EVT100

**EVT100** is an orally active small molecule from the EVT100 series, originally discovered by Roche and licensed to Evotec for development. It functions as a selective antagonist of the NR2B (GluN2B) subtype of NMDA receptors, aimed at providing rapid antidepressant effects similar to ketamine but with oral bioavailability. The compound showed good tolerability in Phase I/Ib studies across young and elderly healthy volunteers, with brain penetration confirmed via CSF measurements and fMRI evidence of NR2B blockade at therapeutic doses. Development focused primarily on treatment-resistant depression but was discontinued after voluntary termination of a Phase II proof-of-concept trial due to recruitment challenges, toxicology concerns, and dosing issues; potential also explored in Alzheimer's disease, neuropathic pain, and Parkinson's disease.

Other names

EVT-100 seriesEVT100 seriesEVT 100 seriesNR2B selective NMDA receptor antagonistsNR-2B selective NMDA receptor antagonistsNR 2B selective NMDA receptor antagonists