Pharmacokinetics, Safety, and Tolerability of Intramuscular 5-MeO-DMT in Healthy Volunteers

NCT ID: NCT05698095

Last Updated: 2023-11-30

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

54 participants

Study Classification

INTERVENTIONAL

Study Start Date

2022-12-27

Study Completion Date

2023-09-07

Brief Summary

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The primary objective of the study is to assess the pharmacokinetics, safety, and tolerability of a single-dose and multiple-doses of 5-MeO-DMT administered by intramuscular (IM) injections in healthy subjects.

Detailed Description

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This study is a phase 1, first-in-human, double-blind, placebo-controlled, randomized, single-dose and multiple-ascending-dose study of 5-MeO-DMT administered by intramuscular injection in 54 healthy subjects (adult male and/or females, 18-65 years of age). Subjects will be randomized 6:1 to receive 5-MeO-DMT or placebo.

Conditions

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Pharmacokinetics Safety Tolerability

Keywords

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5-MeO-DMT Psychedelics Safety Pharmacokinetics First-in-human 5-methoxy-N,N-dimethyltryptamine

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

SEQUENTIAL

This study will include separate single- and multiple-dose parts.

Single-dose part:

A double-blind, placebo-controlled, randomized, sequential-group design with 5-MeO-DMT administered by intramuscular injection in 6 cohorts of 6 subjects (randomized as 5 active and 1 placebo subject(s) per group).

Multiple-dose part:

A double-blind, placebo-controlled, randomized, sequential-group design with 5-MeO-DMT administered by intramuscular injection in up to two doses within a single day (3-hour interval) with two different dose levels (6 subjects per group).
Primary Study Purpose

OTHER

Blinding Strategy

TRIPLE

Participants Caregivers Investigators

Study Groups

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Cohort 1 - 0.5 mg single-dose

A single 0.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 2 - 2.5 mg single-dose

A single 2.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 3 - 4.5 mg single-dose

A single 4.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 4 - 7 mg single-dose

A single 7 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 5 - 10 mg single-dose

A single 10 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 6 - 13 mg single-dose

A single 5-MeO-DMT 13 mg or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 7 - multiple-dose, 3 hour interval

Administration of up to two 5-MeO-DMT (2.5 mg followed by 4.5 mg) or placebo doses administered intramuscularly within a single day with a 3 hour dose interval (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 8 - multiple-dose, 3 hour interval

Administration of up to two 5-MeO-DMT (2.5 mg followed by 7 mg) or placebo doses administered intramuscularly within a single day with a 3 hour dose interval (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Cohort 9 - multiple-dose, 3 hour interval

Administration of up to two 5-MeO-DMT (2.5 mg followed by 10.5 mg) or placebo doses administered intramuscularly within a single day with a 3 hour dose interval (randomized as 5 active and 1 placebo subject).

Group Type EXPERIMENTAL

5-methoxy-N,N-dimethyltryptamine succinate salt

Intervention Type DRUG

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Placebo

Intervention Type DRUG

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Interventions

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5-methoxy-N,N-dimethyltryptamine succinate salt

The 5-MeO-DMT drug product is comprised of the appropriate concentration of 5-MeO-DMT succinate salt drug substance in solution with 0.9% sodium chloride injection solution (USP) in a 5 mL glass vial, and is administered intramuscularly.

Intervention Type DRUG

Placebo

The placebo is commercially available 0.9% sodium chloride solution (USP) for injection. The placebo is provided by the pharmacy in single-use sterile syringes of the appropriate dose.

Intervention Type DRUG

Other Intervention Names

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5-MeO-DMT succinate salt 5-MeO-DMT 0.9% sodium chloride solution (USP)

Eligibility Criteria

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Inclusion Criteria

* Healthy adult male or female.
* Aged at least 18 years but not older than 65 years, inclusive.
* Body mass index (BMI) within 18.0 kg/m2 to 32.0 kg/m2, inclusive.

Exclusion Criteria

* History of significant hypersensitivity to the IP or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (like angioedema) to any drugs.
* Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, or endocrine disorders, as determined by the investigator (or designee).
* Participants who, in the opinion of the investigator (or designee), should not participate in this study.
* Participant is participating in another study with a medical device or IP within the last 30 days prior to first study drug administration.
Minimum Eligible Age

18 Years

Maximum Eligible Age

65 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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Usona Institute

OTHER

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Locations

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Altasciences Clinical Kansas, Inc

Overland Park, Kansas, United States

Site Status

Countries

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United States

References

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Reckweg J, Mason NL, van Leeuwen C, Toennes SW, Terwey TH, Ramaekers JG. A Phase 1, Dose-Ranging Study to Assess Safety and Psychoactive Effects of a Vaporized 5-Methoxy-N, N-Dimethyltryptamine Formulation (GH001) in Healthy Volunteers. Front Pharmacol. 2021 Nov 25;12:760671. doi: 10.3389/fphar.2021.760671. eCollection 2021.

Reference Type BACKGROUND
PMID: 34912222 (View on PubMed)

Shen HW, Jiang XL, Winter JC, Yu AM. Psychedelic 5-methoxy-N,N-dimethyltryptamine: metabolism, pharmacokinetics, drug interactions, and pharmacological actions. Curr Drug Metab. 2010 Oct;11(8):659-66. doi: 10.2174/138920010794233495.

Reference Type BACKGROUND
PMID: 20942780 (View on PubMed)

Barsuglia J, Davis AK, Palmer R, Lancelotta R, Windham-Herman AM, Peterson K, Polanco M, Grant R, Griffiths RR. Intensity of Mystical Experiences Occasioned by 5-MeO-DMT and Comparison With a Prior Psilocybin Study. Front Psychol. 2018 Dec 6;9:2459. doi: 10.3389/fpsyg.2018.02459. eCollection 2018.

Reference Type BACKGROUND
PMID: 30574112 (View on PubMed)

Davis AK, Barsuglia JP, Lancelotta R, Grant RM, Renn E. The epidemiology of 5-methoxy- N, N-dimethyltryptamine (5-MeO-DMT) use: Benefits, consequences, patterns of use, subjective effects, and reasons for consumption. J Psychopharmacol. 2018 Jul;32(7):779-792. doi: 10.1177/0269881118769063. Epub 2018 Apr 30.

Reference Type BACKGROUND
PMID: 29708042 (View on PubMed)

Ermakova AO, Dunbar F, Rucker J, Johnson MW. A narrative synthesis of research with 5-MeO-DMT. J Psychopharmacol. 2022 Mar;36(3):273-294. doi: 10.1177/02698811211050543. Epub 2021 Oct 19.

Reference Type BACKGROUND
PMID: 34666554 (View on PubMed)

Uthaug MV, Lancelotta R, van Oorsouw K, Kuypers KPC, Mason N, Rak J, Sulakova A, Jurok R, Maryska M, Kuchar M, Palenicek T, Riba J, Ramaekers JG. A single inhalation of vapor from dried toad secretion containing 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) in a naturalistic setting is related to sustained enhancement of satisfaction with life, mindfulness-related capacities, and a decrement of psychopathological symptoms. Psychopharmacology (Berl). 2019 Sep;236(9):2653-2666. doi: 10.1007/s00213-019-05236-w. Epub 2019 Apr 13.

Reference Type BACKGROUND
PMID: 30982127 (View on PubMed)

Sherwood AM, Claveau R, Lancelotta R, Kaylo KW, Lenoch K. Synthesis and Characterization of 5-MeO-DMT Succinate for Clinical Use. ACS Omega. 2020 Dec 2;5(49):32067-32075. doi: 10.1021/acsomega.0c05099. eCollection 2020 Dec 15.

Reference Type BACKGROUND
PMID: 33344861 (View on PubMed)

Other Identifiers

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MEO101

Identifier Type: -

Identifier Source: org_study_id