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

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.