Anti-HER2 Therapy

  • Pertuzumab:
    • Is approved for use preoperatively in advanced disease and in the metastatic setting
  • Trastuzumab:
    • Is approved for use in neoadjuvant, adjuvant, and metastatic settings
  • Ado-trastuzumab-emtansine and lapatinib:
    • Are approved for use in the metastatic setting:
      • Among patients who have progressed on previous lines of systemic chemotherapy, including trastuzumab
  • Lapatinib:
    • Is an oral small molecule receptor tyrosine kinase inhibitor of both:
      • HER2 and EGFR
  • Trastuzumab and pertuzumab:
    • Are humanized monoclonal antibodies:
      • That target the extracellular HER2 domain
    • However, pertuzumab:
      • Binds to a different HER2 epitope than trastuzumab:
        • Resulting in more HER2 blockade when they are given together
  • Ado-trastuzumab-emtansine:
    • Is a HER2-antibody drug conjugate:
      • That incorporates trastuzumab with emtansine:
        • A microtubule inhibitor DM1:
      • The conjugate:
        • Which is linked via a stable thioether linker:
          • Allows for selective delivery into HER2 overexpressing cells:
            • Resulting in cell cycle arrest and apoptosis

REFERENCES

  1. Lin JJ, Cardarella S, Lydon CA, et al. Five-year survival in EGFR-mutant metastatic lung adenocarcinoma treated with EGFR-TKIs. J Thorac Oncol. 2016;11(4):556-565.
  2. Weickhardt AJ, Price TJ, Chong G, et al. Dual targeting of the epidermal growth factor receptor using the combination of cetuximab and erlotinib: preclinical evaluation and results of the phase II DUX study in chemotherapy-refractory, advanced colorectal cancer. J Clin Oncol. 2012;30(13):1505-1512.
  3. Jiang H, Rugo HS. Human epidermal growth factor receptor 2 positive (HER2+) metastatic breast cancer: how the latest results are improving therapeutic options. Ther Adv Med Oncol. 2015;7(6):321-339.

#Arrangoiz #BreastCancer #CancerSurgeon #SurgicalOncology #BreastSurgeon

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