GM-3009 is a κ-opioid receptor (KOR) agonist and noribogaine analogue which is under development for the treatment of opioid-related disorders.[1][3][2] 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.[2] In contrast to noribogaine, it did not show pro-arrhythmic effects in fresh human ventricular cardiomyocytes ex vivo.[2] GM-3009 produces antinociceptive effects and dose-dependently reduces oxycodone self-administration in rodents.[2] It is being developed by Gilgamesh Pharmaceuticals.[1][3] As of June 2024, it is in the preclinical research stage of development.[1][3] The exact chemical structure of GM-3009 does not yet appear to have been disclosed.[1]
See also
References
- ^ a b c d e f "GM 3009". AdisInsight. 19 June 2024. Retrieved 16 February 2025.
- ^ a b c d e Cunningham M, Nicholson K, Hughes Z, Sames D, Kruegel A (2023). "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" (PDF). Neuropsychopharmacology. 48 (S1): 355–495 (478–478). doi:10.1038/s41386-023-01757-3. ISSN 0893-133X. PMC 10729598. PMID 38040811. Retrieved 16 February 2025.
- ^ a b c "Delving into the Latest Updates on GM-3009 with Synapse". Synapse. 23 January 2025. Retrieved 16 February 2025.