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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
Protein chemical formulaC25H45N5O13
Protein average weight623.6505
Sequences
Synonyms
SynonymLanguageCode
COP-1Not AvailableNot Available
Copolymer-1Not AvailableNot Available
Copoylmer 1Not AvailableNot Available
SaltsNot Available
Brand names
NameCompany
CopaxoneNot Available
Brand mixturesNot Available
Categories
CAS number147245-92-9
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot 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.
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
Manufacturers
  • Teva neuroscience inc
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionSubcutaneous
SolutionSubcutaneous
Prices
Unit descriptionCostUnit
Copaxone 20 mg/ml Kit 20 mg Solution, 1 Box = 30 Pre-Filled Syringes3775.25USDbox
Copaxone 20 mg injection kit2264.26USDkit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States59815891994-05-242014-05-24
Canada21910882004-09-282015-05-23
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 Reference
  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
  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
  3. Francis DA: Glatiramer acetate (Copaxone). Int J Clin Pract. 2001 Jul-Aug;55(6):394-8. Pubmed
  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
External Links
ResourceLink
PharmGKBPA449760
Drug Product Database2233014
RxListhttp://www.rxlist.com/cgi/generic/glatiramer.htm
Drugs.comhttp://www.drugs.com/cdi/glatiramer.html
WikipediaGlatiramer_acetate
ATC CodesL03AX13
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelshow(558 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
Rilonaceptresults in increased immunosuppressive effects; increases the risk of infection.
Food InteractionsNot Available

Targets

1. HLA class II histocompatibility antigen, DRB1-1 beta chain

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
HLA class II histocompatibility antigen, DRB1-1 beta chain P04229 Details

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
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

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Drug created on November 18, 2007 11:22 / Updated on September 13, 2013 11:14