esmethadone

Esmethadone, also known as REL-1017 or dextromethadone, is the (S)-enantiomer of the racemic drug methadone. Unlike its (R)-enantiomer counterpart, esmethadone exhibits very low affinity for mu-opioid receptors, which minimizes the risk of opioid-related side effects such as respiratory depression, sedation, and physical dependence. Its primary therapeutic action is as a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. Developed by Relmada Therapeutics, esmethadone is currently in Phase 3 clinical trials as an adjunctive oral treatment for major depressive disorder (MDD). It is designed to provide rapid and sustained antidepressant activity by modulating the glutamatergic system, offering a potentially safer and more convenient alternative to other NMDA-targeting therapies like ketamine.

Brand names

REL-1017REL1017REL 1017

Other names

(S)-methadonedextromethadone(+)-methadoneS-(+)-methadone