The metastatic process is the major cause of mortality in cancer patie
nts. Metastasis involves tumour cell adhesion to other cells and extra
cellular matrix glycoproteins, and eventual invasion through basement
membranes. Such interactions may be mediated by a great variety of cel
l surface biomolecules, including integrins. The development of integr
in antagonists offers a promising strategy to inhibit metastasis. Pote
ntial integrin-based therapeutics include synthetic peptides that have
been modified via cyclisation, or inclusion of all-D amino acids, as
well as a variety of organic molecules. Issues of specificity have bee
n addressed and ligands that bind to only one particular integrin have
been isolated. Improved bioavailability appears to be the next area f
or consideration to create efficient delivery of potential antimetasta
tic compounds.