Clinical Trials

Sponsored by GlaxoSmithKline, several completed clinical trials have evaluated linerixibat for therapeutic applications in liver and metabolic conditions, focusing on cholestasis and associated pruritus. Spanning Phase 1 and Phase 2, these studies evaluated pharmacokinetic profiles, safety in hepatic impairment, drug-drug interactions, and food effects. Ultimately, the trials demonstrated the drug's dose-dependent tolerability and therapeutic efficacy in reducing cholestatic symptoms.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05435170 Completed
Pruritus
GlaxoSmithKline
 2022-08-11 Phase 1
NCT05393076 Completed
Pruritus
GlaxoSmithKline
 2022-07-19 Phase 1
NCT04053023 Completed
Cholestasis
GlaxoSmithKline
 2019-08-27 Phase 1
NCT02966834 Completed
Cholestasis
GlaxoSmithKline
 2017-01-11 Phase 2
NCT02801981 Completed
Cholestasis
GlaxoSmithKline
 2016-06 Phase 1

(data from https://clinicaltrials.gov, updated on 2024-05-22)

Check the Linerixibat product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Linerixibat acts as a highly potent, nonabsorbable inhibitor of the apical sodium-dependent bile acid transporter (ASBT, IC50 = 42 nM), effectively blocking the ileal reabsorption of bile acids into the enterohepatic circulation. By promoting the fecal excretion of bile acids and reducing systemic bile salt accumulation, this targeted inhibition alleviates cholestasis and relieves debilitating cholestatic pruritus in clinical conditions such as primary biliary cholangitis.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

Jump to

Note: Technical data last updated: Sep 1, 2026.