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药品详细

Trastuzumab(曲妥珠单抗)

化学结构式图
没有图片
中文名
曲妥珠单抗
英文名
Trastuzumab
分子式
Not Available
化学名
分子量
CAS号
180288-69-1
ATC分类
L01X 其它抗肿瘤药
药物类型
biotech
阶段
商品名
Herceptin (Genentech);
同义名
Anti HER2;Ig gamma-1 chain C region;
基本介绍

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.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Bange J, Zwick E, Ullrich A: Molecular targets for breast cancer therapy and prevention. Nat Med. 2001 May;7(5):548-52. Pubmed
    2. Menard S, Pupa SM, Campiglio M, Tagliabue E: Biologic and therapeutic role of HER2 in cancer. Oncogene. 2003 Sep 29;22(42):6570-8. Pubmed
    3. Kute T, Lack CM, Willingham M, Bishwokama B, Williams H, Barrett K, Mitchell T, Vaughn JP: Development of Herceptin resistance in breast cancer cells. Cytometry A. 2004 Feb;57(2):86-93. Pubmed
    4. Albanell J, Codony J, Rovira A, Mellado B, Gascon P: Mechanism of action of anti-HER2 monoclonal antibodies: scientific update on trastuzumab and 2C4. Adv Exp Med Biol. 2003;532:253-68. Pubmed
    5. Tan AR, Swain SM: Ongoing adjuvant trials with trastuzumab in breast cancer. Semin Oncol. 2003 Oct;30(5 Suppl 16):54-64. Pubmed
    6. IGMT Link
    7. IGMT Link
    剂型
    Form Route Strength
    Injection, powder, lyophilized, for solution Intravenous
    规格
    Unit description Cost Unit
    Herceptin 440 mg Solution Vial 3581.2 USD vial
    Herceptin 440 mg vial 3443.46 USD vial
    化合物类型
    Type biotech
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For treatment of early stage HER2-positive breast cancer, or metastatic breast cancer that substantially overexpress HER2.
    Pharmacodynamics 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.
    Mechanism of action 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.
    Absorption Not Available
    Volume of distribution
    • 44 mL/kg
    Protein binding Not Available
    Metabolism

    Most likely removed by opsonization via the reticuloendothelial system.
    Route of elimination Not Available
    Half life average 28.5 days
    Clearance Not Available
    Toxicity 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.
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00476 Trastuzumab Pathway SMP00476
    理化性质
    Properties
    State liquid
    Melting point 61 oC (FAB fragment), 71 oC (whole mAb)-Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000).
    Experimental Properties
    Property Value Source
    hydrophobicity -0.415 PhysProp
    isoelectric point 8.45 Various sources
    药物相互作用
    食物相互作用
    Not Available

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