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Identification
NameGlatiramer Acetate
Accession NumberDB05259  (APRD00999)
TypeBiotech
GroupsApproved, Investigational
Description

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

Protein structureNo structure small
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Protein chemical formulaC254H422N70O72
Protein average weight7000.0 Da (range 5000-9000)
Sequences
>Example Glatiramer peptide
EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK
Download FASTA Format
Synonyms
COP-1
Copolymer-1
Copoylmer 1
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Copaxoneinjection, solution20 mg/mLsubcutaneousTeva Neuroscience, Inc.2008-04-28Not applicableUs
Copaxonesolution20 mgsubcutaneousTeva Canada Limited2002-05-01Not applicableCanada
Copaxonepowder for solution20 mgsubcutaneousTeva Pharmaceutical Industries Ltd1997-10-142011-04-28Canada
Copaxoneinjection, solution40 mg/mLsubcutaneousTeva Neuroscience, Inc.2014-01-29Not applicableUs
Teva-glatiramer Acetatesolution20 mgsubcutaneousTeva Canada LimitedNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Glatopainjection, solution20 mg/mLsubcutaneousSandoz Inc2015-06-18Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5M691HL4BO
CAS number147245-92-9
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis.
PharmacodynamicsGlatiramer 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 actionGlatiramer 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.
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AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hydrolyzed by proteases

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityAdverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionsubcutaneous40 mg/mL
Powder for solutionsubcutaneous20 mg
Solutionsubcutaneous20 mg
Injection, solutionsubcutaneous20 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)
CA2191088 No2004-09-282015-05-23Canada
US5981589 No1994-05-242014-05-24Us
US8232250 No2010-08-192030-08-19Us
US8399413 No2010-08-192030-08-19Us
US8969302 No2010-08-192030-08-19Us
US9155776 No2010-08-192030-08-19Us
Properties
StateLiquid
Experimental PropertiesNot Available
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. [PubMed:17920545 ]
  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. [PubMed:15371592 ]
  3. Francis DA: Glatiramer acetate (Copaxone). Int J Clin Pract. 2001 Jul-Aug;55(6):394-8. [PubMed:11501229 ]
  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. [PubMed:9548401 ]
External Links
ATC CodesL03AX13
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (558 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Glatiramer Acetate.
LeflunomideThe risk or severity of adverse effects can be increased when Glatiramer Acetate is combined with Leflunomide.
NatalizumabThe risk or severity of adverse effects can be increased when Glatiramer Acetate is combined with Natalizumab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Glatiramer Acetate.
RoflumilastRoflumilast may increase the immunosuppressive activities of Glatiramer Acetate.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Glatiramer Acetate.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Glatiramer Acetate.
TofacitinibGlatiramer Acetate may increase the immunosuppressive activities of Tofacitinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Glatiramer Acetate.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Virus receptor activity
Specific Function:
Binds peptides derived from antigens that access the endocytic route of antigen presenting cells (APC) and presents them on the cell surface for recognition by the CD4 T-cells. The peptide binding cleft accommodates peptides of 10-30 residues. The peptides presented by MHC class II molecules are generated mostly by degradation of proteins that access the endocytic route; where they are processe...
Gene Name:
HLA-DRB1
Uniprot ID:
P04229
Molecular Weight:
29913.945 Da
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. [PubMed:15371592 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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Drug created on November 18, 2007 11:22 / Updated on August 24, 2016 01:51