Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Độ tan chảy
61 °C (FAB fragment), 71 °C (whole mAb)
Dược Lực Học :
Used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 25%-30% of primary breast cancers.Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumorcells that overexpress HER2. It is a mediator of antibody dependent cellular cytotoxicity, in that the binding of the antibody to HER2 overexpressing cells leads to preferential cell death.
Cơ Chế Tác Dụng :
A recombinant IgG1 kappa, humanized monoclonal antibody that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein. Produced in CHO cell culture.*
Trastuzumab binds to the HER2 (or c-erbB2) proto-oncogene, an EGF receptor-like protein found on 20-30% of breast cancer cells. The binding leads to antibody mediated (complement mediated) killing of the HER2 positive cells.
Dược Động Học :
▧ Absorption :
Peak and trough plasma concentrations at steady state (between weeks 16 and 32) approximately 123 and 79 mcg/mL, respectively.
▧ Volume of Distribution :
* 44 mL/kg
▧ Metabolism :
Most likely removed by opsonization via the reticuloendothelial system.
▧ Half Life :
average 28.5 days. Pharmacokinetics are nonlinear; increased doses are associated with increased mean half-life and decreased clearance.
▧ Clearance :
Elimination may involve clearance of IgG through the reticuloendothelial system.
Độc Tính :
Administration of trastuzumab can result in ventricular dysfunction and congestive heart failure. Risk of cardiotocity is especially elevated in patients recieving concurrent anthracycline or cyclophosphamide therapy.
Chỉ Định :
For treatment of early stage HER2-positive breast cancer, or metastatic breast cancer that substantially overexpress HER2.
Liều Lượng & Cách Dùng :
Injection, powder, lyophilized, for solution - Intravenous
Tài Liệu Tham Khảo Thêm
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