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Completed

NCT Number: NCT02743260

Drug Transporter Interaction Study PHENTRA_2015_KPUK

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.

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Key information

Conditions

Healthy

Age range

18 year–85 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 4

Primary location

Department of Pharmacology I, University Hospital Cologne

Cologne, North Rhine-Westphalia, 50931, Germany

About this study

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.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Caucasian
  • Body mass index (BMI) between and inclusive 18.5 and 30 kg/m2
  • Willing and capable to confirm written consent prior to enrolment after ample information has been provided
  • Normal findings in the medical history unless the principal investigator considers an abnormality to be clinically relevant.
  • Considered to be healthy by the principal investigator on the basis of extensive pre-study screening-

Exclusion criteria

Standard for healthy volunteers, including:

  • Female subjects only: positive results in pregnancy test
  • Female subjects only: lactating women
  • Female subjects only: subjects who do not use or do not agree to use appropriate contraceptive methods during the study as defined in Note for Guidance on Non-Clinical Safety Studies for the Conduct of Human Clinical Trials for Pharmaceuticals (CHMP/ICH/286/95 modification)

Treatment and study plan

Pitavastatin

Drug

Other names: Livazo®

metformin

Drug

Other names: Metformin-CT®

Digoxin

Drug

Other names: Digacin®

Adefovir

Drug

Other names: Hepsera®

Sitagliptin

Drug

Other names: Januvia®

Primary outcomes

  1. organic anionic transporter polypeptide 1B1 (OATP1B1): Clearance over bioavailability (CL/F) of pitavastatin

    Time frame: 24 hours

    PK parameter

  2. organic cation transporters 1 and 2 (OCT1/2), multidrug and toxic compound extrusion transporters 1 and 2,kidney splice variant (MATE1/2K): Renal clearance (CLr) of metformin

    Time frame: 24 hours

    PK parameter

  3. intestinal p-glycoprotein (P-gp): Peak Plasma Concentration (Cmax) of digoxin

    Time frame: 24 hours

    PK parameter

  4. renal p-glycoprotein (P-gp): Renal clearance (CLr) of digoxin:

    Time frame: 24 hours

    PK parameter

  5. organic anion transporter 1 (OAT1): Renal clearance (CLr) of adefovir

    Time frame: 24 hours

    PK parameter

  6. organic anion transporter 3 (OAT3): Renal clearance (CLr) of sitagliptin

    Time frame: 24 hours

    PK parameter

Sponsors and collaborators

Lead sponsor

University of Cologne

Other

Collaborators

  • Institute for Biomedical and Pharmaceutical Research (IBMP), Nürnberg-Heroldsberg, Germany
  • Umm Al-Qura University

Registry information

Official study title

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

Important dates

Study start
2016
Primary completion
2017
Study completion
2017
First posted
Apr 19, 2016
Registry last updated
Sep 10, 2019

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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