Delivery of small molecule therapeutics to the brain has been challenging as most small molecule drugs are actively excluded by efflux pumps. It has been estimated that approximately 98% of small molecule drugs do not cross the BBB.
We are focused on engineering small molecule therapeutics that achieve exposure levels in the brain sufficient to bind to protein targets and drive a therapeutic effect. Efficacious orally administered small-molecule medicines for brain diseases must be readily absorbed from the gut into the blood and penetrate the BBB while avoiding transporter-mediated efflux. Our small molecule drug discovery scientists have many years of experience designing small molecules for brain diseases