Chemistry:Deupsilocin

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Deupsilocin (INN, USAN; former developmental code names HLP003 and CYB0003), also known as deuterated psilocin or as psilocin-d10, is a psychedelic drug of the tryptamine family related to psilocin which is under development for the treatment of major depressive disorder, alcoholism, and other psychiatric disorders.[1][2][3][4][5][6][7] It is taken orally.[1] The drug is a deuterated isotopologue of psilocin with altered pharmacokinetics.[1][3][4][6]

Interactions

Pharmacology

The pharmacodynamic profile of deupsilocin, including its interactions with serotonin receptors and its effects in animals, is similar to that of psilocin.[6] As with psilocin, deupsilocin is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals.[6] However, it was developed to have improved pharmacokinetic properties compared to psilocybin, including reduced variability in circulating levels, a faster onset of action, and a shorter duration.[7]

In humans, deupsilocin has been reported to have 2.2-fold higher peak levels and 3.5-fold higher area-under-the-curve (AUC) levels than psilocybin at equivalent doses.[8] It is said to have a rapid onset of less than 15 minutes and a duration of 4 to 6 hours.[8]

Chemistry

Analogues

In addition to deupsilocin, Helus Pharma has also patented other deuterated psilocin isotopologues.[9] Other deuterated drugs related to deupsilocin include the deuterated dimethyltryptamine (DMT) isotopologues deudimethyltryptamine (HLP004; CYB004; DMT-d10; deudimethyltryptamine) and SPL028 (D2-DMT) and the deuterated phenethylamine HLP005 (CYB005).[3][10]

Research

In 2024, deupsilocin received a breakthrough therapy designation from the U.S. FDA[11] and was in phase 3 clinical trials for major depressive disorder and is in the preclinical stage of development for alcoholism and other psychiatric disorders.[1][2][12] Two phase 3 clinical trials for major depressive disorder are being initiated in November 2024 and February 2025.[1][2][12] The drug is under development by Helus Pharma (formerly Cybin).[1][2][12]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "Deupsilocin". 4 October 2024. https://adisinsight.springer.com/drugs/800062409. 
  2. ↑ 2.0 2.1 2.2 2.3 "Delving into the Latest Updates on CYB-003 with Synapse". 12 October 2024. https://synapse.patsnap.com/drug/dcb535376933495783bad0ae5504a571. 
  3. ↑ 3.0 3.1 3.2 "Key Characteristics and Development of Psychoceuticals: A Review". Int J Mol Sci 23 (24). December 2022. doi:10.3390/ijms232415777. PMID 36555419. 
  4. ↑ 4.0 4.1 "Deuterium in drug discovery: progress, opportunities and challenges". Nat Rev Drug Discov 22 (7): 562–584. July 2023. doi:10.1038/s41573-023-00703-8. PMID 37277503. 
  5. ↑ "Psychedelic renaissance: Revitalized potential therapies for psychiatric disorders". Drug Discov Today 28 (12). December 2023. doi:10.1016/j.drudis.2023.103818. PMID 37925136. 
  6. ↑ 6.0 6.1 6.2 6.3 "ACNP 61st Annual Meeting: Poster Abstracts P271-P540: P361. In Vitro and In Vivo Profile of CYB003: A Novel, Deuterated Psilocybin Analog for the Potential Treatment of Major Depressive Disorder". Neuropsychopharmacology 47 (Suppl 1): 220–370 (271). December 2022. doi:10.1038/s41386-022-01485-0. PMID 36456694. PMC 9714399. https://cybin.com/wp-content/uploads/2023/09/ACNP_2022_CYB003_Poster-1.pdf. 
  7. ↑ 7.0 7.1 "ACNP 61st Annual Meeting: Poster Abstracts P271-P540: P362. Pharmacokinetic Profile of CYB003: A Novel, Deuterated Psilocybin Analog for the Potential Treatment of Major Depressive Disorder". Neuropsychopharmacology 47 (Suppl 1): 220–370 (271–272). December 2022. doi:10.1038/s41386-022-01485-0. PMID 36456694. PMC 9714399. https://cybin.com/wp-content/uploads/2023/09/ACNP-2022-CYB003-Poster-2.pdf. 
  8. ↑ 8.0 8.1 "Corporate Presentation - Helping Minds Heal". March 2026. https://s28.q4cdn.com/259445127/files/doc_presentations/2026/Mar/18/Helus-Corporate-Deck-March-18-2026-Final.pdf. 
  9. ↑ "Deuterated tryptamine derivatives and methods of use". 17 July 2023. https://patents.google.com/patent/US20230357147A1/en. "Binding affinity (Ki) and functional potency (EC50) values of PI and PI-α-d2 are summarized in Table 1. Deuteration was found to have little effect on the affinity and function at key receptor targets. [...] TABLE 1: PI and PI-α,α-d2 Affinities and Functions at Target Serotonin Receptors [...]" 
  10. ↑ "Next-generation psychedelics: should new agents skip the trip?". Nat Biotechnol 42 (6): 827–830. June 2024. doi:10.1038/s41587-024-02285-1. PMID 38831049. 
  11. ↑ Jenkins, Cassandra (19 March 2024). "FDA grants breakthrough designation to psilocybin analog for major depressive disorder". https://www.healio.com/news/psychiatry/20240319/fda-grants-breakthrough-designation-to-psilocybin-analog-for-major-depressive-disorder. 
  12. ↑ 12.0 12.1 12.2 Kuntz, Leah (10 February 2025). "CYB003 for the Adjunctive Treatment of Major Depressive Disorder". https://www.psychiatrictimes.com/view/cyb003-for-the-adjunctive-treatment-of-major-depressive-disorder. 



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