Domperidone

Summary

Domperidone (CHEMBL219916) is an approved small-molecule dopaminergic antagonist (ATC A03FA03) targeting DRD2 and DRD3; indicated across 9 conditions including gastroparesis and gastroenteritis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A03FA03
• Targets: 2 (DRD2, DRD3)
• Indications: 9 conditions
• Clinical trials: 52
• Chemistry: 425.9 Da · C22H24ClN5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL219916
Name	Domperidone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3151
ChEBI	CHEBI:31515
ATC	A03FA03
Molecular formula	C22H24ClN5O2
Molecular weight	425.9
InChIKey	FGXWKSZFVQUSTL-UHFFFAOYSA-N

SMILES: C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O

IUPAC name: 6-chloro-3-[1-[3-(2-oxo-3H-benzimidazol-1-yl)propyl]piperidin-4-yl]-1H-benzimidazol-2-one

ChEBI definition: 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.

Pharmacological roles (ChEBI): antiemetic, dopaminergic antagonist.

Also known as: Domilium, Domperidona, Domperidone, Evoxin, Motilium, Motilium 10, Motilium instants, NSC-299589, NSC-759575, R 33,812, R-33812, Vivadone

Parent form; salt/anhydrous children: CHEMBL3436365, CHEMBL4594380

Patent coverage: 5,463 distinct patent families (18,305 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 18,181 (99%) 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

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
DRD2	D2 receptor	Antagonist	8.4	0%	P14416
DRD3	D3 receptor	Antagonist	7.6	0%	P35462

Broader ChEMBL bioactivity targets: 51 (assay-derived). Sample: Ubiquitin carboxyl-terminal hydrolase 2, Prelamin-A/C, Inositol monophosphatase 1, Geminin, Peripheral myelin protein 22, Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor.

Bioactivity

ChEMBL activities: 86 potent at pChembl ≥ 5 of 106 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P61169	9.28	Ki	0.52	nM	CHEMBL_ACT_12456281
P61169	9.24	Ki	0.57	nM	CHEMBL_ACT_12456267
DRD2	9.05	Ki	0.88	nM	CHEMBL_ACT_7709507
P61169	9	IC50	1	nM	CHEMBL_ACT_25495702
P19020	8.99	Ki	1.02	nM	CHEMBL_ACT_12456243
DRD2	8.89	Ki	1.3	nM	CHEMBL_ACT_17705192
P61169	8.6	IC50	2.5	nM	CHEMBL_ACT_194108
DRD2	8.58	IC50	2.65	nM	CHEMBL_ACT_7709506
P19020	8.57	IC50	2.68	nM	CHEMBL_ACT_1197583
P61169	8.55	IC50	2.8	nM	CHEMBL_ACT_173098
P19020	8.51	Ki	3.08	nM	CHEMBL_ACT_12456257
DRD3	8.46	Ki	3.5	nM	CHEMBL_ACT_688774
P61169	8.28	IC50	5.2	nM	CHEMBL_ACT_818233
DRD2	8.22	AC50	6	nM	CHEMBL_ACT_25140265
DRD3	8.21	Ki	6.24	nM	CHEMBL_ACT_7709509
DRD3	8.12	Ki	7.5	nM	CHEMBL_ACT_17705196
DRD3	8.12	Ki	7.5	nM	CHEMBL_ACT_26603611
HTR2A	7.96	Ki	11	nM	CHEMBL_ACT_7711693
P19020	7.93	Ki	11.7	nM	CHEMBL_ACT_12456219
P61169	7.87	IC50	13.6	nM	CHEMBL_ACT_1197582
P19020	7.84	Ki	14.4	nM	CHEMBL_ACT_12456229
DRD3	7.75	IC50	18	nM	CHEMBL_ACT_7709508
DRD3	7.62	AC50	24	nM	CHEMBL_ACT_25193460
HTR2A	7.43	IC50	37	nM	CHEMBL_ACT_7711692
HTR2A	7.25	AC50	55.6	nM	CHEMBL_ACT_25173593
KCNH2	7.24	IC50	57.54	nM	CHEMBL_ACT_2616691
P15823	7.06	Ki	87	nM	CHEMBL_ACT_7707337
P43140	6.94	Ki	116	nM	CHEMBL_ACT_7707335
ADRA1A	6.89	AC50	128.3	nM	CHEMBL_ACT_25137889
NFKB1	6.85	Potency	141.3	nM	CHEMBL_ACT_3671982

Target pathways

Aggregated over 2 target gene(s): DRD2, DRD3.

Top Reactome pathways

2 total, by targets touching each:

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

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor internalization	2
intracellular calcium ion homeostasis	2
adenylate cyclase-inhibiting dopamine receptor signaling pathway	2
locomotory behavior	2
visual learning	2
response to xenobiotic stimulus	2
regulation of dopamine secretion	2
positive regulation of cytokinesis	2
circadian regulation of gene expression	2
response to histamine	2
response to cocaine	2
dopamine metabolic process	2
regulation of potassium ion transport	2
response to morphine	2
negative regulation of blood pressure	2

Indications & clinical

Indications

9 indications (1 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
gastroparesis	3	MONDO:0006769	EFO:1000948
gastroenteritis	3	MONDO:0002269	EFO:1001463
gastroesophageal reflux disease	3	MONDO:0007186	EFO:0003948
dyspepsia	3	MONDO:0002268	EFO:0008533
relapsing-remitting multiple sclerosis	2	MONDO:0005314	EFO:0003929
chronic progressive multiple sclerosis	2	MONDO:0005284	EFO:0003840
Parkinson disease	2	MONDO:0005180	MONDO:0005180

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

Clinical trials

Total trials: 52.

Phase distribution

Phase	Trials
Not specified	21
PHASE4	9
PHASE3	9
PHASE2	8
PHASE2/PHASE3	2
PHASE1	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02264587	PHASE4	UNKNOWN	Effects and Mechanism of Mosapride Citrate on Diabetic Gastroparesis
NCT02685436	PHASE4	COMPLETED	Role of Pepsin Assay in Wheezy Infants
NCT02958046	PHASE4	COMPLETED	The Efficacy of Lansoprazole and Domperidone Combination on Intragastric and Intraesophageal Acidity
NCT03022201	PHASE4	COMPLETED	Comparing the Therapeutic Efficacy and Safety of DA-9701 With Domperidone in Patients With Parkinson’s Disease
NCT03355170	PHASE4	WITHDRAWN	Cardiac Safety of Lansoprazole and Domperidon Combination
NCT03617016	PHASE4	COMPLETED	Preliminarily Evaluate the Efficacy of Domperidone in Adult Chinese Participants With Functional Dyspepsia
NCT03806062	PHASE4	COMPLETED	EFFECT OF LOW LEVEL LASER THERAPY VERSUS ELECTROACUPUNCTURE ON POSTNATAL SCANTY MILK SECRETION
NCT04583111	PHASE4	UNKNOWN	The Effect of Antiemetics on Bowel Preparation Before Colonoscopy
NCT05030116	PHASE4	COMPLETED	Clinical Trial for ‘Shen Qu Xiao Shi’ Oral Liquid in the Treatments of Children’s Functional Dyspepsia
NCT01696734	PHASE3	RECRUITING	Domperidone in Treating Patients With Gastrointestinal Disorders
NCT06695962	PHASE3	NOT_YET_RECRUITING	Efficacy of Domperidone (a Prokinetic Agent) on Time in Range in Digestively Asymptomatic Type I Diabetic Patients With Delayed Gastric Emptying (Gastro-TIR)
NCT00308334	PHASE2/PHASE3	COMPLETED	Effect of Domperidone on the Nutrient Composition of Preterm Mother’s Breast Milk
NCT01257672	PHASE3	COMPLETED	Symptomatic Treatment of Acute Gastroenteritis
NCT01355276	PHASE3	COMPLETED	Efficacy and Safety of Cinitapride Tablets in the Treatment of Mild to Moderate Functional Dyspepsia
NCT01378884	PHASE3	WITHDRAWN	The Use of Domperidone for Gastroparesis
NCT01710462	PHASE3	WITHDRAWN	Clinical Study, Multicenter, Randomized With 2 Arms of Pantoprazole + Domperidone and Pantoprazole Isolated at the Gastroesophageal Reflux Disease
NCT01878526	PHASE3	COMPLETED	Gastroesophageal Reflux Treatment in Scleroderma
NCT02699385	PHASE3	TERMINATED	A Study to Evaluate the Safety and Efficacy of Domperidone in Pediatric Participants With Nausea and Vomiting Due to Acute Gastroenteritis
NCT04802785	PHASE2/PHASE3	UNKNOWN	The Impact of Air Travel on Passenger Cognitive Functions
NCT05570292	PHASE3	COMPLETED	Study of Effects of Preoperative Oral Domperidone on Gastric Residual Volume After Clear Fluid Ingestion in Patients Scheduled for Elective Surgeries
NCT00006077	PHASE2	COMPLETED	Effects of Monoamine Reuptake Inhibitor NS2330 in Parkinson’s Disease
NCT00238056	PHASE2	COMPLETED	Effect of Domperidone on QT Interval in Premature Infants
NCT00284024	PHASE2	TERMINATED	Effectiveness of Domperidone to Increase Breastmilk Supply in Mothers With Low Supply
NCT00305331	PHASE2	TERMINATED	Domperidone as a Treatment for Dopamine Agonist-induced Peripheral Edema in Patients With Parkinson’s Disease
NCT00760461	PHASE2	TERMINATED	Domperidone in Refractory Gastroparesis
NCT01512225	PHASE2	COMPLETED	Enhancing Breast Milk Production With Domperidone in Mothers of Preterm Neonates
NCT02308137	PHASE2	COMPLETED	Domperidone in Secondary Progressive Multiple Sclerosis (SPMS)
NCT02493049	PHASE2	COMPLETED	Pilot Trial of Domperidone in Relapsing-Remitting Multiple Sclerosis (RRMS)
NCT00103597	PHASE1	COMPLETED	Efficacy of Therapeutic Interventions for Orthostatic Hypotension in Parkinson’s Disease and Multiple System Atrophy
NCT02816853	PHASE1	COMPLETED	Study to Evaluate the Effects of Domperidone on Cardiac Repolarization in Chinese Healthy Participants
NCT03221855	EARLY_PHASE1	COMPLETED	Use of Domperidone to Increase Milk Production in Mothers With Newborns in Neonatology
NCT02494687	Not specified	AVAILABLE	Domperidone Expanded Access Program for Oncology Patients With Gastroparesis Who Have Failed Standard Therapy
NCT04699591	Not specified	RECRUITING	Compassionate Use of Domperidone for Refractory Gastroparesis
NCT00552422	Not specified	TERMINATED	Domperidone for Gastroparesis in Solid Organ Transplantation
NCT00761254	Not specified	TERMINATED	Domperidone for Relief of Gastrointestinal Disorders
NCT00777439	Not specified	UNKNOWN	Domperidone for Refractory Gastrointestinal Disorders
NCT00874133	Not specified	TERMINATED	The Effect of Acupuncture on Symptoms, Gastric Emptying Rate and Glucose Control in Patients With Diabetic Gastroparesis
NCT00925457	Not specified	COMPLETED	Evaluating the Risk of Serious Ventricular Arrhythmia and Sudden Cardiac Death Among Users of Domperidone
NCT01347814	Not specified	COMPLETED	Effect of 10mg Domperidone on Gastric Emptying of a High-fat Meal and Appetite Sensations in Healthy Adults
NCT01711918	Not specified	COMPLETED	Domperidone for the Treatment of Chronic Nausea and Vomiting Secondary to Gastroparesis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

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

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARMODAFINIL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BEPRIDIL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BROMPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BUSPIRONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BUTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CINACALCET	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DESIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DESLORATADINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DISULFIRAM	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOPAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOTHIEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DROPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DULOXETINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EBASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ECONAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EPALRESTAT	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EPINEPHRINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ERGOTAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
FENOLDOPAM	ChEMBL	Phase 4 (approved)	DRD2, DRD3
FENTANYL	ChEMBL	Phase 4 (approved)	DRD2, DRD3