Brilaroxazine

Summary

Brilaroxazine (CHEMBL5095172) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including schizoaffective disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 2
• Chemistry: 450.4 Da · C22H25Cl2N3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5095172
Name	Brilaroxazine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	46861612
Molecular formula	C22H25Cl2N3O3
Molecular weight	450.4
InChIKey	PMKMNTBZJOXTJW-UHFFFAOYSA-N

SMILES: C1CN(CCN1CCCCOC2=CC3=C(C=C2)OCC(=O)N3)C4=C(C(=CC=C4)Cl)Cl

IUPAC name: 6-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-4H-1,4-benzoxazin-3-one

Also known as: Brilaroxazine, RP-5063, Rp5063, BRILAROXAZINE

Parent form; salt/anhydrous children: CHEMBL6068404

Patent coverage: 55 distinct patent families (131 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 81 (62%) 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: 6 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, 5-hydroxytryptamine receptor 1A, D(2) dopamine receptor, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 7, 5-hydroxytryptamine receptor 6.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR2B	9.72	Ki	0.19	nM	CHEMBL_ACT_27765485
DRD2	9.21	Ki	0.61	nM	CHEMBL_ACT_27635468
DRD2	9.21	Ki	0.62	nM	CHEMBL_ACT_27765476
HTR1A	8.82	Ki	1.5	nM	CHEMBL_ACT_27088431
HTR1A	8.82	Ki	1.5	nM	CHEMBL_ACT_27635474
HTR1A	8.82	Ki	1.5	nM	CHEMBL_ACT_27765479
DRD2	8.71	IC50	1.96	nM	CHEMBL_ACT_27635465
HTR1A	8.65	IC50	2.25	nM	CHEMBL_ACT_27088432
HTR1A	8.65	IC50	2.25	nM	CHEMBL_ACT_27635471
HTR2A	8.6	Ki	2.5	nM	CHEMBL_ACT_27765482
HTR7	8.57	Ki	2.7	nM	CHEMBL_ACT_27765491
HTR6	7.29	Ki	51	nM	CHEMBL_ACT_27765488
HTR2A	7.23	Ki	58.5	nM	CHEMBL_ACT_27088435
HTR2A	7.23	Ki	58.5	nM	CHEMBL_ACT_27635480
HTR2A	6.89	IC50	130	nM	CHEMBL_ACT_27088436
HTR2A	6.89	IC50	130	nM	CHEMBL_ACT_27635477

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
schizoaffective disorder	2	MONDO:0005487	EFO:0005411

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

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05184335	PHASE3	RECRUITING	Safety and Efficacy of Brilaroxazine (RP5063) in Schizophrenia
NCT01490086	PHASE2	COMPLETED	RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder

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).