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Completed

NCT Number: NCT01731067

Cocktail Approach for Cytochrome P450 and P-glycoprotein Activity Assessment Using Dried Blood Spot

Phenotyping is an approach largely used for the evaluation of the activity of cytochromes and transporters in vivo. It consists of the administration of probe substances metabolised by a specific cytochrome or transported by P-glycoprotein (P-gp) for example, followed by the determination of a metabolic ratio or the evaluation of the plasmatic or urinary concentrations of the probe substances. The administration of a cocktail containing several probe substances allows the simultaneous evaluation of the activity of several cytochromes and P-gp in a single test.

The aim of this project is the validation of a phenotyping cocktail of low dose probe drugs for the assessment of cytochrome P450 and P-gp activities by simple capillary blood sampling and dried blood spot (DBS) analysis. The cocktail consists of caffeine, bupropion, flurbiprofen, omeprazole, dextromethorphan, midazolam and fexofenadine for the simultaneous phenotyping of CYP1A2, CYP2B6, CYP2C9, CAP2C19, CYP2D6, CYP3A4 and P-gp, respectively.

The modulation of the activity of cytochromes or P-gp will be evaluated by the administration of inhibitors (fluvoxamine, voriconazole, quinidine) or inducer (rifampicin) of the metabolic pathways or the P-gp mediated transport.

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Key information

Conditions

Healthy Volunteers

Age range

18 year–65 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

University Hospitals

Geneva, Switzerland

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Healthy male volunteers aged from 18 to 60 years
  • BMI between 18 and 25
  • Understanding of French language and able to give a written inform consent.

Exclusion criteria

  • Smoker
  • Taking drugs which alter CYPs activity
  • Renal or hepatic impairment
  • Medical history of porphyria
  • Medical history of chronic alcoholism or abuse of psychoactive drugs
  • Liver transplantation
  • Sensitivity to any of the drugs used
  • Wearing contact lenses (risk of coloration with rifampicin)
  • ECG showing long QT interval (>0.46sec)
  • Alteration of hepatic tests
  • Presenting genetic polymorphism of poor CYP 2B6, 2C9, 2C19, 2D6 metabolisers

Treatment and study plan

Cocktail probe drugs

Drug

Other names: Oral intake of the cocktail probe drugs :, bupropion 25 mg, flurbiprofen 25 mg, omeprazole 5 mg, dextromethorphan 5 mg, midazolam 1 mg, fexofenadine 25mg, Caffeine (a cup of coffee)

Primary outcomes

  1. Probe cocktail drugs plasma and capillary concentrations in presence/absence of CYP1A2,2B6, 2C9, 2C19, 2D6, 3A4 and P-gp inhibitor or inducer

    Time frame: 4 singles days spaced out with one week wash-out periods

Secondary outcomes

  1. correlation between plasma or urine and capillary concentrations for each probe cocktail drug

    Time frame: 4 singles days spaced out with one week wash-out periods

  2. comparison. between genotype and phenotype for each enzyme

    Time frame: one day

Sponsors and collaborators

Lead sponsor

Jules Desmeules

Other

Registry information

Important dates

Study start
2012
Primary completion
2013
Study completion
2014
First posted
Nov 21, 2012
Registry last updated
Sep 16, 2014

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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