Influence of OATP1B1 and CYP2C9 Genotypes on the Pharmacokinetics of Bosentan Before and During Clarithromycin
Status:
Completed
Trial end date:
2012-12-01
Target enrollment:
Participant gender:
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).