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Table 3 Target-directed agents classified by class of agent and whether established or emergent

From: Patterns in target-directed breast cancer research

Drug class and description Established Emergent
Anti-angiogenic therapy: Drugs that interfere with angiogenesis and block tumor growth (target VEGF, VEGF receptor or block kinases involved in VEGF signaling)   Bevacizumab, Cabozantinib, Endostar, Icrucumab, Nintedanib (BIBF 1120), Pazopanib, Ramucirumab, Sorafenib, Sunitinib, Tivozanib, Trebananib (AMG 386), Vandetanib
HER2 targeted therapy: Drugs that bind to Her2 or inhibit its tyrosine-kinase activity Lapatinib, Pertuzumab, T-DM1, Trastuzumab Afatinib, AZD8931, Neratinib, Trastuzumab biosimilars (ABP 980 and BCD-022)
Growth factor-inhibitors: Drugs that bind to EGFR, HER3, HER4, IGFR, FGFR, PDGFR and RANKL or inhibit the tyrosine-kinase activity of these receptors Denosumab AZD4547, BMS-754807, Cetuximab, Cixutumumab, Dalotuzumab, Dovitinib, Erlotinib, Ganitumab, Gefitinib, Imatinib, MEDI-573, MM-121, U3-1287
mTOR/PI3K/Akt-pathway-inhibitors: Drugs that inhibit signaling of the pathway Everolimus AZD5363, BEZ235, BKM120, BYL719, DLBS1425, GDC-0941, GDC-0980, MK-2206, PF-4691502, Ridaforolimus
Therapies that target ER or hormonal production: Drugs that interfere with estrogen/androgen ability to promote tumor growth and proliferation Anastrozole, Exemestane, Fulvestrant, Goserelin (ZD9393), Letrozole, Leuprorelin, Progesterone, Tamoxifen, Toremifene, Triptorelin Abiraterone, AEZS-108, CDB-4124, Irosustat
PARP1/2-Inhibitors: Drugs that inhibit of the activity of PARPs.For historical reasons, iniparib was included in this class   Iniparib, Niraparib, Rucaparib, Veliparib (ABT-888)
Intracellular, non-receptor PK-inhibitors: Includes inhibitors of Aurora A kinase, CDK4-6, c-Met, Src-family, MEK/MAPK/ERK and AMPK   Alisertib (MLN8237), AZDO530, Dasatinib, LEE011, Metformin, Onartuzumab, Palbociclib (PD-0332991), Selumetinib
Immunotherapy/cancer vaccines: Drugs that target the immune system to destroy cancer cells or interfere with growth of specific cancer cells   Allogeneic GM-CSF-secreting breast cancer vaccine, autologous dendritic cell-adenovirus p53 vaccine, GSK2302024A, HER-2/neu peptide vaccines, Ipilimumab, PANVAC-V/F, Reolysin
Antibody–drug conjugates: Drugs composed of an targeted drug (antibody) and a cytotoxic drug, delivered only to the targeted cancer cell T-DM1 AEZS-108, Glembatumumab vedotin
Other targeted therapies: Drugs with other targets not included previously or trials that include multiple targeted therapies Biphosphonates (Ibandronate, Zoledronate) Bortezomib, Erismodegib (LDE225), Ganetespib, Imetelstat, Indoximod, LCL161, Litronesib, RO4929097, Tigatuzumab, Tipifarnib, YM155, Zibotentan (ZD4054)
  1. CDK cyclin-dependent kinase, EGFR epidermal growth factor receptor, ER estrogen receptor, HER2 human epidermal growth factor receptor 2, HER3 human epidermal growth factor receptor 3, HER4 human epidermal growth factor receptor, IGFR insulin-like growth factor receptor, FGFR dibroblast growth factor receptor, mTOR mammalian target of rapmycin, PARP poly(ADP-ribose) polymerase, PI3K phosphoinositide 3-kinase, PDGFR platelet-derived growth factor receptor, RANKL receptor activator of nuclear factor kappa-B ligand, T-DM1 trastuzumab emtansine, VEGF vascular endothelial growth factor