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 | Â | Â | Â | Â |
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 | Â | Â | Â | Â | |||
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 % | Â | Â | Â | ||
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 % | Â | 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 % | Â | Â | Â | ||
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 |