Eprotirome

Summary

Eprotirome (CHEMBL2035874) is a phase-3 clinical-stage small molecule; indicated across 3 conditions including familial hypercholesterolemia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 3 conditions
• Clinical trials: 4
• Chemistry: 487.1 Da · C18H17Br2NO5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2035874
Name	Eprotirome
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10299876
Molecular formula	C18H17Br2NO5
Molecular weight	487.1
InChIKey	VPCSYAVXDAUHLT-UHFFFAOYSA-N

SMILES: CC(C)C1=C(C=CC(=C1)OC2=C(C=C(C=C2Br)NC(=O)CC(=O)O)Br)O

IUPAC name: 3-[3,5-dibromo-4-(4-hydroxy-3-propan-2-ylphenoxy)anilino]-3-oxopropanoic acid

Also known as: Bms-356384, Eprotirome, Eprotiromo, Kb-2115, Kb2115, EPROTIROME

Patent coverage: 190 distinct patent families (486 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 340 (70%) 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: 2 (assay-derived). Sample: Thyroid hormone receptor alpha, Thyroid hormone receptor beta.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
THRB	9.37	Ki	0.43	nM	CHEMBL_ACT_10901777
THRA	8.02	Ki	9.6	nM	CHEMBL_ACT_10901790

Target pathways

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

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
familial hypercholesterolemia	3	MONDO:0005439	EFO:0004911

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

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE2	3
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01410383	PHASE3	TERMINATED	Efficacy and Safety Study of Eprotirome in HeFH Patients Who Are on Optimal Standard of Care
NCT00593047	PHASE2	COMPLETED	LDL-Cholesterol Lowering Effect of KB2115 as Add on to Statin
NCT00677248	PHASE2	COMPLETED	LDL-Cholesterol Lowering Effect of KB2115 as Add on to Ezetimibe
NCT00776321	PHASE2	COMPLETED	Eprotirome for the Treatment of Dyslipidemia, Efficacy and Safety 12-Week, Phase ii Study to Assess the Safety and Efficacy of KB2115 in Patients With Primary Hypercholesterolemia

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).