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Product Details:

  • CAS No: 180288-69-1
  • AHFC code:
  • Synonyms: Anti HER2, Ig gamma-1 chain C region
  • ATC Code: L01XC03
  • Chemical Formula: C6470H10012N1726O2013S42
  • Molecular Weight: 145531.5
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00072 (BIOD00098, BTD00098)
  • SMILES:
  • InChl:
  • PubChem: BTD00098
  • IUPAC:

Additional Details

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.
Mode 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.
Metabolism:
Most likely removed by opsonization via the reticuloendothelial system.
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.
General Reference:
Bange J, Zwick E, Ullrich A: Molecular targets for breast cancer therapy and prevention. Nat Med. 2001 May;7(5):548-52. PubmedMenard S, Pupa SM, Campiglio M, Tagliabue E: Biologic and therapeutic role of HER2 in cancer. Oncogene. 2003 Sep 29;22(42):6570-8. PubmedKute 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. PubmedAlbanell 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. PubmedTan AR, Swain SM: Ongoing adjuvant trials with trastuzumab in breast cancer. Semin Oncol. 2003 Oct;30(5 Suppl 16):54-64. PubmedIGMT LinkIGMT Link
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