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Table 2 Main trials of targeted agents for ER+/HER2- advanced/metastatic breast cancer: CDK inhibitors, FGFR inhibitors, HDAC inhibitors, and combined therapy

From: Targeted therapies for ER+/HER2- metastatic breast cancer

Target Function Agent Trial Phase Design Results with significance/Study status
Population Arms CBR TTP Median PFS Median OS
CDK CDK4/6 inhibitor Palbociclib PALOMA-1 [28] II First line Palbociclib + LET vs. LET     
PALOMA-2 NCT01740427 III HTfailure Palbociclib + FUL vs. FUL Ongoing
PALOMA-3 NCT01942135 III First line Palbociclib + LET vs. LET Ongoing
PEARL NCT02028507 III AI failure Palbociclib + EXE vs. capecitabine Ongoing
LEE011 MONALEESA-2 NCT01958021 III First line LEE011 + LET vs. LET Ongoing
MONALEESA-7 NCT02278120 III Pre/peri menopausal First line LEE011 + nsAI/TAM + gos vs. nsAI/TAM + gos     
NCT01709370 II AI failure Monotherapy Ongoing
LY2835219 Monarch3 NCT02246621 III First line LY2835219+nsAI vs. nsAI Ongoing
FGFR TKI inhibitor FGFR VEGFR PDGFR Lucitanib FINESSE NCT02053636 II 1 line HT failure Monotherapy Ongoing
Dovitinib NCT00958971 II With or without FGFR amplification Monotherapy 21.1 % vs. 12.0 %    
NCT01528345 II HT failure Dovitinib + FUL vs. FUL Ongoing
FGFR1-3 AZD4547 NCT01791985 I/II 1 line nsAI failure AZD4547 vs. EXE Ongoing
HDAC HDAC inhibitor Entinostat ENCORE 301 [35] II nsAI failure Entinostat + EXE vs. EXE 28.1 % vs. 25.8 %   4.3 mo vs. 2.3 mo 28.1 mo vs. 19.8 mo
NCT02115282 III nsAI failure Entinostat + EXE vs. EXE Ongoing
NCT02115594 II HT failure Entinostat + FUL vs. FUL Ongoing
Vorinostat [34] II HT failure Vorinostat + TAM 40 %    
NCT00616967 II HT failure Vorinostat + AI Ongoing
Combined CDK inhibitor/mTOR inhibitor LEE011 vs. everolimus NCT01857193 I/II First line LEE011 + everolimus + EXE vs. LEE011 + EXE vs. everolimus + EXE Ongoing
Pan-PI3K inhibitor/CDK inhibitor BYL719 vs. LEE011 NCT01872260 I/II HT failure LEE011 + LET vs. BYL719 + LET vs. LEE011 + BYL719 + LET Ongoing
Pan-PI3K inhibitor/PI3K-α inhibitor BKM120 vs. BYL719 with LEE001 NCT02088684 I/II HT failure no more than 2 lines of CT BKM120 + LEE001 + FUL vs. BYL719 + LEE001 + FUL vs. LEE001 + FUL Ongoing
  1. Abbreviations; CDK: cyclin-dependent kinase, LET: letrozole, FUL: fulvestrant, HT: hormonal therapy, EXE: exemestane, AI: aromatase inhibitor, nsAI: non-steroidal AI, FGFR: fibroblast growth factor receptor, TK: tyrosine kinase, VEGFR: vascular endothelial growth factor receptor, PDGFR: platelet-derived growth factor receptor, HDAC: histone deacetylase, TAM: tamoxifen, PI3K: phosphatidylinositol-3-kinase, CT: chemotherapy