NCT01425229

Influence of OATP1B1 and CYP2C9 Genotypes on the Pharmacokinetics of Bosentan Before and During Clarithromycin

Influence of OATP1B1 and CYP2C9 Genotypes on the Pharmacokinetics of Steady State Bosentan Before and During CYP3A4-inhibition by Clarithromycin

• Status: Completed
• Phase: —
• Study type: Observational
• Enrollment: 16 (actual)
• Sponsor: Gerd Mikus · Academic / Other
• Sex: All
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

The aim of the present study is to assess the impact of the OATP1B1 genotype (SLCO1B1\*15 vs. wild type; \~2% SLCO1B1\*15 haplotypes in Caucasian population) and the CYP2C9 genotype (\*2 and \*3 allele vs. wild type; \~5% poor metabolisers in Caucasian population) on the pharmacokinetics of bosentan and the impact of CYP3A4-inhibition by clarithromycin on steady state bosentan which is a CYP3A4 inducer itself. This study will focus on differential effects of genotypes and co-medication on the pharmacokinetics of bosentan at the metabolic and transport level. Participants will be genotyped for CYP2C9 (inclusion criterion), OATP1B1 (inclusion criterion), and CYP3A5 (no inclusion criterion).

Conditions

• Drug Interactions

Interventions

Type	Name	Description
DRUG	Bosentan	* Administration of bosentan: 1 x 125 mg p.o. on day 1, 2 x 125 mg p.o. on day 2-14 * Administration of clarithromycin: 2 x 500 mg p.o. on day 11-14

Timeline

• Start date: 2011-06-01
• Primary completion: 2012-05-01
• Completion: 2012-12-01
• First posted: 2011-08-29
• Last updated: 2017-05-31
• Results posted: 2015-08-04

Locations

1 site across 1 country: Germany