Identifying novel therapies with increased safety margins and robust efficacy for chronic conditions like diabetes and obesity remains a formidable task for drug discovery. To achieve this goal our group has focused on the restriction of therapeutic molecules to the gastrointestinal tract, referred to as luminal restriction, as a method to increase the safety margin for new anti-diabetic and anti-obesity therapies. This talk will describe the design parameters and assays used to identify luminally restricted compounds as well as examples from our ileal bile acid transport inhibitor (iBATi) program and additional early discovery programs.

Luminally restricted therapeutics: Low permeability molecules for gastrointestinal targets

247th National Meeting (2014)

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