RO0506997

RO0506997 is an orally bioavailable small molecule antagonist of alpha-4 integrin (A4I), specifically targeting the VLA-4 (alpha-4 beta-1) and potentially alpha-4 beta-7 integrin heterodimers. Developed by Roche, the drug was designed to treat relapsing multiple sclerosis (MS) by preventing the adhesion and subsequent migration of inflammatory leukocytes across the blood-brain barrier into the central nervous system. By blocking the interaction between alpha-4 integrins on the surface of white blood cells and their ligands, such as vascular cell adhesion molecule-1 (VCAM-1) on endothelial cells, RO0506997 aimed to reduce the inflammatory MRI lesions and clinical relapses associated with MS. Clinical development reached Phase 2 testing, where it was evaluated for safety and efficacy in reducing brain lesions, but the program appears to have been discontinued in favor of other therapeutic modalities.

Other names

A4I AntagonistA-4I AntagonistA 4I Antagonist