Flupentixol

Summary

Flupentixol (CHEMBL6066864) is a phase-3 clinical-stage unknown (ATC N05AF01) targeting DRD1, DRD2, and DRD3; indicated across 5 conditions including psychotic disorder and anxiety.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Unknown
• ATC class: N05AF01
• Targets: 4 (DRD1, DRD2, DRD3…)
• Indications: 5 conditions
• Clinical trials: 13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL6066864
Name	Flupentixol
Type	Unknown
Max phase	3
ATC	N05AF01

Also known as: Flupenthixol, Flupentixol, LC 44, LC-44, N-7009, Flupentixole, flupenthixol, SID26755684, SID29216405, SID90341514, SID50111069, SID50111070

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
DRD1	D1 receptor	Antagonist	8.4	0%	P21728
DRD2	D2 receptor	Antagonist	8.82	0%	P14416
DRD3	D3 receptor	Antagonist	8.96	0%	P35462
DRD5	D5 receptor	Antagonist	8.1	0%	P21918

Broader ChEMBL bioactivity targets: 36 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, 5-hydroxytryptamine receptor 2B, Protein deacetylase HDAC6.

Bioactivity

ChEMBL activities: 21 potent at pChembl ≥ 5 of 47 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD1	8.52	AC50	3	nM	CHEMBL_ACT_25115088
DRD3	8.52	AC50	3	nM	CHEMBL_ACT_25194403
HRH1	8.34	AC50	4.6	nM	CHEMBL_ACT_25212203
DRD3	8.33	AC50	4.7	nM	CHEMBL_ACT_25193229
HTR2B	7.2	AC50	63	nM	CHEMBL_ACT_25227243
ADRA2C	6.57	AC50	270	nM	CHEMBL_ACT_25147570
ADRA2A	6.53	AC50	296.5	nM	CHEMBL_ACT_25156307
HTR1A	6.23	AC50	593.7	nM	CHEMBL_ACT_25164902
SLC6A3	6.05	AC50	897.1	nM	CHEMBL_ACT_25124837
CHRM1	5.89	AC50	1295	nM	CHEMBL_ACT_25210108
HDAC6	5.81	IC50	1547	nM	CHEMBL_ACT_23141072
KCNH2	5.8	AC50	1600	nM	CHEMBL_ACT_25117413
CHRM2	5.77	AC50	1686	nM	CHEMBL_ACT_25195614
KCNK2	5.7	IC50	2000	nM	CHEMBL_ACT_16619990
SLC6A4	5.23	AC50	5894	nM	CHEMBL_ACT_25151205
USP1	5.16	IC50	7000	nM	CHEMBL_ACT_16667645
SLC6A2	5.14	AC50	7189	nM	CHEMBL_ACT_25145878
Q9F4F7	5.1	Potency	7943	nM	CHEMBL_ACT_4398365
SLC6A3	5.09	AC50	8100	nM	CHEMBL_ACT_25123649
TBXA2R	5.07	AC50	8506	nM	CHEMBL_ACT_25197738
MEN1	5	Potency	10000	nM	CHEMBL_ACT_4595511

Target pathways

Aggregated over 4 target gene(s): DRD1, DRD2, DRD3, DRD5.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Dopamine receptors	4	DRD1, DRD2, DRD3, DRD5
G alpha (s) signalling events	2	DRD1, DRD5
G alpha (i) signalling events	1	DRD3

Dominant GO biological processes

GO term	Targets
phospholipase C-activating dopamine receptor signaling pathway	4
synaptic transmission, dopaminergic	4
signal transduction	4
G protein-coupled receptor signaling pathway	4
response to cocaine	4
response to amphetamine	3
adenylate cyclase-activating dopamine receptor signaling pathway	3
G protein-coupled dopamine receptor signaling pathway	3
visual learning	3
response to xenobiotic stimulus	3
dopamine metabolic process	3
behavioral response to cocaine	3
regulation of dopamine uptake involved in synaptic transmission	3
locomotory behavior	3
associative learning	3

Indications & clinical

Indications

5 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
psychotic disorder	3	MONDO:0005485	EFO:0005407
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050

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

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE4	4
PHASE2	4
PHASE3	2
PHASE1	2
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01164059	PHASE4	COMPLETED	Clinical Effectiveness of Newer Antipsychotics in Comparison With Conventional Antipsychotics in Schizophrenia
NCT02307396	PHASE4	COMPLETED	Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients
NCT04898270	PHASE4	COMPLETED	Adjunctive Use of Fute (Flupentixol) in Multi-acting Receptor-targeted Antipsychotics Treated Schizophrenia Patients
NCT04970667	PHASE4	COMPLETED	Flupentixol and Melitracen Tablets in the Treatment of Emotional Disorder
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT03205228	PHASE3	COMPLETED	Treatment in Patients With Globus: Psychoeducation, Anxiolytics or Proton Pump Inhibitors
NCT00000241	PHASE2	COMPLETED	Flupenthixol Decanoate in Methamphetamine Smoking - 1
NCT00000266	PHASE2	COMPLETED	Flupenthixol Treatment in Schizophrenic Cocaine Abusers - 1
NCT00000274	PHASE2	COMPLETED	Flupenthixol and Haloperidol for Treating Cocaine Abuse Schizophrenics - 9
NCT00000275	PHASE2	COMPLETED	Cocaine Abuse and ADHD - 10
NCT00000349	PHASE1	UNKNOWN	Infusion Laboratory: Protocol 5 (Flupenthixol) - 14
NCT02179931	PHASE1	COMPLETED	Bioequivalence Study in Healthy Men and Women to Compare Two Pharmaceutical Formulations of Flupentixol/Melitracen (Deanxit®)
NCT06756139	Not specified	RECRUITING	Effects of Cognitive Behavioral Therapy Through a Mobile App on Patients With Refractory Functional Dyspepsia

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.

590 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
DOPAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
HALOPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
IMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
KETOTIFEN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
LOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
MAPROTILINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
PROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
RISPERIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
ROPINIROLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
TEGASEROD	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
NIGULDIPINE	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD5
PENFLURIDOL	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD5
RACLOPRIDE	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD5
RITANSERIN	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD5
TETRAHYDROPALMATINE	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD5
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3
Tamsulosin	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DISULFIRAM	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
DROPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
EBASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3
ECONAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3