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.
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.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
10
A single and concomittant administration of 10 parent drugs will be performed: Acetaminophene, cafeine, dextrometorphan, digoxin, memantine,midazolam, omeprazole, repaglinide, rosuvastatine, tolbutamide.
Center of clinical investigation
Paris, France
Pharmacokinetic parameters
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
Time frame: one week
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)
All clinical and biological adverse events will be recorded within the 7 days following drug administration.
Time frame: one week
pharmacokinetic
To determine which sampling times will provid the most pharmacokinetic information on the most compounds
Time frame: one week
Genotypes
Depending on the genotypes of the volunteers included, to evaluate the influence of these genotypes ont he pharmacokinetics of the substrates and their metabolites
Time frame: one month
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.