Harnessing the tumor microenvironment: targeted cancer therapies through modulation of epithelial-mesenchymal transition

Table 7 Inhibitors, antibodies, and PEGylated enzymes targeting ECM in the TME for cancer therapy used in clinical trials. Data has been collected from http://www.fda.gov, and http://www.clinicaltrials.gov accessed in November 2023

Drugs targeting ECM in the TME
Targeting ECM
Targeted Molecule	Drug Name	Type of Agent/s	Mechanism of Action	Status	Cancer Type/s	NCTs	References
HA	PEGPH20	PEGylated enzyme	Degradation of HA	Phase 3	ASTs (PC)	NCT02715804	PMID: 29,235,360
LOXL2	Simtuzumab	Blocking antibody	Destabilization of collagen
networks	Phase 2	ASTs (CRC, PC)	NCT01472198	PMID: 28,246,206
Collagen	Pirfenidone	Small-molecule inhibitors	Reduce collagen and HA	N/A	ASTs	NCT00020631	PMID: 38,561,001
	Losartan			Phase 2	ASTs (PC)	NCT01821729	PMID: 31,145,418
	Metformin			Phase 3	ASTs (BC)	NCT01101438	PMID: 35,608,580
FAK	Defactinib	Small-molecule inhibitors	Prevent integrin signaling	Phase 2	ASTs	NCT01870609	PMID: 30,785,827
	GSK-2256098			Phase 2	ASTs (PC)	NCT02428270	PMID: 36,636,049
CTGF	Pamrevlumab	Blocking antibody	Prevents integrin signaling	Phase 2	ASTs (PC)	NCT02210559	PMID: 32,817,130

Targeted Molecules: CTGF: Connective tissue growth factor; FAK: Focal adhesion kinase; HA: Hyaluronan; LOXL2: Lysyl oxidase like-2. Cancer Types: ASTs: Advanced Solid Tumors; BC: Breast Cancer; CRC: Colorectal Cancer; PC: Pancreatic Cancer. In case drugs targeting ECM in the TME for cancer therapy are being used in several ASTs, only a representative clinical trial (NCT) and its related reference (PMID) have been selected for (a) specific AST(s)

ISSN: 1756-8722