αβ integrin inhibitors: a patent review.

The αβ integrin is heterodimeric cell surface receptors expressed on most leukocytes. Mucosal addressing cell adhesion molecule 1(MAdCAM-1) is an exclusive ligand for αβ integrin. Areas covered: This article will highlight the progress that has been made in the discovery and development of αβ integrin inhibitors, and their use in the treatment of inflammatory bowel diseases, multiple sclerosis, asthma, hepatic disorders, human immunodeficiency virus, allergic conjunctivitis and type 1 diabetes. Expert opinion: αβ integrin inhibitors have attracted much interest for their clinical implication. Natalizumab and Vedolizumab are monoclonal antibodies (mAbs) successfully utilized clinically. Natalizumab is a mAbs of α-subunit blocking both αβ and αβ integrin. Vedolizumab selectively targets the αβ integrin. Several mAbs are still in the process of research and development. Among these mAbs, etrolizumab selectively against the β-subunit and AMG-181 specifically against the αβ integrin are the most promising anti-αβ integrin antibodies. Despite the unclear development stage of TR-14035 and R411, several low molecular compounds show bright future of further development, such as AJM300 and CDP323. In addition, results from laboratory data show that peptide inhibitors, such as peptide X, are effective αβ integrin inhibitors.