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R1295 (also known as RO0271295) is a small molecule antagonist of the alpha-4/beta-1 (α4β1) integrin, also known as Very Late Antigen-4 (VLA-4). Developed by Roche, the drug was designed to inhibit the interaction between VLA-4 on the surface of leukocytes and its ligands, such as Vascular Cell Adhesion Molecule-1 (VCAM-1) and the CS-1 fragment of fibronectin. By blocking this interaction, R1295 aims to prevent the recruitment and infiltration of inflammatory cells into tissues, which is a key driver of autoimmune and inflammatory diseases. The compound was primarily evaluated in Phase II clinical trials for the treatment of rheumatoid arthritis and was also explored for potential use in multiple sclerosis and asthma. However, Roche discontinued the development of R1295, and it did not progress to late-stage clinical trials or regulatory approval.
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