First-In-Human (FIH), Single Ascending Dose (SAD) Study of FluoroEthylNorMemantine (FENM)

Phase 1

Withdrawn

• Conditions: Alzheimer Disease; Treatment Resistant Depression; PTSD; Major Depressive Disorder; Neuro-Degenerative Disease; Brain Diseases
• Interventions: Drug: Fluoroethylnormemantine (FENM)

• Registration Number: NCT05921929
• Lead Sponsor: ReST Therapeutics

Brief Summary

The goal of this First-In-Human (FIH) trial is to learn about safety and PharmacoKinetics (PK) in healthy adult volunteers. The main questions it aims to answer are:

* What is the safety of single ascending doses of the FluoroEthylNorMemantine (FENM)?

* What is the PK profile of single ascending doses of the FENM in human?

* What is the preliminary exploratory time course of Brain Disease Neurotrophic Factor (BDNF) plasmatic levels of single ascending doses of the FENM? Participants will receive one single oral dose of FENM.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2023-06-06
• Study First Submitted QC: 2023-06-23
• Study First Posted: 2023-06-27
• Status Verified: 2024-05
• Study Start: 2024-05-02
• Primary Completion: 2024-05-02
• Study Completion: 2024-05-02
• Last Update Submitted: 2024-05-02
• Last Update Posted: 2024-05-03

Recruitment & Eligibility

• Status: WITHDRAWN
• Sex: Male
• Target Recruitment: Not specified

Inclusion Criteria

• willing and able to sign written informed consent,
• Body Mass Index (BMI) of 17.5 to 30.5 kg/m2, a total body weight >65 kg,
• efficient contraceptive mean,
• no major psychiatric disorder per the Mini-International Neuropsychiatric Interview (MINI) questionnaire,
• normal laboratory tests results, arterial Blood Pressure/pulse rate, 12-lead Electrocardiogram recording.

Exclusion Criteria

• evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, allergic disease including drug allergies, or other severe acute or chronic medical or psychiatric condition or laboratory abnormality,
• history of febrile illness within 5 days prior to administration,
• any condition possibly affecting drug absorption,
• using of prescription drugs, vaccine, routine or as needed consumption of medications or herbal supplements,
• having positive serology, positive urine test for drugs of abuse, a general medical or psychological condition or behavior, including current substance dependence or abuse,
• history of drug or alcohol abuse within 1 year before screening,
• consuming currently of nicotine containing products, any food or any beverage containing grapefruit or grapefruit juice within 48 h prior to administration,
• having blood donation or loss of significant amount of blood within 2 months prior to study.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
One single oral dose per participant	Fluoroethylnormemantine (FENM)	-

Primary Outcome Measures

Name	Time	Method
Number of participants with treatment-related adverse events as assessed by CTCAE v4.0	From single dose administration to the end of the study follow-up (2 weeks later)

Secondary Outcome Measures

Name	Time	Method
To assess last observed plasma concentration [Clast]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess time to Cmax [Tmax]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess area under the plasma concentration-time curve from dosing (time 0) to the time of last measured concentration [AUC 0-last]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess preliminary exploratory time course of Brain Disease Neurotrophic Factor plasmatic levels of single ascending doses of the FENM	At pre-dose, at Cmax (estimated at 6-8hours post-dose) and at 48, 72 and 264hours post-dose
To assess minimum concentration within the dosing interval [Cmin]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess area under the plasma concentration-time curve from 0 to the end of the dose interval [AUC 0-tau]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess total area under the plasma concentration-time curve from dosing (time 0) taken to the limit as the end time becomes arbitrarily large (infinity) [AUC 0-∞]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess time of the minimum concentration [Tmax]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess apparent volume of distribution [Vz/F]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess terminal half-life, apparent elimination half-life [T1/2]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess apparent oral clearance [CL/F]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess maximum plasma concentration [Cmax]	At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose

Trial Locations

Locations (1)

CHU of Liège - Clinical Pharmacology Unit; 🇧🇪 Liège, Belgium