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Table 1 Therapeutic agents targeting the HER2 pathway in breast cancer

From: Recent advances in systemic therapy: Advances in systemic therapy for HER2-positive metastatic breast cancer

Agent Molecule Target/mechanism Status
Trastuzumab Monoclonal antibody Blocks extracellular domain of HER2 US FDA approved in metastatic and adjuvant settings [16]
Pertuzumab (2C4) Monoclonal antibody Blocks HER2 and HER3 dimerization Phase III (with trastuzumab)
Trastuzumab-DM1 Antibody-drug conjugate Binds HER2, conjugate is internalized, and DM1 toxin causes cancer cell death Phase III
Ertumaxomab Monoclonal antibody Trifunctional anti-HER2 × anti-CD3 antibody Phase II
Lapatinib Small molecule TKI Reversible inhibitor of EGFR and HER2 TK FDA approved in metastatic setting [52]
Gefitinib Small molecule TKI Reversible inhibitor of EGFR Phase II (discontinued because of poor results)
Erlotinib Small molecule TKI Reversible inhibitor of EGFR Phase II
HKI-272 Small molecule TKI Irreversible inhibitor of the HER-2 and EGFR TK Phase I/II
BIBW2992 Small molecule TKI Irreversible inhibitor of the HER-2 and EGFR TK Phase II
Temsirolimus (CCI779) Rapamycin analogue mTOR inhibitor and Akt deactivation Phase III (with letrozole)
Everolimus (RAD001) Rapamycin analogue mTOR inhibitor and Akt deactivation Phase III (with paclitaxel)
Tanespimycin (17AAG) Derivate of geldanamycin Hsp-90 inhibitor (anti-downstream pathway element) Phase II
Tipifarnib Analogue of imidazole farnesyltranstransferase inhibitor (downstream pathway element) Phase II (with chemo and/or homonaltherapy)
GDC-0941 Small molecule PI3K inhibitor Phase I
  1. EGFR, epidermal growth factor receptor; FDA, Food and Drug Administration; HER, human epidermal growth factor receptor; Hsp, heat shock protein; mTOR, mammalian target of rapamycin; TK, tyrosine kinase; TKI, tyrosine kinase inhibitor.