ARTICLE | Cover Story

Truly Boronic

October 2, 2008 7:00 AM UTC

Researchers at Tufts University have shown that peptide boronic acid inhibitors of dipeptidyl peptidase-4 could provide effective, low-toxicity treatments for diabetes.1 The findings challenge the long-held assumption that boronic acids are too toxic for therapeutic use. Arisaph Pharmaceuticals Inc. has already in-licensed the related IP and has ARI-2243, a boronic acid inhibitor of dipeptidyl peptidase-4, in Phase I testing to treat diabetes.

Other companies contacted by SciBX said the findings make the case for taking another look at boronic acids as therapeutics, but they noted that the high potency makes selectivity a key issue, because that potency increases the likelihood of off-target effects at therapeutic doses...