The Effect of Food on the Oral Bioavailability of AEF0117 in Healthy Volunteers

NCT05451017 | Terminated Phase 1 Results FDA Drug

• 2 other identifiers: AEF0117-105U01DA053832
• Study Type: interventional
• Target: 22
• Locations: 1 country
• Sites: 1

Brief Summary

Cannabis use is increasing and will only further escalate with legalization of recreational and medical cannabis use in western countries , with a prevalence greater than 30 % in the US and most European countries for individuals between 16 and 24 years of age. There are no available pharmacological treatments of cannabis use disorder (CUD). Thus, the development of safe and effective medications for the treatment of CUD is an urgent public health priority. The preclinical efficacy and available ADMET (Administration, Distribution, Metabolism, Elimination and Toxicology) in animal and human data suggest that AEF0117, an investigational new study drug, could constitute a very efficacious and safe treatment for cannabis abuse disorders. In the 3 early studies conducted with AEF0117, AEF0117 was administered orally after a light breakfast. AEF0117 showed a good bioavailability and favorable, dose-proportional pharmacokinetics . In this protocol, the effects of food on AEF0117 bioavailability in healthy volunteers will be investigated by comparing the rate and extent of AEF0117 when 1 mg AEF0117 is administered in fed state versus fasting state. The safety and tolerability of AE0117 has been demonstrated in the clinical studies conducted to date. This trial will provide data on the effect of food on the oral bioavailability of AEF0117 to support the next stage of the clinical development of the drug.

Conditions

Marijuana Abuse

Keywords

AEF0117; Cannabis-related Use Disorder; Cannabis subjective effects; Cannabis self-administration cannabis-induced analgesia; Cannabis-related cognitive disorder

Outcome Measures

Primary Outcomes (5)

• Cmax of AEF0117

  Plasma concentration maximum(Cmax) of a single dose of AEF0117 will be determined based on serial blood sample collections and plasma AEF0117 concentration after fed conditions relative to fasting conditions.

  up to 312 hours after dosing

• Tmax of AEF0117

  Time to maximum plasma concentration (tmax) of a single dose of AEF0117 will be determined based on serial blood sample collections and plasma AEF0117 concentration after fed conditions relative to fasting conditions.

  up to 312 hours after dosing

• AUC (Area Under Curve) t to Last Concentration of AEF0117

  Area under the plasma concentration (AUC to Last Nonzero Conc) based on serial blood sample collections and plasma AEF0117 concentration after fed conditions relative to fasting conditions

  up to 312 hours after dosing

• AUC (Area Under Curve) t to Infinity Observed of AEF0117

  Area under the plasma concentration (AUC infinity obs) based on serial blood sample collections and plasma AEF0117 concentration after fed conditions relative to fasting conditions

  up to 312 hours after dosing

• Bioavailibility of AEF0117 (Tlag)

  Tlag is the Time point of first quantifiable concentration after dose administration

  up to 312 hours after dosing

Secondary Outcomes (3)

• Lowest Peak Plasma (Cmin) of AEF0117 Plasma Exposure

  up to 312 hours after dosing

• Terminal Elimination Half-life (t1/2) of AEF0117

  up to 312 hours after dosing

• Incidence of Treatment-Emergent Adverse Event

  up to 312 hours after AEF0217 dosing

Study Arms (2)

AEF0117 1.0 mg in fasted condition

EXPERIMENTAL

16 participants receive 1 dose of AEF0117 1 mg in fasted condition

Drug: 3ß-(4-methoxybenzyloxy)pregn-5-en-20-one in fasting condition

AEF0117 1.0 mg in fed condition

EXPERIMENTAL

16 participants receive 1 dose of AEF0117 1 mg fed condition

Drug: 3ß-(4-methoxybenzyloxy)pregn-5-en-20-one in fed condition

Interventions

3ß-(4-methoxybenzyloxy)pregn-5-en-20-one in fed condition DRUG

a single dose of 1 mg AEF0117 in fed condition

Also known as: AEF0117

AEF0117 1.0 mg in fed condition

3ß-(4-methoxybenzyloxy)pregn-5-en-20-one in fasting condition DRUG

a single dose of 1 mg AEF0117 in fasting condition

Also known as: AEF0117

AEF0117 1.0 mg in fasted condition

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy, non-smoking male or female of any race, 18 to 55 years old, both inclusive.
• Both males and female participants must use highly effective contraception during the entire trial period. Male participants should refrain from donating sperm or planning a pregnancy throughout the trial. Male participants must agree to use double-barrier contraceptive methods: male condoms and spermicide. FHeterosexually active females are only eligible if they are documented to be surgically sterile (e.g., hysterectomy, tubal ligation) or post-menopausal (amenorrhea \>1 year and follicle-stimulating hormone \[FSH\] \>25.8 mIU/mL) and with a negative pregnancy test.
• Body mass index (BMI) of 22.0-35.0 kg/m2 (inclusive).
• Be informed of the nature of the trial and provide signed informed consent to participate in the trial prior to any trial-specific procedures.
• After being shown the high fat meal, understands and accepts that the entire meal should be consumed within 30 minutes.
• Be legally competent and able to communicate effectively (in English) with trial personnel.

You may not qualify if:

• Tobacco cigarette smokers within the last 3 months prior to dosing with trial drug.
• Any disease or condition that might compromise the cardiovascular, hematologic, renal, hepatic, pulmonary (including chronic asthma), endocrine (e.g., diabetes), central nervous, or gastrointestinal (including an ulcer and cholecystectomy) systems, or any clinical laboratory values assessed as potentially clinically significant by the investigator .
• Blood pressure outside normal range (140/80 mmHg systolic/diastolic) and considered potentially clinically significant.
• Congenital long QT syndrome, history of prolonged QT in the 3 months prior to screening.
• A corrected QT interval (Fridericia's - QTcF) \>450 msec (male) or \>470 msec (female) or history of risk factors for Torsades de Pointes.
• A history of alcoholism or drug addiction within the past 2 years, recent use (in the last month) of any illicit drugs, or positive results from a urine screen for substances of abuse or from an alcohol breath test.
• A history of or current serious mental illness including active or recent suicidal ideation, severe psychological distress (e.g., active suicidal plans, psychosis, debilitating panic disorder) and/or an abnormal Columbia-Suicide Severity Rating Scale (C-SSRS) result.
• Severe learning disability, brain damage, or pervasive developmental disorder.
• A history of difficulty donating blood or inadequate venous access.
• Clinically significant anemia or low hemoglobin (levels \<9 g/dL) at screening, or donation of \>250 mL of blood or plasma within the 30 days prior to prior to receiving trial drug or received any blood and plasma for medical/surgical reasons within the 30 days prior to prior to receiving trial drug, or intention to donate blood or plasma within 1 month after receiving trial drug.
• History of or current HIV or hepatitis B or C.
• History of COVID-19 within 4 weeks prior to Day -1, or positive COVID 19 test, according to standard procedures at the site, at screening or Day 1.
• Positive serum pregnancy test (ß-hCG) at screening or positive urine pregnancy test at Day 1 confirmed by a serum pregnancy test result.
• Allergies to the trial drug and known allergies to pregnenolone or to corn and corn derivatives.
• Use of any prescription or over-the-counter drug therapy, including psychoactive and/or psychotropic medication, herbal, homeopathic, vitamins, minerals, and nutritional supplements, bodybuilding supplements unapproved by the sponsor, within 2 weeks prior to receiving the trial drug (for drugs with an elimination half-life greater than 10 days, this will be extended to 60 days).

Sponsors & Collaborators

• Aelis Farma: lead
• National Institute on Drug Abuse (NIDA): collaborator

Study Sites (1)

Substance Use Research Center

New York, New York, 10032, United States

Location

MeSH Terms

Conditions

Marijuana Abuse

Condition Hierarchy (Ancestors)

Substance-Related Disorders; Chemically-Induced Disorders; Mental Disorders

Results Point of Contact

• Title: Stephanie Monlezun, Chief Operating Officer
• Organization: Aelis Farma

s.monlezun@aelisfarma.com

0554542327

Study Officials

• Margaret Haney, PhD

  Substance Use Research Center

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: LTE60
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: This is a single center, randomized, parallel-group, 2-arm, open-label, single-dose trial in healthy male and female volunteers aged 18-55 years to obtain data on the effect of food on the oral bioavailability of AEF0117.

Study Record Dates

• First Submitted: June 27, 2022
• First Posted: July 11, 2022
• Study Start: January 4, 2023
• Primary Completion: June 26, 2023
• Study Completion: June 28, 2023
• Last Updated: January 22, 2026
• Results First Posted: January 22, 2026

Record last verified: 2026-01

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)