Healthy Volunteers
Conditions
Keywords
pharmacokinetics, enzymes, metabolism prediction
Brief summary
The study aims to descibe the pharmacokinetics of 10 substrates of enzymes involved in drug metabolism and their metabolites, after administration singly and simultaenously at predefined doses in 10 health volunteers.
Detailed description
The aim of this study is to test the administration of combination of substrates and thereby to characterise simultaneously the main enzymes and transporters involved in drug metabolism. The doses of substrates administered will first assessed in terms of safety and their appropriateness for determination of pharmacokinetic parameters. Ten volunteers will be used, this number having been defined in view of the aims of this proof-of-concept pilot study,ie,safety and determination of pharmacokinetic parameters. The number was not the result of statistical calculation.
Interventions
DRUG10 parents drugs adminstration
A single and concomittant administration of 10 parent drugs will be performed: Acetaminophene, cafeine, dextrometorphan, digoxin, memantine,midazolam, omeprazole, repaglinide, rosuvastatine, tolbutamide.
Sponsors
Nuclear Energy Commission (CEA)
Institut National de la Santé Et de la Recherche Médicale, France
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* healthy volunteers
Exclusion criteria
* pregnancy
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic parameters | one week | The aim endpoint is based on the main pharmacokinetic parameters of each subject for all substrates and all metabolites. These main parameters are the area under the curve (AUC), the maximum concentration (Cmax), the half-life (T1/2)and the ratios of AUCs of the substrate and metabolites |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Tolerance of the concomittant administration of the 10 drugs: 1/number of volunteers with grade 4 adverse events 2/ number of volunteers with any adverse event, (grade 1 to grade 4) | one week | All clinical and biological adverse events will be recorded within the 7 days following drug administration. |
| pharmacokinetic | one week | To determine which sampling times will provid the most pharmacokinetic information on the most compounds |
| Genotypes | one month | Depending on the genotypes of the volunteers included, to evaluate the influence of these genotypes ont he pharmacokinetics of the substrates and their metabolites |
Countries
France
Outcome results
None listed