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Table 4 Biologic anti-HER2 agents approved for breast cancer treatment

From: Molecular characterization and targeted therapeutic approaches in breast cancer

Agent Approval Mechanism of action Indications
Trastuzumab 1998 Humanized monoclonal antibody against the extracellular domain of HER2. It triggers HER2 internalization and degradation. Adjuvant BC
Metastatic BC
(from the first line)
Lapatinib 2006 Dual inhibitor of the intracellular tyrosine kinase domains of both HER1 (EGFR) and HER2. Metastatic BC
(after prior anthracycline, taxane, and trastuzumab)
Pertuzumab 2012 Humanized monoclonal antibody against the extracellular dimerization domain of HER2. It blocks the heterodimerization of HER2 with other HER family. Neoadjuvant BC
(with trastuzumab and docetaxel in locally advanced, inflammatory, or early stage BC -either >2 cm or node-positive)
Metastatic BC
(with trastuzumab and docetaxel for first-line therapy)
T-DM1 2013 Trastuzumab-like activity. Metastatic BC (after the first line or in first line if trastuzumab-resistance)
Targeted intracellular delivery of cytotoxic emtansine.
  1. BC, breast cancer; EGFR, epidermal growth factor receptor; HER2, human epidermal growth factor receptor 2.