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

Phase 1

Completed

• Conditions: Pharmacokinetics; Safety; Tolerability
• Interventions: Drug: 5-methoxy-N,N-dimethyltryptamine succinate salt; Drug: Placebo

• Registration Number: NCT05698095
• Lead Sponsor: Usona Institute

Brief Summary

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

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.

Study Timeline

• Study Start: 2022-12-27
• Study First Submitted: 2023-01-05
• Study First Submitted QC: 2023-01-13
• Study First Posted: 2023-01-26
• Primary Completion: 2023-09-07
• Study Completion: 2023-09-07
• Status Verified: 2023-11
• Last Update Submitted: 2023-11-29
• Last Update Posted: 2023-11-30

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 54

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.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Cohort 2 - 2.5 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 2.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 3 - 4.5 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 4.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 1 - 0.5 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 0.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 1 - 0.5 mg single-dose	Placebo	A single 0.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 2 - 2.5 mg single-dose	Placebo	A single 2.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 3 - 4.5 mg single-dose	Placebo	A single 4.5 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 4 - 7 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 7 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 4 - 7 mg single-dose	Placebo	A single 7 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 5 - 10 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 10 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 5 - 10 mg single-dose	Placebo	A single 10 mg 5-MeO-DMT or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 6 - 13 mg single-dose	5-methoxy-N,N-dimethyltryptamine succinate salt	A single 5-MeO-DMT 13 mg or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 6 - 13 mg single-dose	Placebo	A single 5-MeO-DMT 13 mg or placebo dose administered intramuscularly (randomized as 5 active and 1 placebo subject).
Cohort 7 - multiple-dose, 3 hour interval	5-methoxy-N,N-dimethyltryptamine succinate salt	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).
Cohort 7 - multiple-dose, 3 hour interval	Placebo	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).
Cohort 8 - multiple-dose, 3 hour interval	5-methoxy-N,N-dimethyltryptamine succinate salt	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).
Cohort 8 - multiple-dose, 3 hour interval	Placebo	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).
Cohort 9 - multiple-dose, 3 hour interval	5-methoxy-N,N-dimethyltryptamine succinate salt	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).
Cohort 9 - multiple-dose, 3 hour interval	Placebo	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).

Primary Outcome Measures

Name	Time	Method
Number of participants with Treatment Emergent Adverse Events as coded by MedDRA and assessed by CTCAE v4.0	Up to 30 Days	Number of participants with TEAEs following administration of 5-MeO-DMT.

Secondary Outcome Measures

Name	Time	Method
Plasma pharmacokinetic parameters of 5-MeO-DMT and bufotenine following a single-dose and multiple-doses of 5-MeO-DMT	Up to 24 hours	For PK analysis, blood samples will be collected before and up to 24 hours after the intramuscular administration of 5-MeO-DMT to determine 5-MeO-DMT and bufotenine serum concentrations.
Urine pharmacokinetic parameters of 5-MeO-DMT and bufotenine following a single-dose and multiple-doses of 5-MeO-DMT	Up to 24 hours	For PK analysis, urine samples will be collected before and up to 24 hours after the intramuscular administration of 5-MeO-DMT to determine 5-MeO-DMT and bufotenine urine concentrations.

Trial Locations

Locations (1)

Altasciences Clinical Kansas, Inc; 🇺🇸 Overland Park, Kansas, United States