RecruitingPhase 1NCT07014930

Identification of New Tools for Predicting Natural Metabolic Performance of the Liver

Endobiotics for Phenotyping Cytochrome P450 Enzymes: Using Metabolomics to Identify Novel Endogenous CYP2C19 Activity Biomarkers in Healthy Volunteers


Sponsor

Caroline Samer

Enrollment

40 participants

Start Date

Dec 5, 2024

Study Type

INTERVENTIONAL

Conditions

Summary

The objective of this clinical trial is to identify endogenous compounds (substances naturally present in the human body) that may serve as predictors of the activity of a key liver enzyme, CYP2C19. This enzyme plays a crucial role in the metabolism of several important drugs and exhibits significant interindividual variability in its activity, which can contribute to adverse drug reactions or reduced therapeutic efficacy. The study will involve 40 healthy volunteers, divided into two groups: 10 poor metabolizers and 30 non-poor metabolizers. Each participant will undergo three sessions. In the first session, 24-hour urine collection and plasma sampling will be conducted. Omeprazole will be administered orally, and the baseline blood OH-omeprazole/omeprazole ratio will be determined via capillary blood sampling. The second session, identical in procedure to the first, will take place after 7 days of fluvoxamine administration (inhibition phase). The third session will also mirror the first but will follow 10 days of rifampicin administration (induction phase). Endogenous compounds showing significant variation across sessions and between metabolizer groups will be evaluated as potential biomarkers for predicting CYP2C19 activity.


Eligibility

Min Age: 18 YearsMax Age: 65 Years

Inclusion Criteria6

  • Healthy men and women
  • Age 18-65 years
  • Body Mass Index (BMI) 18-27
  • Understanding of French language and able to give a written inform consent
  • CYP2C19 genotype: PMs, NMs, RMs or UMs
  • At least one barrier method contraception during the whole study and 1 month after the end of the study (in addition of hormonal contraception if applicable)

Exclusion Criteria14

  • CYP2C19 IMs
  • Participation in any other interventional clinical study within 3 months prior to inclusion
  • Pregnant or breastfeeding woman
  • Any pathologies, use of drugs or food that may affect CYP activity (based on the 'drug interactions and cytochromes P450 table published by the Service of Clinical Pharmacology and Toxicology, HUG50 and on the investigator's knowledge)
  • Medical history of liver transplantation
  • Regular smokers of ≥ 10 cigarettes/day
  • Alcohol intake 2 days prior to session 1 and during fluvoxamine and rifampicin intake
  • Alteration of hepatic tests (ASAT, ALAT, GGT, bilirubin more than 3x normal)
  • Renal failure (serum urea, serum creatinine and eGFR outside the norms)
  • Medical history of chronic alcoholism or abuse of psychoactive drugs
  • Sensitivity to any of the drugs used
  • Psychiatric disorders
  • Beck Score ≥10 (question related to suicide >0)
  • Contact lens wearers

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Interventions

DRUGControl session

Plasma and urine sampling as well as the determination of the blood OH-omeprazole/omeprazole ratio at baseline by capillary blood sampling.

DRUGInhibition session

Plasma and urine sampling as well as the determination of the blood OH-omeprazole/omeprazole ratio at baseline by capillary blood sampling, with prior administration of 50 mg of fluvoxamine for 7 consecutive days (CYP2C19 inhibitor).

DRUGInduction session

Plasma and urine sampling as well as the determination of the blood OH-omeprazole/omeprazole ratio at baseline by capillary blood sampling, with prior administration of 600 mg of rifampicin for 10 consecutive days (CYP2C19 inducer).


Locations(1)

The Geneva University Hospitals (HUG)

Geneva, Switzerland

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NCT07014930


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