Tìm theo
Pegaspargase
Các tên gọi khác (2) :
  • L-asparagine amidohydrolase
  • Putative L-asparaginase precursor
Thuốc điều trị ung thư
Thuốc Gốc
Biotech
CAS: 130167-69-0
ATC: L01XX24
ĐG : Ben Venue Laboratories Inc. , http://www.benvenue.com
CTHH: C1377H2208N382O442S17
PTK: 31731.9000
Pegylated L-asparagine amidohydrolase from E. coli. Pegylation substantially (by a factor of 4) extends the protein half life.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C1377H2208N382O442S17
Phân tử khối
31731.9000
Độ kỵ nước
0.059
Điểm đẳng điện tích
4.67
Dược Lực Học : In a significant number of patients with acute leukemia, the malignant cells are dependent on an exogenous source of asparagine for survival. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase. Oncaspar exploits a metabolic defect in asparagine synthesis of some malignant cells.
Cơ Chế Tác Dụng : Pegylated L-asparagine amidohydrolase from E. coli. Pegylation substantially (by a factor of 4) extends the protein half life. Pegaspargase, more effective than asparaginase, converts asparagine to aspartic acid and ammonia. It facilitates production of oxaloacetate which is needed for general cellular metabolism. Some malignant cells lose the ability to produce asparagine and so the loss of exogenous sources of asparagine leads to cell death.
Dược Động Học :
▧ Absorption :
Onset of Asparagine depletion by IM is within 4 days Time to peak: IM: 3 to 4 days
▧ Volume of Distribution :
IV: Adults (asparaginase naive): 2.4 L/m2 Distributes into CSF (reportedly reducing CSF asparagine concentrations to a similar extent as asparaginase
▧ Half Life :
IM: ~6 days; half-life decreased to ~3 days (range: 1.4 to 5 days) in patients with previous hypersensitivity to native L-asparaginase; IV: Adults (asparaginase naive): 7 days
Độc Tính : Adverse effects that occur more than 10% of the time include hepatotoxicity as it is known to increase serum transaminases (ALT, AST). Also known to induce hypersensitivity reactions including anaphylaxis, erythema and bronchospasm.
Chỉ Định : For treatment of acute lymphoblastic leukemia
Tương Tác Thuốc :
  • Denosumab Monitor therapy due to increased immunosuppressive effect and risk of infections.
  • Leflunomide Immunosuppressants can increase toxic effects of leflunomide such as hematologic toxicity.
  • Natalizumab Avoid combination because of increased immunosuppressants and risk of infections.
  • Pimecrolimus Avoid combination because pimecrolimus enhances the adverse effects of immunosuppressants.
  • Roflumilast Consider therapy modification because pegaspargase enhances the immunosuppressive effect of roflumilast.
  • Sipuleucel-T Monitor therapy because pegaspargase may diminish therapeutic effect of sipuleucel-T.
  • Tacrolimus Tacrolimus enhances adverse effects of pegaspargase therefore the combination should be avoided.
  • Tofacitinib Avoid combination due to enhanced immunosuppressive effect of tofacitinib.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Injection, solution - Intramuscular
Injection, solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Enzon Inc
    Sản phẩm biệt dược : Oncaspar
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00059
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/57665-002-02
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/U00096
PharmGKB
http://www.pharmgkb.org/drug/PA164760860
Wikipedia
http://en.wikipedia.org/wiki/Pegaspargase
RxList
http://www.rxlist.com/cgi/generic2/pegaspargase.htm
Drugs.com
http://www.drugs.com/cdi/pegaspargase.html
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