CYB003

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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.
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