In a news release earlier this week, Relmada Therapeutics, Inc. announced the completion of its multiple ascending dose (MAD) study of d-Methadone (dextromethadone, REL-1017), its novel, N-methyl-D-aspartate ("NMDA") receptor antagonist being developed for the treatment of neuropathic pain. The company stated that the results demonstrated a potential therapeutic dosing regimen for d-Methadone with a favorable side effect and tolerability profile. Based on this outcome, the company plans design and implementation of a Phase II proof-of-concept study of neuropathic pain during the first half of 2016. Sergio Traversa, PharmD, MBA, and CEO of Relmada Therapeutics said "Given the high level of need for more effective and better-tolerated therapies for chronic neuropathic pain, we remain committed to advancing d-Methadone with the goal of providing a novel treatment option with virtually no opioid-related adverse effects for patients suffering from a wide range of pain syndromes."
As a single isomer, d-Methadone (REL-1017) has been shown to possess NMDA antagonist properties with virtually no opioid activity at the expected therapeutic doses. The activation of NMDA receptors has been associated with neuropathic pain and the company expects that REL-1017 will have a role in pain management by blocking this activity. The goal of the just completed study was to evaluate the safety, tolerability, pharmacodynamics and pharmacokinetics of oral multiple ascending doses of d-Methadone in healthy subjects. Read a news release about the study results and future research here.