Chemistry:GM-3009
GM-3009 is a κ-opioid receptor (KOR) agonist and noribogaine analogue which is under development for the treatment of opioid-related disorders.[1][2][3] Its route of administration is unspecified.[1]
The drug is a highly potent agonist of the human KOR, with an affinity (Ki) of 0.9 nM or 87.3 nM depending on the radioligand and an EC50 of 0.8 nM.[3] In contrast to noribogaine, it did not show pro-arrhythmic effects in fresh human ventricular cardiomyocytes ex vivo.[3] GM-3009 produces antinociceptive effects and dose-dependently reduces oxycodone self-administration in rodents.[3]
It is being developed by Gilgamesh Pharmaceuticals.[1][2] As of June 2024, it is in the preclinical research stage of development.[1][2] The exact chemical structure of GM-3009 does not yet appear to have been disclosed.[1] However, it is known to be an "oxa-iboga" derivative.[4] Oxa-ibogaine analogues have notably been patented and studied by Dalibor Sames and colleagues, with Sames being a co-founder of Gilgamesh Pharmaceuticals.[5][6][7]
See also
- List of investigational hallucinogens and entactogens
- Oxa-noribogaine
- 4-Allyl-6-oxa-noribogainalog
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "GM 3009". 19 June 2024. https://adisinsight.springer.com/drugs/800077750.
- ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on GM-3009 with Synapse". 23 January 2025. https://synapse.patsnap.com/drug/73f39db6d983477c95dd040cb74052d2.
- ↑ 3.0 3.1 3.2 3.3 "ACNP 62nd Annual Meeting: Poster Abstracts P501 – P753: P720. GM-3009 is a Novel Noribogaine Analog That Disrupts Opioid Self-Administration in Rats Via Agonism of Kappa Opioid Receptors Without Pro-Arrhythmic Effects on Human Cardiomyocytes". Neuropsychopharmacology 48 (S1): 355–495 (478–478). 2023. doi:10.1038/s41386-023-01757-3. ISSN 0893-133X. PMID 38040811. PMC 10729598. https://www.nature.com/articles/s41386-023-01757-3.pdf. Retrieved 16 February 2025.
- ↑ Gerard Joseph Marek (2024). "Development of a Safer and More Effective Ibogaine Analog for the Treatment of Opioid Use Disorder". https://reporter.nih.gov/project-details/10835278. "To leverage ibogaine’s potential as an OUD therapeutic and address the risks to patient safety, we have developed a new class of synthetic iboga alkaloids, named “oxa-iboga”. These compounds show no pro-arrhythmic potential, no neurotoxic effects, and enhanced efficacy in OUD-relevant preclinical behavioral assays compared to ibogaine. We propose to advance one of these compounds, GM-3009, into clinical studies by advancing GMP-manufacturing and formulation of GM-3009, completing IND-enabling toxicity studies, and determining the expected therapeutic exposures of GM-3009 and target engagement via translational biomarkers."
- ↑ "Oxa-ibogaine analogues for treatment of substance use disorders". 17 February 2022. https://patents.google.com/patent/US20240150372A1/en.
- ↑ "Oxa-ibogaine inspired analogues for treatment of neurological and psychiatric disorders". 7 August 2023. https://patents.google.com/patent/US20230382919A1/en.
- ↑ "Oxa-Iboga alkaloids lack cardiac risk and disrupt opioid use in animal models". Nat Commun 15 (1): 8118. September 2024. doi:10.1038/s41467-024-51856-y. PMID 39304653.
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