Fazamorexant

Summary

Fazamorexant (CHEMBL5314459) is a phase-3 clinical-stage small molecule targeting HCRTR1 and HCRTR2; indicated across 1 condition including insomnia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 2 (HCRTR1, HCRTR2)
• Indications: 1 condition
• Clinical trials: 9

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314459
Name	Fazamorexant
Type	Small molecule
Max phase	3

Also known as: Fazamorexant, YZJ-1139, FAZAMOREXANT

Patent coverage: 1 distinct patent families (1 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HCRTR1	OX1 receptor	Antagonist	7.7	4.9%	O43613
HCRTR2	OX2 receptor	Antagonist	7.44		O43614

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 2 target gene(s): HCRTR1, HCRTR2.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Orexin and neuropeptides FF and QRFP bind to their respective receptors	2	HCRTR1, HCRTR2
G alpha (q) signalling events	2	HCRTR1, HCRTR2

Dominant GO biological processes

GO term	Targets
neuropeptide signaling pathway	2
chemical synaptic transmission	2
feeding behavior	2
cellular response to hormone stimulus	2
regulation of cytosolic calcium ion concentration	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
positive regulation of ERK1 and ERK2 cascade	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
regulation of circadian sleep/wake cycle, wakefulness	1
circadian sleep/wake cycle process	1
locomotion	1
glucose homeostasis	1

Indications & clinical

Indications

1 indication (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

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE1	6
PHASE3	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06975514	PHASE3	RECRUITING	Safety and Efficacy Study of YZJ-1139 Tablets in Insomnia Disorder
NCT05525637	PHASE3	UNKNOWN	Safety and Efficacy Study of YZJ-1139 in Insomnia Disorder
NCT06680505	PHASE2	COMPLETED	Safety and Efficacy Study of YZJ-1139 in Primary Chronic Insomnia Disorder
NCT06671444	PHASE1	ACTIVE_NOT_RECRUITING	Pharmacokinetics and Safety Study of YZJ-1139 in Subjects With Severe Renal Impairment and Normal Renal Impairment
NCT06671470	PHASE1	ACTIVE_NOT_RECRUITING	A Drug-drug Interaction Study of YZJ-1139 Tablets and Ticagrelor Tablets in Healthy Subjects
NCT06680531	PHASE1	ACTIVE_NOT_RECRUITING	A Clinical Study to Evaluate the Drug Interaction Between YZJ-1139 Tablets and Escitalopram Oxalate Tablets
NCT06671509	PHASE1	COMPLETED	Pharmacokinetics and Safety Study of YZJ-1139 in Subjects With Mild, Moderate and Normal Hepatic Impairment
NCT06673927	PHASE1	COMPLETED	A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses of YZJ-1139 in Healthy Participants
NCT06685341	PHASE1	COMPLETED	PK/PD Study of YZJ-1139

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

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

11 molecules share ≥1 primary target. Top 11 by shared-target count:

Molecule	Source	Status	Shared targets
DARIDOREXANT	ChEMBL	Phase 4 (approved)	HCRTR1, HCRTR2
LEMBOREXANT	ChEMBL	Phase 4 (approved)	HCRTR1, HCRTR2
SUVOREXANT	ChEMBL	Phase 4 (approved)	HCRTR1, HCRTR2
ALMOREXANT	ChEMBL	Phase 3	HCRTR1, HCRTR2
SELTOREXANT	ChEMBL	Phase 3	HCRTR1, HCRTR2
FILOREXANT	ChEMBL	Phase 2	HCRTR1, HCRTR2
NIVASOREXANT	ChEMBL	Phase 2	HCRTR1, HCRTR2
SB-649868	ChEMBL	Phase 2	HCRTR1, HCRTR2
NALFURAFINE	ChEMBL	Phase 4 (approved)	HCRTR1
DANAVOREXTON	ChEMBL	Phase 2	HCRTR2
Belzutifan	PubChem	Approved	HCRTR1