Table 2.

Integrin targeting methods

Therapeutic agent	Targeting moiety	Tumour model(s)	Results	Refs
Mutant RAF1	Organic ανβ3 ligand	Subcutaneous human melanoma cells	Regression of established primary and metastatic tumours and apoptosis of the tumour-associated vasculature	113
Nanoparticle loaded with doxorubicin	cRGD	Orthotopic mouse pancreatic tumour cells and human melanoma and renal tumour cells	Suppressed spontaneous metastases by disrupting the associated vasculature at very low doses	167
Nanoparticle loaded with fumagillin	cRGD	Vx-2 rabbit adenocarcinoma	Suppressed angiogenesis and tumour development at low doses	183
Oncolytic measles virus	cRGD	Subcutaneous human myeloma cells	Targeted delivery of virus to tumour neovessels	184
TRAIL	RGD	Subcutaneous human colon cancer cells	Inhibited primary tumour burden to a greater extent than TRAIL alone	185
p53	RGDK-lipopeptide	Orthotopic mouse melanoma cells	Targeted tumour vasculature and inhibited tumour volume	186
Radionucleotide	cRGD	Subcutaneous human ovarian cancer cells	Increased survival compared with untreated mice	187, 188
Radionucleotide	Etaracizumab	Orthotopic human glioblastoma cells and subcutaneous human colon cancer cells	Decreased angiogenesis and reduced tumour volume better than delivery of the antibody alone	189
Cytotoxic immunoconjugates	CNTO 95	Subcutaneous human colon and lung cancer cells	Reduced primary tumour burden above the level observed with antibody alone	190

cRGD, cyclic arginine-glycine-aspartic acid; RGDK, arginine-glycine-aspartic acid-lysine; TRAIL, tumour necrosis factor-related apoptosis-inducing ligand.