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Identification
Name Glatiramer Acetate
Accession Number DB05259 (APRD00999)
Type biotech
Groups approved
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 structure
Protein chemical formula C25H45N5O13
Protein average weight 623.6505
Sequences
Synonyms
  • COP-1
  • Copolymer-1
  • Copoylmer 1
  • glatiramer acetate
Brand names
  • Copaxone
Brand name mixtures Not Available
Categories
  • Immunosuppressive Agents
  • Adjuvants, Immunologic
CAS number 147245-92-9
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis.
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.
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
Toxicity Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia.
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Teva neuroscience inc
Packagers
Dosage forms
Form Route Strength
Powder, for solution Subcutaneous
Solution Subcutaneous
Prices
Unit description Cost Unit
Copaxone 20 mg/ml Kit 20 mg Solution, 1 Box = 30 Pre-Filled Syringes 3775.25 USD box
Copaxone 20 mg injection kit 2264.26 USD kit
Patents
Country Patent Number Approved Expires
United States 5981589 1994-05-24 2014-05-24
Canada 2191088 2004-09-28 2015-05-23
Properties
State liquid
Melting point Not Available
Experimental Properties Not Available
References
Synthesis Reference Not Available
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
Resource Link
PharmGKB PA449760 Link_out
Drug Product Database 2233014 Link_out
RxList http://www.rxlist.com/cgi/generic/glatiramer.htm Link_out
Drugs.com http://www.drugs.com/cdi/glatiramer.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Glatiramer_acetate Link_out
ATC Codes Not Available
AHFS Codes Not Available
PDB Entries Not Available
FDA label show (558 KB)
MSDS Not Available
Interactions
Drug Interactions
Drug Interaction
Food Interactions Not Available
Targets

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

Pharmacological action: unknown
Actions: binder
Organism class: human
UniProt ID: P04229 Link_out
Gene: HLA-DRB1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
Comments
Drug created on November 18, 2007 11:22 / Updated on September 29, 2010 14:35

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.