Tìm theo
Glatiramer Acetate
Các tên gọi khác (3) :
  • COP-1
  • Copolymer-1
  • Copoylmer 1
Thuốc giảm miễn dịch
Thuốc Gốc
Biotech
CAS: 147245-92-9
ATC: L03AX13
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C254H422N70O72
PTK: 5000-9000
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
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C254H422N70O72
Phân tử khối
5000-9000
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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 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.
Dược Động Học :

▧ Metabolism :
Hydrolyzed by proteases
Độc Tính : Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia.
Chỉ Định : For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis.
Tương Tác Thuốc :
  • Denosumab Monitor therapy due to enhanced immunosuppressive effects and the risk of infections.
  • Leflunomide Consider therapy modification due to enhanced adverse effects of leflunomide including hematologic toxicity.
  • Natalizumab Avoid combination due to enhanced adverse effects of natalizumab including the risk of infections.
  • Pimecrolimus Avoid combination due to enhanced immunosuppressive effects.
  • Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
  • Roflumilast Consider therapy modification due to enhanced immunosuppressive effects.
  • Sipuleucel-T Monitor therapy due to decreased therapeutic effect of sipuleucel-T.
  • Tacrolimus Avoid combination due to enhanced adverse effects of immunosuppressants.
  • Tofacitinib Avoid combination due to enhanced immunosuppressive effect of tofacitinib.
  • Trastuzumab Monitor therapy due to enhanced neutropenic effects of immunosuppressants.
Liều Lượng & Cách Dùng : Powder, for solution - Subcutaneous
Solution - Subcutaneous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Copaxone
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05259
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0088-1153-30
PharmGKB
http://www.pharmgkb.org/drug/PA449760
Wikipedia
http://en.wikipedia.org/wiki/Glatiramer_acetate
RxList
http://www.rxlist.com/cgi/generic/glatiramer.htm
Drugs.com
http://www.drugs.com/cdi/glatiramer.html
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