A Phase I, Randomized, Open-label, Single Dose, 2 Period, Crossover Study to Evaluate the Effect of Food on the Pharmacokinetics of Linerixibat Tablets in Healthy Adult Participants

GlaxoSmithKline1 site in 1 country23 target enrollmentAugust 11, 2022

ConditionsPruritus

Interventionslinerixibat

Overview

Phase: Phase 1
Intervention: linerixibat
Conditions: Pruritus
Sponsor: GlaxoSmithKline
Enrollment: 23
Locations: 1
Primary Endpoint: Plasma linerixibat area under the concentration-time curve from time zero (pre-dose) to the time of the last quantifiable concentration [AUC(0-t)]
Status: Completed
Last Updated: 3 years ago

Overview Investigators Eligibility Criteria Arms & Interventions Outcomes Sites Similar Trials

Overview

Brief Summary

This study will evaluate the effect of food on the Pharmacokinetic (PK) and Pharmacodynamic (PD) parameters of linerixibat administered in fed and fasted states in heathy adult participants

Registry

clinicaltrials.gov

Start Date

August 11, 2022

End Date

October 10, 2022

Last Updated

3 years ago

Study Type

Interventional

Study Design

Crossover

Sex

All

Investigators

Sponsor

GlaxoSmithKline

Responsible Party

Sponsor

Eligibility Criteria

Inclusion Criteria

Not provided

Exclusion Criteria

•History of cholecystectomy.
•Current symptomatic cholelithiasis or inflammatory gall bladder disease.
•Significant history of or current disorders capable of significantly altering the absorption, metabolism, or elimination of drugs.
•Current clinically significant diarrhea.
•History of gastrointestinal surgery with ileal resection or ileal bypass at any time.
•Any malignancy within the past 5 years except for basal cell or squamous epithelial carcinomas of the skin that have been resected with no evidence of metastatic disease for 3 years.
•Administration of any other Ileal Bile Acid Transport (IBAT) inhibitor (including linerixibat) in the 3 months prior to screening.
•Past or intended use of over the counter or prescription medication, including vitamins and dietary or herbal supplements) within 7 days (or 14 days if the drug is a potential enzyme inhibitor) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless approved by the Investigator in conjunction with GSK Medical Monitor.
•Current enrollment in a clinical trial or recent participation in a clinical trial and has received an investigational product within the following time period prior to study drug administration: 30 days, 5 half-lives, or twice the duration of the biological effect of the investigational product (whichever is longer).
•Exposure to more than 4 new chemical entities within 12 months before the first dose in the current study.

Arms & Interventions

Treatment sequence AB

Participants will receive linerixibat in fed state (Treatment A) in period 1 followed by linerixibat in fasted state (Treatment B) in period 2. The washout period will be of at least 7 days.

Intervention: linerixibat

Treatment sequence BA

Participants will receive linerixibat in fasted state (Treatment B) in period 1 followed by linerixibat in fed state (Treatment A) in period 2. The washout period will be of at least 7 days.

Intervention: linerixibat

Outcomes

Primary Outcomes

Plasma linerixibat area under the concentration-time curve from time zero (pre-dose) to the time of the last quantifiable concentration [AUC(0-t)]

Time Frame: Up to 36 hours post dose

Maximum observed plasma concentration (Cmax) of linerixibat

Time Frame: Up to 36 hours post dose

Secondary Outcomes

Apparent terminal phase half-life (t1/2) of linerixibat(Up to 36 hours post dose)
Apparent terminal phase volume of distribution (Vz/F) of linerixibat(Up to 36 hours post dose)
Plasma linerixibat area under the concentration-time curve from time zero (pre-dose) to 24 hour [AUC (0-24)](Up to 24 hours post dose)
Apparent clearance (CL/F) of linerixibat(Up to 36 hours post dose)
Incidence of adverse events (AEs) and of serious adverse events (SAEs)(Up to day 52)
Plasma linerixibat area under the concentration-time curve from time zero (pre-dose) to infinite time [AUC (0-∞)](Up to 36 hours post dose)
Time of occurrence of Cmax (Tmax) of linerixibat(Up to 36 hours post dose)
Serum C4 area under the concentration-time curve from time zero (pre-dose) to 24 hour [AUC (0-24)](Up to 24 hours post dose)
Delay in achieving Tmax (Tlag) of linerixibat(Up to 36 hours post dose)
Serum C4 area under the concentration-time curve from time zero (pre-dose) to the time of the last quantifiable concentration [AUC(0-t)](Up to 36 hours post dose)