An Open-Label Study to Evaluate the Effect of Eluxadoline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Participants.

ABSTRACT: Eluxadoline is a mixed μ-opioid, κ-opioid receptor agonist, and δ-opioid receptor antagonist, approved in the United States for adults with diarrhea-predominant irritable bowel syndrome. This phase 1, single-center, open-label, single-sequence study was conducted on 30 healthy participants to establish whether steady-state eluxadoline increases systemic exposure of the cytochrome P450 (CYP) 3A4 substrate midazolam. Participants received oral midazolam 4 mg on day 1 with a 7-day washout period. On days 8-16, oral eluxadoline 100 mg was administered twice daily. On day 15, midazolam 4 mg was coadministered with the eluxadoline 100-mg morning dose. Primary outcome measures were pharmacokinetic parameters of midazolam and 1-hydroxy-midazolam. The midazolam and 1-hydroxy-midazolam geometric mea

SUBMITTER: Boinpally R 

PROVIDER: S-EPMC9805131 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature