| Primary information |
|---|
| ThPP ID | Th1113 |
| Therapeutic Peptide/Protein Name | Glatiramer acetate |
| Sequence | EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYK view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 5000-9000 |
| Chemical Formula | C254H422N70O72 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Glatiramer acetate comprises 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, known to reduce the 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 | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | N.A. |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Copaxone |
| Company | Teva Pharmaceutical Industries |
| Brand Discription | N.A. |
| Prescribed for | Glatiramer acetate, the active ingredient of COPAXONE, 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. Glatiramer acetate is identified by specific antibodies. Chemically, glatiramer acetate is designated L-glutamic acid polymer with L-alanine, L-lysine and L-tyrosine, acetate (salt). |
| Chemical Name | N.A. |
| Formulation | Each 1 mL of COPAXONE solution contains 20 mg or 40 mg of glatiramer acetate and the following inactive ingredient: 40 mg of mannitol. The pH of the solutions is approximately 5.5 to 7.0. The biological activity of glatiramer acetate is determined by its ability to block the induction of experimental autoimmune encephalomyelitis (EAE) in mice. |
| Physcial Appearnce | Clear, colorless to slightly yellow, sterile, nonpyrogenic solution |
| Route of Administration | Subcutaneous |
| Recommended Dosage | COPAXONE is for subcutaneous use only. Do not administer intravenously. The dosing schedule depends on the product strength that is selected. The recommended doses are: COPAXONE 20 mg per mL: administer once per day or COPAXONE 40 mg per mL: administer three times per week and at least 48 hours apart. COPAXONE 20 mg per mL and COPAXONE 40 mg per mL are not interchangeable. |
| Contraindication | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. |
| Side Effects | most commonly associated with discontinuation were: injection site reactions, dyspnea, urticaria, vasodilatation, and hypersensitivity. The most common adverse reactions were: injection site reactions, vasodilatation, rash, dyspnea, and chest pain. |
| Useful Link | http://www.rxlist.com/copaxone-drug/side-effects-interactions.htm https://www.copaxone.com/ http://en.wikipedia.org/wiki/Glatiramer_acetate http://www.drugs.com/copaxone.html |
| PubMed ID | 17920545, 15371592, 11501229, 9548401 |
| 3-D Structure | N.A. |