Next generation NMDAR modulators for CNS disorders
Esmethadone (REL-1017) is an investigational compound. Safety and efficacy have not been established, and no regulatory authority has approved this product for any indication. Statements herein reflect interpretations of published or presented data.
Esmethadone (REL-1017): a non-dissociative oral NMDAR modulator and neuroplastogen in development for the adjunctive treatment of MDD and other CNS disorders
Esmethadone (REL-1017) is a novel circuit- and region-specific uncompetitive NMDAR modulator and neuroplastogen selective for hyperactive GluN2D-containing subtypes.
Esmethadone is under development as a rapid acting, adjunctive, oral, once-daily, antidepressant for patients with inadequate response to first line therapy.
Esmethadone has completed Phase 1, Phase 2 and Phase З clinical trials, totaling over 1000 individual patient exposures. Across all trials, esmethadone was safe and well tolerated, with no meaningful opioid-like effects, ketamine-like effects or abuse liability, confirming state of the art studies indicating lack of psychoactive side effects and lack of meaningful abuse potential.
The development of REL-1017 is at a turning point
On July 22, 2025, Levomecor Inc. acquired a perpetual, worldwide, exclusive license to the REL-1017 program.
With a patient-centered vision, the Levomecor team is focused on preparing the esmethadone program for NDA readiness.
Strongly supported by the scientific and medical community
The scientific community is strongly supportive of the esmethadone program. The esmethadone literature is authored by renowned experts.
There is an urgent medical need for novel, rapid acting, safe and well tolerated oral adjunctive antidepressant for patients with MDD who do not respond to first line therapy.