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.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
OTHER
Masking
NONE
Single ascending oral dose administration according to the following scheme: 20, 40, 80, 120-160, 200-240, 260-320mg/kg (six dose levels). The three upper dose levels to be administered (120-160, 200-240, 260-320mg/kg) will be precisely determined with the data collected at the end of the first three dose levels administered.
CHU of Liège - Clinical Pharmacology Unit
Liège, Belgium
Number of participants with treatment-related adverse events as assessed by CTCAE v4.0
Time frame: From single dose administration to the end of the study follow-up (2 weeks later)
To assess maximum plasma concentration [Cmax]
Time frame: 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]
Time frame: At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess minimum concentration within the dosing interval [Cmin]
Time frame: At pre-dose and at 2, 4, 6, 8, 10, 12, 24, 48, 96, 189, 264 and 336hours post-dose
To assess last observed plasma concentration [Clast]
Time frame: 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]
Time frame: 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]
Time frame: 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]
Time frame: 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-∞]
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Time frame: 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]
Time frame: 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]
Time frame: 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]
Time frame: 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
Time frame: At pre-dose, at Cmax (estimated at 6-8hours post-dose) and at 48, 72 and 264hours post-dose