Dedicated DMPK for Bifunctional Degraders: A Flexible Approach for Flexible Molecules

Bifunctional degraders are compounds that bind to and induce degradation of a target by simultaneously binding to a ubiquitin ligase. Despite their size and physical properties lying outside the space usually required for oral absorption (beyond rule of 5, bRo5) there are many reports of bifunctional degraders with high bioavailability and acceptable oral exposure in pre-clinical models. However, challenges still exist due to the physicochemical space occupied by these molecules, and how well in vitro DMPK assays translate into in vivo performance.

Download this poster to see how Sygnature Discovery applies dedicated assays to support drug discovery projects involving bifunctional degraders, together with exemplar data for a variety of compounds.