RO7117997

RO7117997 is an IND-ready small-molecule inhibitor of Equilibrative Nucleoside Transporter 1 (ENT1, SLC29A1) being developed for central nervous system indications, particularly sleep initiation and maintenance disorders and seizure disorders. It was discovered in a Roche–PsychoGenics collaboration using AI-enabled phenotypic screening platforms and subsequently identified as an ENT1 inhibitor, and PsychoGenics has licensed global development, manufacturing, and commercialization rights from Roche.[1][3][5][7] By selectively blocking ENT1-mediated cellular uptake of adenosine, RO7117997 is designed to increase extracellular adenosine levels in the brain, thereby enhancing adenosine receptor signaling to improve sleep quality and reduce seizure frequency, with additional potential applications across neuropsychiatric disorders (such as schizophrenia and addiction), neurodegenerative diseases, pain, and inflammation.[1][2][3][11][14]