CYB003

Last updated

CYB003
Clinical data
Other namesCYB-003; deuterated psilocybin analogue; deuterated psilocin analogue
Routes of
administration
By mouth [1]
Drug class Serotonergic psychedelic [1] [2]
ATC code
  • None
Pharmacokinetic data
Onset of action 30 minutes (Cmax) (rats) [3]
Elimination half-life 45 minutes (rats) [3]

CYB003, or CYB-003, also known as deuterated psilocybin analogue, is a serotonergic psychedelic related to psilocybin which is under development for the treatment of major depressive disorder, alcoholism, and other psychiatric disorders. [1] [4] [5] [6] [7] [2] [3] It is taken by mouth. [1]

Contents

It is a tryptamine derivative and is a deuterated analogue of psilocybin and psilocin. [1] [5] [6] [2] The pharmacodynamic profile of CYB003, including its interactions with serotonin receptors and its effects in animals, is similar to that of psilocin. [2] As with psilocin, CYB003 is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals. [2] 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. [3]

In 2024, CYB003 received a breakthrough therapy designation from the U.S. FDA [8] 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] [4] [9] Two phase 3 clinical trials for major depressive disorder are being initiated in November 2024 and February 2025. [1] [4] [9] The drug is under development by Cybin. [1] [4] [9] The chemical structure of CYB003 has not yet been disclosed. [6] [5] However, Cybin patented deuterated tryptamines including the dideuterated psilocin analogue PI-α,α-d2 (psilocin dideuterated at the α carbon) in 2023. [10] Other related drugs include the deuterated tryptamine CYB004, the deuterated phenethylamine CYB005, and the phenethylamine CYB210010. [5] [11]

An INN Tooltip International Nonproprietary Name of deupsilocin for a deuterated form of psilocin called d10-psilocin with CAS number 1435934-64-7 was proposed in 2023 and recommended in 2024. [12] [13] [14] This deuterated analogue of psilocin was patented in 2021 by Lennham Pharmaceuticals. [14]

See also

References

  1. 1 2 3 4 5 6 7 8 "CYB 003". AdisInsight. 4 October 2024. Retrieved 23 October 2024.
  2. 1 2 3 4 5 Palfreyman M, Krakowsky J, Morgan M, Canal C, Pathare P, Avery K, et al. (December 2022). "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" (PDF). Neuropsychopharmacology. 47 (Suppl 1): 220–370 (271). doi:10.1038/s41386-022-01485-0. PMC   9714399 . PMID   36456694.
  3. 1 2 3 4 Inamdar A, Morgan M, Krakowsky J, Reichelt A, Canal C, Mueller T, et al. (December 2022). "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" (PDF). Neuropsychopharmacology. 47 (Suppl 1): 220–370 (271–272). doi:10.1038/s41386-022-01485-0. PMC   9714399 . PMID   36456694.
  4. 1 2 3 4 "Delving into the Latest Updates on CYB-003 with Synapse". Synapse. 12 October 2024. Retrieved 23 October 2024.
  5. 1 2 3 4 Cano GH, Dean J, Abreu SP, Rodríguez AH, Abbasi C, Hinson M, et al. (December 2022). "Key Characteristics and Development of Psychoceuticals: A Review". Int J Mol Sci. 23 (24): 15777. doi: 10.3390/ijms232415777 . PMC   9779201 . PMID   36555419.
  6. 1 2 3 Di Martino RM, Maxwell BD, Pirali T (July 2023). "Deuterium in drug discovery: progress, opportunities and challenges". Nat Rev Drug Discov. 22 (7): 562–584. doi:10.1038/s41573-023-00703-8. PMC   10241557 . PMID   37277503.
  7. Rhee TG, Davoudian PA, Sanacora G, Wilkinson ST (December 2023). "Psychedelic renaissance: Revitalized potential therapies for psychiatric disorders". Drug Discov Today. 28 (12) 103818. doi:10.1016/j.drudis.2023.103818. PMID   37925136.
  8. Jenkins C (19 March 2024). "FDA grants breakthrough designation to psilocybin analog for major depressive disorder". Healio. Retrieved 7 August 2025.
  9. 1 2 3 Kuntz L (10 February 2025). "CYB003 for the Adjunctive Treatment of Major Depressive Disorder". Psychiatric Times. Retrieved 7 August 2025.
  10. "Deuterated tryptamine derivatives and methods of use". Google Patents. 17 July 2023. Retrieved 23 October 2024. 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 [...]
  11. Peplow M (June 2024). "Next-generation psychedelics: should new agents skip the trip?". Nat Biotechnol. 42 (6): 827–830. doi:10.1038/s41587-024-02285-1. PMID   38831049.
  12. deupsilocinum deupsilocin 3-[2-{di[(2H3)methyl]amino}(2H4)ethyl]-1H-indol-4-ol psychodysleptic [...] C12H62H10N2O 1435934-64-7 https://www.who.int/docs/default-source/international-nonproprietary-names-(inn)/pl129.pdf#page=35
  13. deupsilocinum deupsilocin 3-[2-{di[(2H3)methyl]amino}(2H4)ethyl]-1H-indol-4-ol [...] C12H62H10N2O https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-%28inn%29/rl91.pdf
  14. 1 2 US 11000534,Bradford Sippy,"Deuterated Derivatives of Psilocybin and Uses Thereof",published 11 May 2021,issued 11 May 2021, assigned to Lennham Pharmaceuticals, Inc.