firategrast (GSK)

Firategrast (SB683699) is an orally active small molecule that acts as a specific antagonist of the α4β1 and α4β7 integrins. It was developed to reduce the trafficking of lymphocytes into the central nervous system (CNS), thereby decreasing disease activity in multiple sclerosis (MS). Firategrast inhibits the binding of these integrins to their ligands, including vascular cell adhesion protein 1 (VCAM-1) and mucosal addressin cell adhesion molecule 1 (MAdCAM-1), which are involved in leukocyte migration across the blood-brain barrier. The drug has been studied primarily for relapsing-remitting multiple sclerosis and has also been investigated for asthma, rheumatoid arthritis, and Crohn’s disease; however, development for these latter indications was discontinued. Firategrast was developed by GlaxoSmithKline under license from Mitsubishi Tanabe Pharma[2][3][4][5][7].

Other names

firategrastum402567-16-2