Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment[1][2].
Valategrast contains a common l-phenylalanine-N-aroyl motif where the carboxylic acid is responsible for binding to the metal ion in the metal-ion-dependent adhesion site (MIDAS)[2].
[1]. Woodside DG, et al. Cell adhesion antagonists: therapeutic potential in asthma and chronic obstructive pulmonary disease. BioDrugs. 2008;22(2):85-100.
[2]. Halland N, et al. Small Macrocycles As Highly Active Integrin α2β1 Antagonists. ACS Med Chem Lett. 2014 Jan 10;5(2):193-8.