Table 3 Selected compounds currently under investigation for use in metastatic breast cancer
From: Current approaches to the management of Her2-negative metastatic breast cancer
Target | Agent (Company) | Mechanism [9] | Status [86] |
|---|---|---|---|
Poly ADP-ribose polymerase (PARP) | Olaparib (AstraZeneca, London, UK) and Iniparib (Sanofi , Paris, France) | Inhibits PARP-mediated repair of single-stranded DNA breaks potentially enhancing cytotoxicity of DNA-damaging agents | Phase II and III (Iniparib) |
Vascular endothelial growth factor receptor-2 (VEGFR-2) | Ramucirumab/IM-111B (Eli Lilly and Company, Indianapolis, IN, USA | Monoclonal antibody targeting VEGFR-2/pro-angiogenic growth factor receptor tyrosine kinase | Phase III |
FK-binding protein-12 (FKBP-12) | Everolimus (Novartis, East Hanover, NJ, USA) | Binds to FKBP-12 to generate activation of mammalian target of rapamycin (mTOR), a complex that inhibits regulatory kinase, resulting in inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine stimulation and inhibition of antibody production. Inhibiting the mTOR pathway could overcome endocrine resistance mediated by ligand-independent receptor activation | Phase III Approved for renal transplant immunosuppressive therapy; application for breast cancer indication yet to be submitted. |