Trastuzumab (Herceptin)

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General information

Class/mechanism: HER2/neu receptor antagonist, humanized IgG1 kappa monoclonal antibody. Trastuzumab binds to the extracellular domain of HER2/erbB2 (human epidermal growth factor receptor 2), which is overexpressed in certain malignancies. Trastuzumab helps to mediate antibody-dependent cellular cytotoxicity (ADCC) preferentially against cells that overexpress HER2.[1][2][3]
Route: IV
Extravasation: neutral

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

HER2+ breast cancer

  • 9/25/1998: Initial FDA approval as a single agent for treatment of patients with metastatic breast cancer whose tumors overexpress the HER2 protein and who have received one or more chemotherapy regimens for their metastatic disease. (Based on Cobleigh et al. 1999)
  • 8/28/2002: Approved in combination with paclitaxel for treatment of patients with metastatic breast cancer whose tumors overexpress the HER2 protein and who have not received chemotherapy for their metastatic disease. (Approval extended to first-line metastatic setting; based on Slamon et al. 2001)
  • 11/16/2006: Label revised: trastuzumab as part of a treatment regimen containing doxorubicin, cyclophosphamide, and paclitaxel is indicated for the adjuvant treatment of patients with HER2-overexpressing, node-positive breast cancer. (Approval extended to adjuvant setting; based on BCIRG 006, HERA, NCCTG N9831, NSABP B-31)
  • 1/18/2008: Labeling simplified: indicated for the treatment of HER2 overexpressing breast cancer. (Approval extended to all settings)

HER2+ gastric/gastroesophageal cancer

History of changes in EMA indication

  • 8/28/2000: Initial market authorization as Herceptin

Also known as

  • Brand names: Biceltis, CANMab, Herceptin, Herclon, Hertraz