Relmada Therapeutics, Inc. (NASDAQ:RLMD), a late-stage biotechnology company addressing diseases of the central nervous system (CNS), announced today the publication of REL-1017 preclinical data in the peer-reviewed journal, Frontiers in Pharmacology. The article is titled, "REL-1017 (Esmethadone), A Novel NMDAR Blocker for the Treatment of MDD is Not Neurotoxic in Sprague-Dawley Rats," and is available online at: Frontiers | REL-1017 (Esmethadone), A Novel NMDAR Blocker for the Treatment of MDD is Not Neurotoxic in Sprague-Dawley Rats | Pharmacology (frontiersin.org).
"These compelling previously presented data confirm that REL-1017 does not produce Olney's lesions, unlike what has been seen in other NMDAR blockers," said Paolo L. Manfredi, M.D., Chief Scientific Officer of Relmada. "The results further contribute to our understanding of the safety profile of REL-1017."
The aim of the study was to determine whether the novel, low affinity, low potency, NMDAR channel blocker, REL-1017, administered once daily via oral gavage for 1–4 days to male and female Sprague-Dawley rats, would induce transient (Olney's lesions) and irreversible (necrosis) pathomorphological changes to the posterior cingulate and retrosplenial brain cortical neurons as compared with animals treated with another NMDAR channel blocker, dizocilpine (MK-801), a positive control.
In REL-1017 treated rats, early Olney's lesions, which usually appear one day after MK-801 treatment, were not observed. Similarly, REL-1017 treated rats did not show necrotic neurons both at the cingulate and olfactory bulb cortex at later time points (Day 3 and 5). This effect is statistically different from what was observed in cortical neurons by using MK-801. Additionally, in contrast with MK-801 treated rats, REL-1017 treated rats did not show evidence of impaired behavior.
These preclinical data, in addition to clinical data to date, have been encouraging to the development of REL-1017 as a potentially safe and effective treatment option for MDD.