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DB05259 - Glatiramer Acetate


Identification
Name Glatiramer Acetate
Accession Number DB05259 (APRD00999)
Type biotech
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
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 623.6505
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis.
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
Protein binding Not Available
Biotransformation Hydrolyzed by proteases
Route of elimination 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
Interactions
Drug Interactions
Drug Mechanism of interaction
Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
Food Interactions Not Available

Targets


HLA class II histocompatibility antigen, DRB1-1 beta chain
Name HLA class II histocompatibility antigen, DRB1-1 beta chain
Gene Name HLA-DRB1
Pharmacological action unknown
Actions binder
References
  • 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
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 2

Predictions


Id Partner name Gene Name Score
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