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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