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| Primary information |
|---|
| ID | 12101 |
| Therapeutic ID | Th1285 |
| Protein Name | Glatiramer |
| Sequence | >Th1285_Glatiramer
EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK
|
| Molecular Weight | 7000 |
| Chemical Formula | C254H422N70O72 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | NA |
| 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. |
| Indication/Disease | 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. |
| Toxicity | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. |
| Metabolism | Hydrolyzed by proteases |
| Absorption | NA |
| NA |
| Clearance | NA |
| Categories | T-Lymphocytes, Helper-Inducer, immunology |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | HLA class II histocompatibility antigen, DRB1-1 beta chain |
| Brand Name | Glatopa |
| Company | Sandoz Inc |
| Brand Description | Sandoz Inc |
| Prescribed For | Subcutaneous |
| Chemical Name | 40 mg/1mL |
| Formulation | Glatopa is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. |
| Physical Appearance | injection site reactions, skin redness, rash, hives, lightheadedness, flushing, palpitations, anxiety, indigestion, throat constriction, and chest pain |
| Route of Administration | Glatopa is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Glatopa will not cure MS, but it can make relapses occur less often. Glatopa may also be used for purposes not listed... |
| Recommended Dosage | Glatopa is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |