Arzoxifene

Summary

Arzoxifene (CHEMBL226267) is a phase-3 clinical-stage small molecule; indicated across 4 conditions including postmenopausal osteoporosis and breast neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 4 conditions
• Clinical trials: 7
• Chemistry: 475.6 Da · C28H29NO4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL226267
Name	Arzoxifene
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	179337
Molecular formula	C28H29NO4S
Molecular weight	475.6
InChIKey	MCGDSOGUHLTADD-UHFFFAOYSA-N

SMILES: COC1=CC=C(C=C1)C2=C(C3=C(S2)C=C(C=C3)O)OC4=CC=C(C=C4)OCCN5CCCCC5

IUPAC name: 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol

Also known as: Arzoxifene, Arzoxifeno, LY-353381, LY353381, arzoxifene, ARZOXIFENE

Parent form; salt/anhydrous children: CHEMBL2105949

Patent coverage: 608 distinct patent families (1,606 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,284 (80%) 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: Estrogen receptor, Estrogen receptor beta.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
ESR1	9.7	EC50	0.2	nM	CHEMBL_ACT_15616085
ESR1	7.67	IC50	21.5	nM	CHEMBL_ACT_1883049
ESR1	7.38	IC50	42	nM	CHEMBL_ACT_15616563
ESR2	7.18	IC50	66.3	nM	CHEMBL_ACT_1883048
ESR2	6.62	IC50	240	nM	CHEMBL_ACT_15616568

Target pathways

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

Indications & clinical

Indications

4 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
postmenopausal osteoporosis	3	MONDO:0008159	EFO:0003854
breast neoplasm	3	MONDO:0021100	EFO:0003869
osteoporosis	2	MONDO:0005298	EFO:0003882

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

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE3	4
PHASE2	2
PHASE4	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00190697	PHASE4	COMPLETED	A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment
NCT00034125	PHASE3	COMPLETED	Phase 3 Study of LY353381 Vs Tamoxifen in Women With Locally Advanced or Metastatic Breast Cancer.
NCT00085956	PHASE3	COMPLETED	Effects of Arzoxifene on Bone Mass and the Uterus
NCT00088010	PHASE3	COMPLETED	Effects of Arzoxifene on Bone Fractures and Incidence of Breast Cancer
NCT00383422	PHASE3	COMPLETED	Study Comparing Arzoxifene With Raloxifene in Women After Menopause With Osteoporosis
NCT00005879	PHASE2	COMPLETED	LY353381 in Preventing Breast Cancer in Women With Hyperplasia
NCT00767299	PHASE2	COMPLETED	A Study of Arzoxifene to Treat Korean Women With Osteoporosis

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).