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HLP004

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For other uses, see Deudimethyltryptamine (disambiguation).
HLP004
Clinical data
Other namesHLP004; HLP-004; CYB004; CYB-004; Deuterated dimethyltryptamine; Deuterated DMT; dDMT
Routes of
administration		Inhalation, intravenous[1][2]
Drug classSerotonergic psychedelic; Serotonin receptor agonist[1][3]
Pharmacokinetic data
Elimination half-life37–40 minutes[4]
Duration of action~40 minutes[4]

HLP004, or HLP-004, also known as deuterated dimethyltryptamine (dDMT) and formerly as CYB004, is a serotonergic psychedelic related to dimethyltryptamine (DMT) which is under development for the treatment of generalized anxiety disorder.[1][5][2][3][4] It is administered by inhalation or intravenous injection.[1][2] The drug is a tryptamine derivative and is a deuterated analogue and form of DMT.[1][5][3]

Interactions

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See also: Psychedelic drug § Interactions, and Trip killer § Serotonergic psychedelic antidotes

Pharmacology

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The pharmacodynamic profile of HLP004, including its interactions with serotonin receptors and its effects in animals, is similar to that of DMT.[3] As with DMT, HLP004 is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals.[1][6][3] However, HLP004, due to its deuteration, is more resistant to metabolism than DMT and shows a longer elimination half-life (by 2.5- to 2.9-fold) and slower clearance (by 38 to 55%) in animals.[3] The brain to plasma ratio of HLP004 was also increased (by 30%) relative to DMT, indicating slightly greater central permeability as well.[3]

The pharmacokinetics and effects of HLP004 in humans have been studied and compared with those of DMT.[4] Its elimination half-life was 37 to 40 minutes and its duration was approximately 40 minutes.[4] For comparison, the half-life of DMT in humans has been reported to be 9 to 12 minutes (range 5–19 minutes).[7][8] HLP004 produced more robust psychedelic effects than DMT at lower concentrations.[4]

Chemistry

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Deudimethyltryptamine (INNTooltip International Nonproprietary Name; DMT-d10) structure.

The exact chemical structure of HLP004 (i.e., which specific hydrogen atoms have been deuterated) does not yet seem to have been disclosed.[1] However, Helus Pharma (formerly Cybin) patented deuterated tryptamines, including deuterated forms of DMT like DMT-d10 (decadeutero-DMT; CAS no. 2742678-60-8), in 2023.[9][10] In addition, DMT-d10 was given the INNTooltip International Nonproprietary Name deudimethyltryptamine in January 2026.[11] Other deuterated drugs related to HLP004 or DMT-d10 include the deuterated DMT analogue SPL028 (D2-DMT; α,α-dideutero-DMT), the deuterated psilocybin analogue HLP003 (CYB003) (possibly deupsilocin or d10-psilocin), and the deuterated phenethylamine HLP005 (CYB005).[6][2]

Research

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As of August 2024, HLP004 is in phase 2 clinical trials for generalized anxiety disorder.[1][5] It was also under development for the treatment of substance-related disorders and of other psychiatric disorders, but development for these indications was discontinued.[1] The drug is under development by Helus Pharma (formerly Cybin).[1][5]

See also

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References

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  1. ^ a b c d e f g h i j "CYB 004". AdisInsight. 14 August 2024. Retrieved 28 October 2024.
  2. ^ a b c d Peplow M (June 2024). "Next-generation psychedelics: should new agents skip the trip?". Nature Biotechnology. 42 (6): 827–830. doi:10.1038/s41587-024-02285-1. PMID 38831049. Cybin's pipeline also includes CYB004, a deuterated analog of DMT. When given intravenously, DMT itself is rapidly metabolized and causes an intense trip that lasts less than 20 minutes, which may be too brief to be an effective therapy. In contrast, a single intravenous injection of CYB004 produces a 90-minute trip, and Cybin is about to start recruiting patients to a phase 2 trial of the drug to treat generalized anxiety disorder.
  3. ^ a b c d e f g Varty G, Morgan M, Giardino O, Krakowsky J, Mueller T, Canal C, et al. (December 2023). "ACNP 62nd Annual Meeting: Poster Abstracts P1 - P250: P80. Preclinical Characterization of CYB004: A Novel, Deuterated N,N-Dimethyltryptamine (DMT) Analog for the Potential Treatment of Generalized Anxiety Disorder (GAD)". Neuropsychopharmacology. 48 (Suppl 1). Springer Science and Business Media LLC: 63–210 (109–110). doi:10.1038/s41386-023-01755-5. PMC 10729595. PMID 38040809.
  4. ^ a b c d e f Inamdar A, van der Heijden K, Nathan P, Reichelt A, Hegle A, Otto M, et al. (December 2023). "ACNP 62nd Annual Meeting: Poster Abstracts P251 – P500: P425. Early Clinical Development of a Deuterated N,N-Dimethyltryptamine (DMT) Analog for the Treatment of Mental Health Conditions" (PDF). Neuropsychopharmacology. 48 (Suppl 1): 211–354 (310–311). doi:10.1038/s41386-023-01756-4. PMC 10729596. PMID 38040810.
  5. ^ a b c d "Delving into the Latest Updates on Deuterated dtryptamine with Synapse". Synapse. 27 October 2024. Retrieved 28 October 2024.
  6. ^ a b Cano GH, Dean J, Abreu SP, Rodríguez AH, Abbasi C, Hinson M, et al. (December 2022). "Key Characteristics and Development of Psychoceuticals: A Review". International Journal of Molecular Sciences. 23 (24) 15777. doi:10.3390/ijms232415777. PMC 9779201. PMID 36555419.
  7. ^ Good M, Joel Z, Benway T, Routledge C, Timmermann C, Erritzoe D, et al. (May 2023). "Pharmacokinetics of N,N-dimethyltryptamine in Humans". European Journal of Drug Metabolism and Pharmacokinetics. 48 (3): 311–327. doi:10.1007/s13318-023-00822-y. PMC 10122081. PMID 37086340.
  8. ^ van der Heijden KV, Otto ME, Schoones JW, van Esdonk MJ, Borghans LG, van Hasselt JG, et al. (February 2025). "Clinical Pharmacokinetics of N,N-Dimethyltryptamine (DMT): A Systematic Review and Post-hoc Analysis". Clin Pharmacokinet. 64 (2): 215–227. doi:10.1007/s40262-024-01450-8. PMC 11782443. PMID 39838235.
  9. ^ US 2023/0357147, Nivorozhkin A, Palfreyman M, "Deuterated tryptamine derivatives and methods of use", published 8 October 2024, assigned to Cybin IRL Ltd. 
  10. ^ "1,1,2,2-tetradeuterio-2-(1H-indol-3-yl)-N,N-bis(trideuteriomethyl)ethanamine". PubChem. Retrieved 19 February 2026.
  11. ^ https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl134.pdf
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