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 |