Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
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 :
Monitor therapy due to increased immunosuppressive effect and risk of infections.
Immunosuppressants can increase toxic effects of leflunomide such as hematologic toxicity.
Avoid combination because of increased immunosuppressants and risk of infections.
Avoid combination because pimecrolimus enhances the adverse effects of immunosuppressants.
Consider therapy modification because pegaspargase enhances the immunosuppressive effect of roflumilast.
Monitor therapy because pegaspargase may diminish therapeutic effect of sipuleucel-T.
Tacrolimus enhances adverse effects of pegaspargase therefore the combination should be avoided.
Avoid combination due to enhanced immunosuppressive effect of tofacitinib.
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
Tài Liệu Tham Khảo Thêm
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