REL-1017 (dextromethadone, d-Methadone)

Our most-advanced new chemical entity, d-methadone (dextromethadone, REL-1017), is a novel, N-methyl-D-aspartate (NMDA) receptor antagonist being developed for the treatment of depression and neuropathic pain, and/or other potential indications. As a single isomer of racemic methadone, d-Methadone has been shown to possess NMDA antagonist properties with virtually no opioid activity or ketamine-like toxicities at the expected therapeutic doses. The activation of NMDA receptors has been associated with depression and neuropathic pain and it is expected that d-Methadone will have a therapeutic role by blocking this activity. In contrast, racemic methadone is a long-acting narcotic producing typical opioid side effects used in the treatment of various pain states and as a substitution therapy in opioid addiction.

d-Methadone Pipeline

Phase 1
Phase 2
Phase 3
Preclinical Phase 1 Phase 2 Phase 3

Projected stage of development in 12-24 months

Key Points

  1. Rapid Onset
    1. NMDA antagonists have demonstrated rapid onset (within ~24 hours) of antidepressant activity. Currently approved products take several weeks to show effectiveness.
  2. Better Efficacy; Novel MOA
    1. NMDA antagonists like d-Methadone may represent a new treatment paradigm. Traditional antidepressant response rates in controlled trials estimated at ~54% and real-world effectiveness data suggest a somewhat lower rate.
  3. Enhanced Safety
    1. Ketamine and current antidepressant drugs associated with significant side effects. d-Methadone safety demonstrated across three human clinical trials.

Market Potential

The World Health Organization (WHO) has estimated that CNS diseases affect nearly 2 billion people globally, making up approximately 40% of total disease burden (based on disability adjusted life years), compared with 13% for cancer and 12% for cardiovascular disease.

The depression treatment market is segmented on the basis of antidepressants drugs, devices and therapies. Antidepressants are the largest and most popular market segment. According to Research and Markets, every year more than five billion antidepressant prescriptions are written globally. The antidepressants segment consists of big pharmaceuticals companies like Eli Lily, Pfizer, GlaxoSmithKline and Forest Laboratories. All these companies are branded drug manufacturers. Some of the popular drugs produced by these companies are Cymbalta (Eli Lily) and Effexor and Pristiq (Pfizer).

The pain market is well established, with many pharmaceutical companies marketing innovative products as well as generic versions of older, non-patent protected products. In 2014, according to data from IMS Health, there were 328 million pain prescriptions representing $13 billion in annual sales in the U.S.

By the Numbers

2 Billion

The World Health Organization (WHO) estimate for people affected by CNS diseases globally


Total disease burden compared with 13% for cancer and 12% for cardiovascular disease

Redefining the Market

  • Leveraging research from Cornell University and Memorial Sloan Kettering Cancer Center
  • May represent a new stand- alone class of drugs with blockbuster potential in treating depression and chronic pain
  • Existing methadone usage in pain treatment provides a springboard for commercial success

Latest News

New York, NY July 27, 2015

Relmada Therapeutics Announces Filing of Clinical Trial Application in Canada for Multiple Ascending Dose Study with Promising NMDA Receptor Antagonist d-Methadone

Relmada Therapeutics, Inc. announces it has filed a Clinical Trial Application (CTA) with Heath Canada to conduct a multiple ascending dose (MAD) clinical study with d-Methadone (dextromethadone, REL-1017), its novel, N-methyl-D-aspartate (NMDA) receptor antagonist being developed for the treatment of neuropathic pain.

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