Historically, oral administration has been considered the easiest and most convenient method of drug delivery, as it requires minimal expertise and invasiveness. Although oral delivery works fairly effectively for small-molecule drug products, oral delivery of macromolecules (particularly proteins and peptides) has been more challenging. Given the increase in biologics over the last decade, injection and infusion have been the chosen choices of delivery to overcome this issue. However, there is much need to find and develop new materials to overcome the physiological challenges of oral delivery for macromolecular agents, including the importance of protease inhibitors, designed to treat HIV – Protease inhibitors work by blocking the activity of HIV protease. . 

This week’s available deck is titled “Structure-guided Discovery of Solid Forms to Drive Oral Bioavailability of Protease Inhibitors” from Phil Snyder and Setu Roday at Vertex Pharmaceuticals. Phil presented this approach at our 2020 Global Drug Bioavailability Enhancement Summit in New York. This presentation explores integrating research & development to accelerate clinical evaluation of medicines, it explores the mechanisms of insolubility and enabling molecules with potential and discusses opportunities to influence decision-making in pre-development.