Table 1.

Inhibitors of EMT in clinical phase trials

Treatment strategies	Target	Drug	Stage/phase	Cancer	Trial identifier
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