Methods and compositions for inhibiting integrin and treating integrin-related conditions, utilizing tellurium-containing compounds, are disclosed. The tellurium-containing compounds comprise at least one tellurium dioxo moiety and may have any one of Formulae I to IV as defined in the specification. Further disclosed are methods and compositions for treating a neoplastic condition characterized by a resistance to an anti-neoplastic agent and by a high level of expression of an integrin by neoplastic cells.