BLOOD-BRAIN BARRIER DRUG TARGETING: THE FUTURE OF BRAIN DRUG DEVELOPMENT

Abstract

The development of new drugs for the brain has not kept pace with progress in the molecular neurosciences, because the majority of new drugs discovered do not cross the blood-brain barrier (BBB). Although approximately 100% of large-molecule drugs do not cross the BBB, the problem is nearly as severe for small-molecule drugs—greater than 98% of small-molecule drugs do not cross the BBB. Despite this situation, no pharmaceutical company in the world today has a BBB drug-targeting program. Nevertheless, BBB drug targeting technology can be built around a knowledge base of the endogenous transporters within the brain capillary endothelium, which forms the BBB in vivo.