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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