NCT02743260

Drug Transporter Interaction Study PHENTRA_2015_KPUK

Single Centre in Vivo Cocktail Phenotyping Study on OATP1B1, OCT1/2, MATE1/2K, OAT1/3, and P-gp Drug Transporters in Healthy Volunteers

• Status: Completed
• Phase: Phase 4
• Study type: Interventional
• Enrollment: 24 (actual)
• Sponsor: University of Cologne · Academic / Other
• Sex: All
• Age: 18 Years – 85 Years
• Healthy volunteers: Accepted

Summary

The objective of the present study is to contribute to establishing in vivo phenotyping procedures for organic anionic transporter polypeptide 1B1 (OATP1B1), organic cation transporters 1 and 2 (OCT1/2), multidrug and toxic compound extrusion transporters 1 and 2,kidney splice variant (MATE1/2K), organic anion transporters 1 and 3 (OAT1/3), and p-glycoprotein (P-gp) transporters via a cocktail approach. To this end, marker substrates for each of the respective transporters are administered as single doses in one period each and as a cocktail in one period to 24 healthy volunteers, and phenotyping metrics are derived from plasma and urine concentrations.

Detailed description

Blood sampling: - 0:15 h pre-dose, 0:15, 0:30, 0:45, 1:00, 1:20, 1:40, 2:00, 2:20, 2:40, 3:00, 3:30, 4:00, 5:00, 6:00, 8:00, 12:00, 16:00, 24:00 hours post-dose Urine Sampling: Pre-dose, 0-4 hours, 4-8 hours, 8-12 hours, 12-16 hours, 16-24 hours Drug analysis: by liquid chromatography - tandem mass spectrometry (LC-MS/MS) Pharmacokinetic Characteristics: Evaluation is carried out using standard noncompartmental characteristics including: area under the plasma concentration vs. time curve truncated at time t (AUC0-t), area under the plasma concentration vs. time curve extrapolated to infinity (AUC0-∞), peak plasma concentration (Cmax), time of occurrence of Cmax (tmax), apparent elimination half-life (t½), clearance over bioavailability (CL/F), renal clearance (CLr) and renal secretion. The evaluation may be completed by compartmental population pharmacokinetic approaches. Statistical evaluation: Pharmacokinetic characteristics are compared for cocktail administration vs. individual administration by standard average bioequivalence assessment. Safety, tolerability: Adverse events, laboratory and clinical parameters and vital signs will be assessed.

Conditions

• Healthy

Interventions

Type	Name	Description
DRUG	pitavastatin
DRUG	Metformin
DRUG	digoxin
DRUG	Adefovir
DRUG	sitagliptin

Timeline

• Start date: 2016-04-01
• Primary completion: 2017-12-01
• Completion: 2017-12-01
• First posted: 2016-04-19
• Last updated: 2019-09-10

Locations

1 site across 1 country: Germany