Glatiramer

Identification

Summary

Glatiramer is an immunomodulator used to reduce the frequency of relapses in Multiple Sclerosis (MS).

Brand Names
Copaxone, Glatect, Glatopa
Generic Name
Glatiramer
DrugBank Accession Number
DB05259
Background

Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Peptides
Protein Chemical Formula
C254H422N70O72
Protein Average Weight
7000.0 Da (range 5000-9000)
Sequences
>Example Glatiramer peptide
EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK
Download FASTA Format
Synonyms
  • (T,G)-A-L
  • COP 1
  • COP-1
  • Copolymer I (synthetic peptide)
  • Copolymer-1

Pharmacology

Indication

For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact.

Mechanism of action

Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells.

TargetActionsOrganism
UHLA class II histocompatibility antigen, DRB1-1 beta chain
binder
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hydrolyzed by proteases

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Glatiramer.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Glatiramer.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Glatiramer.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Glatiramer.
AlefaceptThe risk or severity of adverse effects can be increased when Alefacept is combined with Glatiramer.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Glatiramer.
AltretamineThe risk or severity of adverse effects can be increased when Altretamine is combined with Glatiramer.
AmsacrineThe risk or severity of adverse effects can be increased when Amsacrine is combined with Glatiramer.
AnakinraThe risk or severity of adverse effects can be increased when Anakinra is combined with Glatiramer.
Anthrax immune globulin humanThe therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Glatiramer.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Glatiramer acetate5M691HL4BO147245-92-9Not applicable
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CopaxonePowder, for solution20 mg / vialSubcutaneousTeva Pharmaceutical Industries1997-10-142011-04-28Canada flag
CopaxoneInjection20 mg/1mLSubcutaneousSanofi Aventis2002-04-222010-01-31US flag
CopaxoneSolution40 mg / mLSubcutaneousTEVA Canada Limited2016-08-26Not applicableCanada flag
CopaxoneInjection, solution40 mg/1mLSubcutaneousTeva Neuroscience, Inc.2014-01-29Not applicableUS flag
CopaxoneSolution40 mg / mLSubcutaneousTEVA Canada LimitedNot applicableNot applicableCanada flag
CopaxoneSolution20 mg / mLSubcutaneousTEVA Canada Limited2002-05-01Not applicableCanada flag
CopaxoneInjection, solution20 mg/1mLSubcutaneousTeva Neuroscience, Inc.2008-04-28Not applicableUS flag
GlatectSolution20 mg / mLSubcutaneousPharmascience Inc2017-08-21Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Glatiramer AcetateInjection, solution20 mg/1mLSubcutaneousMylan Pharmaceuticals Inc.2017-10-04Not applicableUS flag
Glatiramer AcetateInjection, solution40 mg/1mLSubcutaneousMylan Pharmaceuticals Inc.2017-10-04Not applicableUS flag
GlatopaInjection, solution20 mg/1mLSubcutaneousSandoz Inc2015-06-18Not applicableUS flag
GlatopaInjection, solution40 mg/1mLSubcutaneousSandoz Inc2018-02-12Not applicableUS flag
Teva-glatiramer AcetateSolution40 mg / mLSubcutaneousTEVA Canada LimitedNot applicableNot applicableCanada flag
Teva-glatiramer AcetateSolution20 mg / mLSubcutaneousTEVA Canada LimitedNot applicableNot applicableCanada flag

Categories

ATC Codes
L03AX13 — Glatiramer acetate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
U782C039QP
CAS number
28704-27-0

References

Synthesis Reference

Tsung-Yu Hsiao, Meng-Fen Ho, "Synthesis of Glatiramer Acetate." U.S. Patent US20100036092, issued February 11, 2010.

US20100036092
General References
  1. Weber MS, Hohlfeld R, Zamvil SS: Mechanism of action of glatiramer acetate in treatment of multiple sclerosis. Neurotherapeutics. 2007 Oct;4(4):647-53. [Article]
  2. Arnon R, Aharoni R: Mechanism of action of glatiramer acetate in multiple sclerosis and its potential for the development of new applications. Proc Natl Acad Sci U S A. 2004 Oct 5;101 Suppl 2:14593-8. Epub 2004 Sep 15. [Article]
  3. Francis DA: Glatiramer acetate (Copaxone). Int J Clin Pract. 2001 Jul-Aug;55(6):394-8. [Article]
  4. Li Q, Milo R, Panitch H, Swoveland P, Bever CT Jr: Glatiramer acetate blocks the activation of THP-1 cells by interferon-gamma. Eur J Pharmacol. 1998 Jan 26;342(2-3):303-10. [Article]
PubChem Substance
46505299
RxNav
214582
ChEMBL
CHEMBL1201507
Therapeutic Targets Database
DAP001315
PharmGKB
PA449760
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Glatiramer_acetate
AHFS Codes
  • 92:20.00 — Immunomodulatory Agents
FDA label
Download (558 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionDisseminated Sclerosis1
4CompletedTreatmentDisseminated Sclerosis3
4CompletedTreatmentRelapsing Forms of Multiple Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)4
4Not Yet RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Relapsing Multiple Sclerosis (RMS)1
4RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedPreventionRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4Unknown StatusTreatmentDiabetic Retinopathy (DR)1
4Unknown StatusTreatmentDisseminated Sclerosis2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Baxter International Inc.
  • Ben Venue Laboratories Inc.
  • Sanofi-Aventis Inc.
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
SolutionSubcutaneous20 mg
Injection, solutionParenteral
InjectionSubcutaneous20 mg/1mL
Injection, powder, for solutionSubcutaneous
Injection, solutionSubcutaneous20 mg/1mL
Injection, solutionSubcutaneous40 mg/1mL
Powder, for solutionSubcutaneous20 mg / vial
SolutionSubcutaneous20 mg / mL
SolutionSubcutaneous40 mg / mL
SolutionSubcutaneous36 mg
Injection, solutionSubcutaneous
SolutionSubcutaneous40 mg
Injection, solution
Injection, solution20 mg/ml
Injection, solution40 mg/ml
Prices
Unit descriptionCostUnit
Copaxone 20 mg/ml Kit 20 mg Solution, 1 Box = 30 Pre-Filled Syringes3775.25USD box
Copaxone 20 mg injection kit2264.26USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5981589No1999-11-092014-05-24US flag
CA2191088No2004-09-282015-05-23Canada flag
US8232250No2012-07-312030-08-19US flag
US8399413No2013-03-192030-08-19US flag
US8969302No2015-03-032030-08-19US flag
US9155776No2015-10-132030-08-19US flag
US9402874No2016-08-022030-08-19US flag

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets
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1. HLA class II histocompatibility antigen, DRB1-1 beta chain
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
References
  1. Arnon R, Aharoni R: Mechanism of action of glatiramer acetate in multiple sclerosis and its potential for the development of new applications. Proc Natl Acad Sci U S A. 2004 Oct 5;101 Suppl 2:14593-8. Epub 2004 Sep 15. [Article]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created on November 18, 2007 18:22 / Updated on June 22, 2021 09:25