The NMDA receptor has long been an attractive target for various neuroscience indications. Recently, an intranasal formulation of the -<i>S</i>- form of ketamine, esketamine, an NMDA receptor blocker, was approved as a rapidly acting antidepressant agent.<br/>We have identified an NMDA NR2B subunit selective, negative allosteric modulator (NAM), with rapidly acting antidepressant clinical activity. We believe this to be the only NR2B NAM currently in clinical development for depression. We will present the discovery of MIJ821 in collaboration with biotech partners. We will include a story of scaffold morphing from a literature lead, balancing properties, in particular hERG and PGP efflux to ensure brain exposure, a target engagement imaging strategy, and a summary of the Phase 1 and Phase 2 clinical data that has led to this molecule moving into full clinical development.

Discovery and first disclosure of MIJ821, a novel, rapidly acting antidepressant

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.