Eplivanserin

Summary

Eplivanserin (CHEMBL257704) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including insomnia and sleep disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 7
• Chemistry: 328.4 Da · C19H21FN2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL257704
Name	Eplivanserin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	135456190
Molecular formula	C19H21FN2O2
Molecular weight	328.4
InChIKey	VAIOZOCLKVMIMN-PRJWTAEASA-N

SMILES: CN(C)CCO/N=C(/C=C/C1=CC=C(C=C1)O)\C2=CC=CC=C2F

IUPAC name: 4-[(E,3Z)-3-[2-(dimethylamino)ethoxyimino]-3-(2-fluorophenyl)prop-1-enyl]phenol

Also known as: Eplivanserin, Eplivanserina, Eplivanserine, SR-46349, SR46349, EPLIVANSERIN, EplivanserinÊ, EplivanserinÂ

Parent form; salt/anhydrous children: CHEMBL2103845

Patent coverage: 199 distinct patent families (505 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 504 (100%) 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: 1 (assay-derived). Sample: Serotonin 2 (5-HT2) receptor.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
HTR2A	8.92	Kd	1.2	nM	CHEMBL_ACT_24710242

Target pathways

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

Indications & clinical

Indications

2 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
insomnia	3	MONDO:0013600	EFO:0004698
sleep disorder	3	MONDO:0100081	EFO:0008568

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE3	5
PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00253903	PHASE3	COMPLETED	Efficacy and Safety of Eplivanserin Treatment for Sleep Maintenance Insomnia Followed by Optional Extension up to 1 Year
NCT00253968	PHASE3	COMPLETED	Efficacy and Safety of Eplivanserin Treatment for Sleep Maintenance Insomnia
NCT00308503	PHASE3	COMPLETED	Efficacy and Safety of Eplivanserin 5mg/Day on Sleep Maintenance Insomnia
NCT00679900	PHASE3	COMPLETED	Comparison of Eplivanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties
NCT00805350	PHASE3	COMPLETED	Efficacy and Safety of Eplivanserin 5mg/Day in Insomnia Characterized by Sleep Maintenance Difficulties
NCT00313885	PHASE2	COMPLETED	Efficacy and Safety of SR46349B in Patients With Sleep Disorders in Fibromyalgia
NCT00913614	PHASE1	COMPLETED	Single Dose Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Evaluation of Eplivanserin in Children With Insomnia

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).