Table 1. Examples of integrin-inhibiting agents used in cancer therapy.

Integrin-inhibiting agent		Target	Clinical phase	Type of cancer	Effect	Outcome	References
Monoclonal antibodies	Intetumumab	αv	I and II	Melanoma, sarcoma, prostate, and colorectal cancer	Inhibits the contact between extracellular matrix (ECM) and tumor cells and inhibits angiogenesis	Improved overall survival with high doses or no benefits	118,119
	Abituzumab	αv	I and II	Melanoma, sarcoma, prostate, and colorectal cancer	Inhibits the contact between ECM and tumor cells and inhibits angiogenesis	No benefits or trials ongoing	120
	Vitaxin	αvβ3	I and II	Metastatic cancers	Inhibits cell adhesion, blocks apoptotic pathway, and upregulates matrix degradation inhibitors	Short half-life and inefficient interaction. No tumor regression	121,122
	Etaracizumab	αvβ3	I and II	Melanoma	Inhibits the contact between ECM and tumor cells and inhibits angiogenesis	Good tolerability and no anti-angiogenic or immunomodulatory effects	123
	Volociximab	α5β1	I and II	Ovarian, pancreatic and renal cancer, melanoma, and non-small-cell lung cancer	Inhibits interaction with ECM, induces apoptosis in cancer cells, and inhibits angiogenesis	Good tolerability, anti-angiogenic effects, or no benefits	124
Peptides	Cilengitide	αvβ3 αvβ5	I, II, and III	Multiple cancer, including glioblastoma	Compete with ligand binding and inhibit angiogenesis and cancer cell invasion	No therapeutic benefits	125–131
	ATN-161	α5β1	I and II	Lung, colon	Anti-tumor, anti-adhesive, and anti- metastatic activities and inhibits angiogenesis	No therapeutic benefits	132
Small-molecule inhibitors	GIPG0187	Arg-Gly-Asp (RGD)-binding integrins	I	Advanced cancers	RGD antagonist	Ongoing, reduced liver metastasis	133