Zaurategrast

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Zaurategrast (CDP323) is a small drug designed to block VCAM-1 from sticking to α4-integrins. By doing this, it aims to stop immune cells from leaving the blood and entering inflamed tissues like the brain, which could help treat multiple sclerosis (MS). It is a prodrug developed by Celltech (now UCB). In 2006, UCB and Biogen Idec planned to develop and commercialize it for MS and other conditions. In 2009, development was stopped after a Phase II trial did not meet expectations. Zaurategrast works in a similar way to natalizumab, a monoclonal antibody with the same target. In mouse studies of autoimmune brain inflammation, it reduced disease severity when given before or after disease started. Phase 1 studies in 75 healthy volunteers showed the drug was generally safe at up to 1000 mg twice daily for a week, with side effects similar to placebo and no gender differences. It also blocked VCAM-1 binding for 12–24 hours at the doses tested. A Phase 2 study started in 2007 with more than 200 relapsing MS patients who had failed interferon-beta, comparing two doses to placebo over six months. Early results showed no clear benefit versus placebo after six months; no cases of progressive multifocal leukoencephalopathy were observed.