies have all been shown to modify several measures of disease activity, including relapse rates, new or enhancing magnetic resonance imaging (MRI) lesions, and disability progression.76 78
The American Academy of Neurology (AAN) recommends that disease-modifying therapy be offered to patients with RRMS who have had recent relapses and/or MRI activity.76 Clinicians should consider adverse effects, tolerability, method of administration, safety, efficacy, and cost of the drugs in addition to patient preferences when selecting an appropriate therapy.76 77
Clinical experience suggests that efficacy of glatiramer acetate is generally similar to that of interferon beta.24 25 76 Efficacy of glatiramer acetate compared with other disease-modifying therapies (e.g., fingolimod, mitoxantrone, natalizumab) not fully evaluated to date.6 24 26
Glatiramer Acetate Dosage and Administration
Administer only by sub-Q injection; do not administer IV.1
Administer initial self-administered dose under supervision of a qualified clinician.1
Several preparations of glatiramer acetate are commercially available (e.g., Copaxone, Glatopa and other generic preparations), and there are 2 available dosage strengths.1 28 29 76 The 20-mg/mL injection is administered once daily and the 40-mg/mL injection is administered 3 times a week; the 2 dosage strengths are not interchangeable.1
Commercially available prefilled syringes intended for single use only; discard unused portion.1
To minimize risk of localized lipoatrophy and skin necrosis, follow proper injection technique and rotate injection areas and sites with each injection.1 22 (See Lipoatrophy and Skin Necrosis under Cautions.)
Available as glatiramer acetate; dosage expressed in terms of the salt.1
If using the 40-mg/mL injection, recommended dosage is 40 mg 3 times a week (administer injections at least 48 hours apart).1
Cautions for Glatiramer Acetate
Known hypersensitivity to glatiramer acetate or mannitol.1
Injection site hypersensitivity, allergic reactions, and anaphylactic or anaphylactoid reactions reported,1 10 18 23 27 including rare cases of anaphylaxis accompanied by anti-glatiramer IgE antibodies.10 18 Some reactions developed from one to several months or more after initiating therapy.7 27
Acute injection reactions reported in some patients immediately after sub-Q injection.1 Symptoms, which are generally transient and self-limited and do not require treatment,1 include flushing,1 2 6 7 chest pain1 2 6 or tightness,6 7 8 palpitations,1 2 5 6 7 8 anxiety,1 2 5 6 7 8 dyspnea,1 2 5 6 7 8 constriction of the throat,1 tachycardia,1 and urticaria.1 23
Reactions generally occur several months after initiation of therapy (although may occur earlier); individual patients may experience one or several episodes of these symptoms.1 6 7 During the postmarketing period, some patients with similar symptoms reportedly received emergency medical care.1
Transient chest pain reported, generally >1 month after initiation of therapy.1 Some episodes occurred as part of immediate post-injection reactions, but many did not.1 Episodes generally last only a few minutes, often are not associated with other symptoms, and do not appear to produce clinically important sequelae.1 Some patients experience >1 such episode.1
Lipoatrophy and Skin Necrosis
Localized lipoatrophy (i.e., loss of subcutaneous fat) and, rarely, skin necrosis at the injection site reported.1 21 22 23 Lipoatrophy may occur at various times after treatment initiation, sometimes after several months and is thought to be permanent.1 22 No known treatment for lipoatrophy.1 22
Advise patients to follow proper injection technique and rotate injection areas and sites daily to minimize risk of these events.1
Potential Effects on Immune Response
Possible modification of immune response and interference with useful immune function.1
Possible interference with the recognition of foreign antigens, which may undermine the body’s tumor surveillance ability and defenses against infection.1
Possibility of adverse effects resulting from continued alteration of cellular immunity associated with chronic administration of the drug.1
Animal studies suggest that immune complexes are deposited in renal glomeruli.1
Safety and efficacy not established in pediatric patients <18 years of age.1
Not studied in geriatric patients.1
Common Adverse Effects
20-mg/mL injection: Injection site reactions1 2 5 23 (e.g., pain,1 2 erythema,1 2 23 inflammation,1 2 pruritus,1 2 23 mass,1 2 edema,1 hypersensitivity,1 fibrosis,1 atrophy or lipoatrophy,1 22 necrosis),23 vasodilatation,1 rash,1 23 dyspnea,1 chest pain.1
40-mg/mL injection: Injection site reactions.1
Interactions for Glatiramer Acetate
Interactions with other drugs not fully evaluated to date.1
No clinically important interactions reported in clinical trials between glatiramer and drugs commonly used in multiple sclerosis, including concurrent corticosteroid therapy for up to 28 days.1 Not formally evaluated in combination with interferon beta.1 6
Glatiramer Acetate Pharmacokinetics
Advice to Patients
Importance of reading the manufacturer’s patient information prior to beginning glatiramer acetate therapy and each time prescription is refilled.1
Importance of clinicians instructing patients and/or caregivers in proper injection techniques (including use of aseptic technique) and about avoiding reuse of syringes and needles and proper disposal of such equipment.1
Risk of post-injection reaction.1 Importance of advising patients that glatiramer acetate may cause various symptoms after injection, including flushing, chest pain, palpitations, anxiety, dyspnea, throat constriction, and urticaria.1 Importance of informing patients that these symptoms usually are transient and self-limited and do not require specific treatment.1 However, patients should be advised to contact their clinician immediately if any serious reactions (e.g., flushing, chest pain, tachycardia, anxiety, breathing difficulties or tightness in the throat, swelling, rash, hives, itching) occur immediately after injection.1 Patients also should be informed that such reactions may occur early or begin several months after initiation of treatment, and that they may experience one or several episodes of these symptoms.1
Importance of advising patients that they may experience chest pain either as part of a post-injection reaction or in isolation.1 Patients should be informed that the pain should be transient (usually lasting only for a few minutes).1 Some patients may experience more than one such episode, usually beginning at least one month after beginning treatment.1 Advise patients to seek medical attention if they experience chest pain of unusual duration or intensity.1
Importance of informing patients of the recommended storage instructions for glatiramer acetate (see Storage under Stability).1 Importance of advising patients not to expose the drug to higher temperatures, freezing temperatures, or to intense light.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of patient informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1
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.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Injection, for subcutaneous use
20 mg/1 mL*
Copaxone (available as 1-mL prefilled syringe)
Glatiramer Acetate Injection
Glatopa (available as 1-mL prefilled syringe)
40 mg/1 mL*
Copaxone (available as 1-mL prefilled syringe)
Glatopa (available as 1-mL prefilled syringe)
AHFS DI Essentials™. © Copyright 2019, Selected Revisions November 4, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Teva Neuroscience, Inc. Copaxone (glatiramer acetate) injection prescribing information. Overland Park, KS; 2018 Jan.
2. Johnson KP, Brooks BR, Cohen JA et al. Copolymer 1 reduces relapse rate and improves disability in relapsing-remitting multiple sclerosis: results of a phase III multicenter, double-blind, placebo-controlled trial. Neurology. 1995; 45:1268-76. http://www.ncbi.nlm.nih.gov/pubmed/7617181?dopt=AbstractPlus
3. Johnson KP, Brooks BR, Cohen JA et al. Extended use of glatiramer acetate (Copaxone) is well tolerated and maintains its clinical effect on multiple sclerosis relapse rate and degree of disability. Neurology. 1998; 50:701-8. http://www.ncbi.nlm.nih.gov/pubmed/9521260?dopt=AbstractPlus
4. Bornstein MB, Miller A, Slagle S et al. A pilot trial of Cop 1 in exacerbating-remitting multiple sclerosis. N Engl J Med. 1987; 317:408-14. http://www.ncbi.nlm.nih.gov/pubmed/3302705?dopt=AbstractPlus
5. Comi G, Filippi M, Wolinsky JS et al. European/Canadian multicenter, double-blind, randomized, placebo-controlled study of the effects of glatiramer acetate on magnetic resonance imaging-measured disease activity and burden in patients with relapsing multiple sclerosis. Ann Neurol. 2001; 49:290-7. http://www.ncbi.nlm.nih.gov/pubmed/11261502?dopt=AbstractPlus
6. Simpson D, Noble S, Perry C. Glatiramer acetate: a review of its use in relapsing-remitting multiple sclerosis. CNS Drugs. 2002; 16:825-50. http://www.ncbi.nlm.nih.gov/pubmed/12421116?dopt=AbstractPlus
7. Calabresi PA. Considerations in the treatment of relapsing-remitting multiple sclerosis. Neurology. 2002; 58(Suppl 4):S10-S22.
8. Miller AE. Glatiramer acetate in the treatment of multiple sclerosis. Neurol Clin. 2005; 23:215-31. http://www.ncbi.nlm.nih.gov/pubmed/15661095?dopt=AbstractPlus
9. Goodin DS, Frohman EM, Garmany GP Jr et al. Disease modifying therapies in multiple sclerosis: report of the therapeutics and technology assessment subcommittee of the American Academy of Neurology and the MS council for clinical practice guidelines. Neurology. 2002; 58: 169-178. http://www.ncbi.nlm.nih.gov/pubmed/11805241?dopt=AbstractPlus
10. Rauschka H, Farina C, Sator P et al. Severe anaphylactic reaction to glatiramer acetate with specific IgE. Neurology. 2005; 64:1481. http://www.ncbi.nlm.nih.gov/pubmed/15851756?dopt=AbstractPlus
11. Ge Y, Grossman RI, Udupa JK et al. Glatiramer acetate (Copaxone) treatment in relapsing-remitting MS. Neurology. 2000; 54:813-7. http://www.ncbi.nlm.nih.gov/pubmed/10690968?dopt=AbstractPlus
12. Johnson KP, Ford CC, LIsak RP et al. Neurologic consequence of delaying glatiramer acetate therapy for multiple sclerosis: 8-year data. Acta Neurol Scand. 2005; 111:42-7. http://www.ncbi.nlm.nih.gov/pubmed/15595937?dopt=AbstractPlus
13. Rizvi SA, Agius MA. Current approved options for treating patients with multiple sclerosis. Neurology. 2004; 63(Suppl 6):S8-S14. http://www.ncbi.nlm.nih.gov/pubmed/15623672?dopt=AbstractPlus
15. Mezzapesa DM, Rovaris M, Filippi M. Glatiramer acetate in multiple sclerosis. Expert Rev Neurotherapeutics. 2005; 5:451-8.
16. Boneschi FM, Rovaris M, Johnson KP et al. Effects of glatiramer acetate on relapse rate and accumulated disability in multiple sclerosis: meta-analysis of three double-blind, randomized, placebo-controlled clinical trials. Multiple Sclerosis. 2003; 9:349-55. http://www.ncbi.nlm.nih.gov/pubmed/12926839?dopt=AbstractPlus
17. Johnson KP, Brooks BR, Ford CC et al. Glatiramer acetate (Copaxone): comparison of continuous versus delayed therapy in a six-year organized multiple sclerosis trial. Multiple Sclerosis. 2003; 9:585-91. http://www.ncbi.nlm.nih.gov/pubmed/14664471?dopt=AbstractPlus
18. Teva Neuroscience, Overland Park, KS. Personal communication.
19. Johnson KP, Panitch HS, Ford CC et al. Long-term slowing of disability progression in patients receiving continuous glatiramer acetate compared with those withdrawing from therapy: 10 year results from an ongoing trial. Neurology. 2004; 62(7 Suppl 5):A180.
20. Teitelbaum D, Brenner T, Abramsky O et al. Antibodies to glatiramer acetate do not interfere with its biological functions and therapeutic efficacy. Mult Scler. 2003; 9:592-9. http://www.ncbi.nlm.nih.gov/pubmed/14664472?dopt=AbstractPlus
21. Feldmann R, Schierl M, Rauschka H et al. Necrotizing skin lesions with involvement of muscle tissue after subcutaneous injection of glatiramer acetate. Eur J Dermatol. 2009 Jul-Aug; 19:385.
22. Edgar CM, Brunet DG, Fenton P et al. Lipoatrophy in patients with multiple sclerosis on glatiramer acetate. Can J Neurol Sci. 2004; 31:58-63. http://www.ncbi.nlm.nih.gov/pubmed/15038472?dopt=AbstractPlus
23. Comi G, Martinelli V, Rodegher M et al. Effect of glatiramer acetate on conversion to clinically definite multiple sclerosis in patients with clinically isolated syndrome (PreCISe study): a randomised, double-blind, placebo-controlled trial. Lancet. 2009; 374:1503-11. http://www.ncbi.nlm.nih.gov/pubmed/19815268?dopt=AbstractPlus
24. Hartung HP, Montalban X, Sorensen PS et al. Principles of a new treatment algorithm in multiple sclerosis. Expert Rev Neurother. 2011; 11:351-62. http://www.ncbi.nlm.nih.gov/pubmed/21375441?dopt=AbstractPlus
25. Carter NJ, Keating GM. Glatiramer acetate: a review of its use in relapsing-remitting multiple sclerosis and in delaying the onset of clinically definite multiple sclerosis. Drugs. 2010; 70:1545-77. http://www.ncbi.nlm.nih.gov/pubmed/20687620?dopt=AbstractPlus
26. Roskell NS, Zimovetz EA, Rykroft CE et al. Annualized relapse rate of first-line treatments for multiple sclerosis: a meta-analysis, including direct comparisons versus fingolimod. Cur Med Res Opinion. 2012; 28:767-80.
27. Baumgartner A, Stich O, Rauer S et al. Anaphylactic reaction after injection of glatiramer acetate (Copaxone) in patients with relapsing-remitting multiple sclerosis. Eur Neurology. 2011; 66:368-70.
28. Mylan. Glatiramer acetate injection prescribing information. Morgantown, WS; 2018 Jan.
29. Sandoz. Glatopa (glatiramer acetate injection) prescribing information. Princeton, NJ; 2018 Jan.
76. Rae-Grant A, Day GS, Marrie RA et al. Practice guideline recommendations summary: Disease-modifying therapies for adults with multiple sclerosis: Report of the Guideline Development, Dissemination, and Implementation Subcommittee of the American Academy of Neurology. Neurology. 2018; 90:777-788. http://www.ncbi.nlm.nih.gov/pubmed/29686116?dopt=AbstractPlus
77. Multiple Sclerosis Coalition. The use of disease-modifying therapies in multiple sclerosis: principles and current evidence summary. Available from National MS Society website. http://www.nationalmssociety.org/getmedia/1e64b96c-9e55-400e-9a64-0cdf5e2d60fe/summaryDMTpaper_-final
78. National MS Society. Disease-modifying therapies for MS. Available from National MS Society website. http://stage.nationalmssociety.org/NationalMSSociety/media/MSNationalFiles/Brochures/Brochure-The-MS-Disease-Modifying-Medications.pdf
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