Linerixibat

Summary

Linerixibat (CHEMBL2387408) is a phase-3 clinical-stage small molecule; indicated across 4 conditions including cholestasis and intrahepatic cholestasis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 4 conditions
• Clinical trials: 14
• Chemistry: 546.7 Da · C28H38N2O7S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2387408
Name	Linerixibat
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	53492727
Molecular formula	C28H38N2O7S
Molecular weight	546.7
InChIKey	CZGVOBIGEBDYTP-VSGBNLITSA-N

SMILES: CCCC[C@@]1(CS(=O)(=O)C2=C(C=C(C(=C2)CNC(CC(=O)O)CC(=O)O)OC)[C@H](N1)C3=CC=CC=C3)CC

IUPAC name: 3-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]pentanedioic acid

Also known as: Gsk-2330672, Gsk2330672, GSK2330672, Linerixibat, LINERIXIBAT, IINERIXIBAT, Iinerixibat

Patent coverage: 103 distinct patent families (373 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 356 (95%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Ileal sodium/bile acid cotransporter, Ileal sodium/bile acid cotransporter, Ileal sodium/bile acid cotransporter.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q62633	8.72	IC50	1.9	nM	CHEMBL_ACT_13319199
P70172	8.68	IC50	2.1	nM	CHEMBL_ACT_13319200
SLC10A2	7.38	IC50	42	nM	CHEMBL_ACT_13320449
SLC10A2	7.37	IC50	43	nM	CHEMBL_ACT_17683580

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
cholestasis	3	MONDO:0001751	MONDO:0001751
intrahepatic cholestasis	2	MONDO:0019072	MONDO:0019072
type 2 diabetes mellitus	2	MONDO:0005148	MONDO:0005148

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 14.

Phase distribution

Phase	Trials
PHASE1	7
PHASE2	4
PHASE3	2
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04167358	PHASE3	ACTIVE_NOT_RECRUITING	Linerixibat Long-term Safety, and Tolerability Study
NCT04950127	PHASE3	COMPLETED	Global Linerixibat Itch Study of Efficacy and Safety in Primary Biliary Cholangitis (PBC) (GLISTEN)
NCT01899703	PHASE2	COMPLETED	A Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK) and Pharmacodynamics (PD) of Repeat Doses of GSK2330672 Administration in Subjects With Primary Biliary Cirrhosis (PBC) and Symptoms of Pruritus
NCT01929863	PHASE2	COMPLETED	Study to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of GSK2330672 in Type 2 Diabetes Patients Taking Metformin
NCT02202161	PHASE2	COMPLETED	A Study Investigating Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of GSK2330672 Administered With Metformin to Type 2 Diabetes Patients
NCT02966834	PHASE2	COMPLETED	Dose Response Study of GSK2330672 for the Treatment of Pruritus in Participants With Primary Biliary Cholangitis
NCT01416324	PHASE1	COMPLETED	First Time in Human Study Using GSK2330672
NCT01607385	PHASE1	COMPLETED	A Study to Evaluate the Safety, Tolerability, Pharmacokinetic a Single Day of Dosing With GSK1614235.
NCT03992014	PHASE1	COMPLETED	Pharmacokinetics (PKs) and Metabolism of Radiolabelled Linerixibat
NCT04053023	PHASE1	COMPLETED	Linerixibat and Obeticholic Acid Drug Interaction Study in Healthy Subjects
NCT05133830	PHASE1	COMPLETED	Linerixibat and Obeticholic Acid Drug Interaction Study in Healthy Adult Participants
NCT05393076	PHASE1	COMPLETED	Phase I Study of Linerixibat in Adults With Moderate Hepatic Impairment and Healthy Controls
NCT05435170	PHASE1	COMPLETED	Food Effect Study of Linerixibat Tablets in Healthy Adult Participants
NCT05448170	Not specified	AVAILABLE	Linerixibat Compassionate Use for Cholestatic Pruritus Adult Patients With Primary Biliary Cholangitis (PBC)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).