Integrin receptors are cell surface molecules that are responsible for cell-to-cell interaction and interaction between cell and extracellular matrix proteins. Integrins’ diversity determines specific ligand binding and induces specific signaling pathways. The key role in metastasis and angiogenesis is played by β3-integrins. Integrin αIIbβ3 (GP IIb/IIIa) is the main membrane glycoprotein receptor on the surface of platelets. It is also present on the surface of cancer cells: breast carcinoma cell line MCF-7, different melanoma cell lines and squamous cell carcinoma line (SCC). Inhibitors of αIIbβ3 receptor (Abcksimab, Eptifibatide, Tirofiban) are parenteral drugs used for inhibiting platelet aggregation in a therapy of acute coronary syndrome. However their influence on cancer cell growth and molecular mechanism of this process is not precisely known. There is evidence that RGD-peptides, anti-integrin antibodies and disintegrins inhibit cancer cell invasion and metastasis. Therefore trials upon biologic activity of αIIbβ3 inhibitors may be helpful in developing a new direction in anticancer therapy.