Blocking α4-integrins - A small molecule approach to treatment of multiple sclerosis

Inhibition of leukocyte trafficking using antibody blockade of the alpha4 (α4)-integrins has now been validated as a therapeutic approach for the treatment of multiple sclerosis (MS). This positive validation has led to the discovery of small molecule α4 antagonists that are progressing through clinical trials. The challenges in development of these antagonists will be discussed along with a clinical update on the most advanced candidates.