Table 1 Inhibitors of EMT in clinical phase trials

I. Blocking upstream signaling pathway

TGF-βR1

Galunisertib monohydrate

II

(Metastatic) breast cancer

NCT02538471

TGF-βR1

Vactosertib

I

Bladder cancer, breast cancer, melanoma, and prostate cancer

NCT03704675

TGF-βR2

SHR-1701

I

Solid cancers

NCT04324814

NF-κB

Bardoxolone methyl

II

Melanoma

NCT00535314

EGFR

Gefitinib

Marketed

Breast cancer and NSCLC

EGFR

Panitumumab

Marketed

Metastatic colorectal cancer

c-MET

Glesatinib

III

Non-small cell lung cancer

GDCT0241492

c-MET

Cabozantinib s-malate

Marketed

Medullary thyroid cancer

WIF1

BI-1361849

I and II

Non-small cell lung cancer

GDCT0251874

WIF1

OXB-301

III

Renal cell cancer

GDCT0017470

NOTCH2

Tarextumab

I/II

Pancreatic cancer

Small cell lung cancer

NCT01647828

NCT01859741

II.Targeting multiple EMT-TFs

HDAC1/4

Mocetinostat

II/III

Bladder cancer

NCT02236195

HDAC1/2/3/6

Vorinostat

III

Lung cancer

NCT00419367

LSD1

Domatinostat

II

Small cell lung cancer

GDCT0245900

LSD1

INCB-59872

I

Ewing sarcoma

NCT03514407

ZEB1/SNAIL2/TWIST/Vimentin

Metformin

II

Pancreatic

III. Targeting mesenchymal cells and ECM or inhibiting MET

N-cadherin

ADH-1

II

Adrenocortical carcinoma and non-small cell lung cancer

NCT00264433

Fibronectin

Monoclonal antibody

II

Breast, colorectal, lung and non-small cell lung cancer

NCT01125085

Vimentin

Pritumumab

II

Brain cancer

GDCT0217875

MMP2/3/9/13

Tanomastat

III

(Non)-small cell lung cancer

GDCT0022508

GDCT0023988

MMP

Batimastat

I

Hepatocellular

FAK

APG-2449

I

Non-small cell lung, ovarian cancer

GDCT0352706

EpCAM

Catumaxomab

I

Epithelial carcinomas

ITGA5/B1

ATN-161

II

Renal cell cancer

NCT00131651

ITGA5/B1

Volociximab

II

Renal cell cancer

NCT00100685

ITGAV

Cilengitide

II

Glioblastoma multiforme

NCT01782976

ITGAV

Intetumumab

II

Prostate cancer

NCT00537381