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Asparaginase Erwinia chrysanthemi
Các tên gọi khác (3) :
  • Asparaginase Erwinia chrysanthemi
  • Erwinia chrysanthemi
  • L-asparaginase (Erwinia)
enzymes
Thuốc Gốc
Biotech
CAS: 1349719-22-7
CTHH: C1546H2510N432O476S9
PTK: 140 kDa
Erwinaze (asparaginase Erwiniachryanthemi) contains an asparaginase specific enzyme derived from Erwiniachrysanthemi. L-asparaginase is a tetrameric enzyme consisting of four identical subunits, each having a molecular weight of about 35 kDa. The activity of Erwinaze is expressed in terms of International Units. It is an antineoplastic agent and was FDA approved in November 19, 2011.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C1546H2510N432O476S9
Phân tử khối
140 kDa
Cơ Chế Tác Dụng : Erwinaze (asparaginase Erwiniachryanthemi) contains an asparaginase specific enzyme derived from Erwiniachrysanthemi. L-asparaginase is a tetrameric enzyme consisting of four identical subunits, each having a molecular weight of about 35 kDa. The activity of Erwinaze is expressed in terms of International Units. It is an antineoplastic agent and was FDA approved in November 19, 2011. Asparaginase Erwinia chrysanthemi catalyzes the deamidation of asparagine to aspartic acid and ammonia, resulting in a reduction in circulating levels of asparagine in the plasma. The mechanism of action of Erwinaze is thought to be based on the inability of leukemic cells to synthesize asparagine due to lack of asparagine synthetase activity, resulting in cytotoxicity specific for leukemic cells that depend on an exogenous source of the amino acid asparagine for their protein metabolism and survival.
Dược Động Học :
▧ Absorption :
denaturation and peptidase digestion within GI tract
▧ Volume of Distribution :
5 L/m2. The partitioning of Erwinia L-asparaginase between lymph and blood shows that this enzyme, in contrast to the K coli derivative, does not penetrate the capillary endothelium well because negligible amounts are found in the lymph: hence, the drug seems to confine itself to the blood compartment of man.
▧ Route of Elimination :
possibly using reticuloendothelial system
▧ Half Life :
Elimination half-life, IM injection = 16 hours, follows first-order kinetics. Compared to E.coli-asparaginase, it has a lower half-life so higher and more frequent doses are necessary.
▧ Clearance :
3.4 mL/min/m2
Độc Tính : Because Erwinaze is injected intramuscularly, there is a higher chance of experiencing major skin reactions. Although the perceived benefit of Erwinia chryanthemi-derivied asparaginase is a lower incidence of hypersensitivity, there is still a chance that one may experience symptoms such as, but not limited to, anaphylaxis, pain, edema. Hypersensitivity to Erwinia chryanthemi-derivied asparaginase may be more likely if the patient had previously had an allergy to E.coli-derived asparaginase. Pancreatitis may also occur during the first few weeks of treatment with asparaginase. In addition, other severe adverse effects associated with Asparaginase Erwinia chrysanthemi are glucose intolerance as well as thrombosis and hemorrhage.
Chỉ Định : Asparaginase Erwinia chryanthemi is for the treatment of patients with acute lymphoblastic leukemia (ALL) that have developed a hypersensitivity to Escherichia coli-derivied asparaginase. It is a component of a multi-agent chemotherpeutic regimen for the treatment of the aforementioned disease and is considered second- or third- line treatment in European and American protocols.
Tương Tác Thuốc :
  • Dexamethasone Monitor therapy as asparaginase erwinia chrysanthemi may increase the serum concentration of dexamethasone due to a decrease of hepatic proteins necessary for dexamethasone metabolism.
Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Intramuscular - 10000 units (1 ea)
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08886
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02997
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/57902-249-05
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/X12746
Wikipedia
http://en.wikipedia.org/wiki/Asparaginase
RxList
http://www.rxlist.com/erwinaze-drug.htm
Drugs.com
http://www.drugs.com/monograph/asparaginase-erwinia-chrysanthemi.html
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