Data show that d-Methadone produces antidepressant activity comparable to ketamine after single dose administration in a well-validated model.
Relmada Therapeutics, Inc. (OTCQB: RLMD), a clinical-stage company developing novel therapies for the treatment of chronic pain, today announced the results of an in vivo study showing that administration of d-Methadone (REL-1017), a N-methyl-d-aspartate (NMDA) receptor antagonist, results in antidepressant-like effects. Results are shown to be comparable to those achieved in similar treatment models using ketamine.
"This study is the first to
clearly demonstrate that d-Methadone exhibits antidepressant-like
effects in a well-validated treatment model to predict antidepressant
activity," said Richard Mangano,
Ph.D., chief scientific officer of Relmada. "Ketamine, also a
noncompetitive NMDA receptor antagonist, has been thoroughly
characterized in this model and has demonstrated rapid onset of activity
in several clinical studies, but has also been shown in multiple
studies to present a high risk of toxicity. Combined with the results of
our recent Phase I single and multiple ascending dose studies, the
encouraging results of this in vivo study support our belief that
d-Methadone warrants further evaluation in a Phase II study as an
effective treatment for depression."
The purpose of this study was to determine
whether d-Methadone elicits antidepressant-like effects after a single
administration in a well-validated animal model to predict
antidepressant effects, the forced swim test. In the study, male Sprague Dawley
rats were administered single doses of vehicle, ketamine, or
d-Methadone on day one (after habituation; 24 hours prior to forced swim
testing). At all doses tested, d-Methadone significantly decreased
immobility of the rats compared to the vehicle, suggesting
antidepressant-like activity. In addition, the effect of d-Methadone on
immobility at the two highest doses tested was larger than the effect
seen with ketamine. Importantly, the effects of d-Methadone in the
forced swim test were not confounded by any changes in the locomotor
activity of the rats.
About d-Methadone (REL-1017)
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 it is expected that REL-1017 will have a role in
pain management by blocking this activity. In contrast, racemic
methadone is a long-acting narcotic used in the treatment of various
pain states and as a substitution therapy in opioid addiction and
associated with typical opioid side effects.
About Relmada Therapeutics, Inc.
Relmada Therapeutics is a
clinical-stage, publicly traded specialty pharmaceutical company
developing novel versions of proven drug products together with new
chemical entities that potentially address areas of high unmet medical
need in the treatment of pain. The Company has a diversified portfolio
of four products at various stages of development, including d-Methadone
(REL-1017), an N-methyl-D-aspartate (NMDA) receptor antagonist for
neuropathic pain; topical mepivacaine (REL-1021), an orphan drug
designated topical formulation of the local anesthetic mepivacaine; oral
buprenorphine (REL-1028),an oral dosage form of the opioid analgesic
buprenorphine; and LevoCap ER (REL-1015), an abuse resistant, sustained
release dosage form of the opioid analgesic levorphanol. The Company's
product development efforts are guided by the internationally recognized
scientific expertise of its research team. The Company's approach is
expected to reduce clinical development risks and costs while
potentially delivering valuable products to address areas of high unmet
medical needs. For more information, please visit Relmada's website at: www.relmada.com.
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