Integrin Antagonists Function Disadvantage/ Advantage   avb3 Monoclonal  ab Vitaxin (LM 609 mAb)     First generation of MEDI – 523 & Second generation of MEDI-522 Intetumumab (CNTO 95) EMD 525797 (DI17E6) mAb Non-peptide inhibitors MK0429   PSK1404   IH1062     S 137 and S247 17E6   GIPG0187,RGD antagonists     DisBa-01, novel monomeric P-II SVMP-derived RGD disintegrin ATN-161, acetylated, amidated PHSCN peptide Inhibits cell adhesion, blocks Vitronectin receptors  & Bax apoptotic pathway, upregulates matrix degradation inhibitors Inhibits  MAPKinase pathway, inhibits MMP- activation, lowers TGF- β1 accumulation Inhibits the contact between ECM and tumor cells, inhibits angiogenesis   Inhibits the ligand binding to αv  heterodimers     Inhibits osteoclast formation in bone metastasis Inhibits osteoclast bone resorption and inhibits ovarian and breast cancer Inhibit the cell growth and enhance apoptosis by inhibiting the interaction with ligand Inhibits vitronectin binding, Inhibits pulmonary metastasis Decreases BCl-2/Bax ratio and survivin protein Promotes endocytosis of αvβ3 integrin, Anti tumor, anti adhesive and anti metastatic activities Decreases Aldehyde dehydrogenase and increases E-cadherin/vimentin ratio Inhibits angiogenesis Impairs TGF-β signalling Inhibits VEGF expression and angiogenesis Inhibits MMP-2 activity Inhibits angiogenesis and metastasis by reducing VEGF expression Anti tumorigenic and anti metastatic Prevents recurrence of cancer Short half life and inefficient interaction No tumor regression No clinical significance due to less affinity and stability Safe for long term administration   Efficacy, dose dependent  tolerability and under phase II trails   Oral compound is not developed even though safe and tolerable Preclinical study is limited   Provides promising results in tumor metastasis     Reduces the development of liver metastasis Under clinical trial   Under Phase I trails in cancer therapy         Novel in anti-metastatic therapy   Under Phase II trails α5β1 Volociximab     GIPG0187, non peptide RGD antagonists   Resveratol, natural polyphenolic antioxidant Inhibits the function of  α5β1integrin  Induces apoptosis in cancer cells Inhibits angiogenesis   Decreases Aldehyde dehydrogenase and increases E-cadherin/vimentin ratio Inhibits angiogenesis Impairs TGF-β signalling Down regulates α5β1 integrins Induces apoptosis Inhibits tumor growth significantly   Under Phase I trails in cancer therapy   Further study is required

Table 1: Monoclonal antibodies and other non peptide mediated antagonists of αvβ3 and α5β1 integrins and the details are given in the text.

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