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

Table 6 Inhibitors and antibodies targeting tumor vasculature in the TME for cancer therapy used in clinical trials or approved by the FDA. Data has been collected from http://www.fda.gov, and http://www.clinicaltrials.gov accessed in November 2023

Drugs targeting tumor vasculature in the TME
Targeting Tumor Vasculature
Targeted Molecule	Drug Name	Type of Agent/s	Mechanism of Action	Status	Cancer Type/s	NCTs	References
VEGF/VEGFR	Cediranib	Neutralizing antibodies, fusion proteins (VEGF-TRAP)	Antiangiogenic therapy	Phase 2	ASTs (GLI)	NCT00777153	PMID: 23,940,216
	Bevacizumab			Approved	ASTs (BC, CC, CRC, FTC, GLI, HCC, NSCLC, OC, PPC, RCC)	NCT03829410	PMID: 38,231,047
	Aflibercept			Approved	ASTs (CRC)	NCT00561470	PMID: 24,368,879
	Ramucirumab			Approved	ASTs (CRC, GC, HCC, NSCLC)	NCT00917384	PMID: 24,094,768
uPAR	WX-671	Small-molecule inhibitor	Antiangiogenic therapy	Phase 2	BC	NCT00615940	PMID: 35,158,766
RTKs	Axitinib	Small-molecule inhibitors	Antiangiogenic therapy	Phase 3	ASTs (RCC)	NCT00678392	PMID: 23,598,172
	Sorafenib			Approved	ASTs (HCC, RCC, TC)	NCT00073307	PMID: 17,215,530
	Sunitinib			Approved	ASTs (GIST, PC, RCC)	NCT00428597	PMID: 27,836,885
	Pazopanib			Approved	ASTs (RCC, STS)	NCT00720941	PMID: 23,964,934
ANG2–TIE2	MEDI3617	Neutralizing antibodies/
peptibodies, small-molecule
inhibitors	Antiangiogenic therapy	Phase 1	ASTs	NCT01248949	PMID: 29,559,563
	Rebastinib			Phase 2	ASTs	NCT03601897	PMID: 34,440,616
	Trebananib			Phase 3	ASTs	NCT01493505	PMID: 31,076,365

Targeted Molecules: ANG2-TIE2: Angiopoietin-2-TIE2; RTK: Receptor tyrosine kinase; uPAR: Urokinase-type plasminogen activator receptor; VEGF: Vascular endothelial growth factor; VEGFR: Vascular endothelial growth factor receptor. Cancer Types: ASTs: Advanced Solid Tumors; BC: Breast Cancer; CC: Cervical Cancer; CRC: Colorectal Cancer; FTC: Fallopian Tube Cancer; GC: Gastric Cancer; GIST: Gastrointestinal stromal tumor; GLI: Glioblastoma; HCC: Hepatocellular Carcinoma; NSCLC: Non-Small Cell Lung Cancer; OC: Ovarian Cancer; PC: Pancreatic Cancer; PPC: Primary Peritoneal Cancer; RCC: Renal Cell Carcinoma; STS: Soft Tissue Sarcoma; TC: Thyroid Cancer. In case drugs targeting tumor vasculature 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