This Keystone Symposium directly addresses an urgent scientific need for innovative, new approaches to central nervous system (CNS) drug delivery. Indeed, the current shortage of disease-modifying treatments for Alzheimer’s, Parkinson’s and other CNS diseases represent among the most significant unmet health needs of our time. Our ability to effectively tap into the vast potential that protein, oligonucleotide, and gene therapies have for treating CNS disorders has been sharply limited by the typically insufficient brain exposure that results after their systemic or central administration. Even many orally administered small molecules suffer from brain exposure limitations. Among the primary reasons for these limitations are the physical and biochemical barriers that exist at key CNS interfaces, including the blood-brain barrier at the level of the cerebrovasculature, other specialized barriers between the blood and cerebrospinal fluid, and further obstacles hindering drug exchange between cerebrospinal fluid and CNS tissue. CNS drug delivery research lies at the crossroads between many different fields, including physiology, pharmacology, pharmaceutical science, neuroscience, neurosurgery, engineering, genetics, and vascular biology, among others. Surprisingly few conferences to date have focused exclusively on the multidisciplinary challenges associated with CNS drug delivery. The goals of this symposium are (i) to bring together international experts and junior investigators from multiple research fields for the purpose of exchanging new ideas and brainstorming novel solutions to existing CNS drug delivery challenges and (ii) to highlight new methods and perspectives with the potential to change how CNS drug delivery research studies are performed and, ultimately, to transform the field. Sessions are to include a number of short talks chosen to integrate late-breaking developments and new research directions from the field.