Esmethadone Explained

Esmethadone (; developmental code name REL-1017), also known as dextromethadone, is the (S)-enantiomer of methadone. It acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist, among other actions. Unlike levomethadone, it has low affinity for opioid receptors and lacks significant respiratory depressant action and abuse liability.[1] Esmethadone is under development for the treatment of major depressive disorder.[2] As of August 2022, it is in phase 3 clinical trials for this indication.

There is an asymmetric synthesis available to prepare both esmethadone (S-(+)-methadone) and levomethadone (R-(−)-methadone).[3]

References

https://seekingalpha.com/article/4679773?gt=007e6ed9bf2fefc2

Notes and References

  1. Web site: METHADONE . Drug & Chemical Evaluation Section . Drug Enforcement Agency . 14 November 2020.
  2. Web site: Dextromethadone - Cornell University/Relmada Therapeutics - AdisInsight.
  3. Hull JD, Scheinmann F, Turner NJ . Synthesis of optically active methadones, LAAM and bufuralol by lipase-catalysed acylations . Tetrahedron: Asymmetry . 14 . 5 . 567–576 . March 2003 . 10.1016/S0957-4166(03)00019-3 .