NCT03992014

Pharmacokinetics (PKs) and Metabolism of Radiolabelled Linerixibat

A Two-period Study in Healthy Male Participants to Determine the Pharmacokinetics, Balance/Excretion, and Metabolism of [14C]-Linerixibat Following a Single Intravenous Radiolabeled Microtracer Dose (Concomitant With a Non-radiolabeled Oral Dose) and a Single Oral Radiolabeled Dose

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 6 (actual)
• Sponsor: GlaxoSmithKline · Industry
• Sex: Male
• Age: 30 Years – 55 Years
• Healthy volunteers: Accepted

Summary

Absorption, metabolism and excretion of linerixibat have been studied in previous clinical trials. However, no dedicated clinical studies of drug absorption, metabolism, and excretion have been conducted for linerixibat. The purpose of this study is to determine the PK, balance/excretion, and metabolism of radiolabeled 14 Carbon \[14C\]-linerixibat following a single intravenous (IV) radiolabeled microtracer dose (concomitant with a non-radiolabeled oral dose) and a single oral radiolabeled dose. This is a single group, two period, single sequence, and mass balance study will enroll 6 healthy male subjects. Each subject will be involved in the study for up to 10 weeks which includes screening period, two treatment periods (treatment Periods 1 and 2), separated by about 7 days (at least 13 days between oral doses), and a follow-up visit 1-2 weeks after the last assessment in treatment Period 2.

Conditions

• Cholestasis

Interventions

Type	Name	Description
DRUG	Linerixibat tablet	Linerixibat will be available as white to slightly colored film-coated round tablet to be administered as two tablets taken in the fasted state in the morning with 240 milliliter (mL) of room temperature water.
DRUG	[14C]-linerixibat intravenous infusion	\[14C\]-linerixibat will be available as clear, colorless solution free from visible particulates to be administered 25 mL IV over 3 hours immediately after the oral dose.
DRUG	Linerixibat oral solution	Linerixibat will be available as clear, colorless solution free from visible particulates to be administered 60 mL solution in the fasted state in the morning.

Timeline

• Start date: 2019-07-08
• Primary completion: 2019-08-26
• Completion: 2019-08-26
• First posted: 2019-06-19
• Last updated: 2020-06-26
• Results posted: 2020-06-26

Locations

1 site across 1 country: United Kingdom

Regulatory

• FDA-regulated drug study