Metoclopramide

Summary

Metoclopramide (CHEMBL86) is an approved small-molecule dopaminergic antagonist (ATC A03FA01) targeting DRD2 and HTR4; indicated across 22 conditions including neoplasm and hiv infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A03FA01
• Targets: 2 (DRD2, HTR4)
• Indications: 22 conditions
• Clinical trials: 123
• Chemistry: 299.79 Da · C14H22ClN3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL86
Name	Metoclopramide
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4168
ChEBI	CHEBI:107736
ATC	A03FA01
Molecular formula	C14H22ClN3O2
Molecular weight	299.79
InChIKey	TTWJBBZEZQICBI-UHFFFAOYSA-N

SMILES: CCN(CC)CCNC(=O)C1=CC(=C(C=C1OC)N)Cl

IUPAC name: 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxybenzamide

ChEBI definition: A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.

Pharmacological roles (ChEBI): antiemetic, dopaminergic antagonist, gastrointestinal drug.

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: Clopra-“yellow”, Elieten, Methoxyclopramide, Metoclopramida, Metoclopramide, Terperan, metoclopramide, Methoclopramide, SID11111421, SID11111422, SID26751627, SID90341551

Parent form; salt/anhydrous children: CHEMBL1200940, CHEMBL1256771

Patent coverage: 10,504 distinct patent families (37,825 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 37,817 (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

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	7.54	0%	P14416
	5-HT3AB	Antagonist	5.7
	5-HT3A	Antagonist	6.45
HTR4	5-HT4 receptor	Full agonist	6	0%	Q13639

Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Prelamin-A/C, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 4, 5-hydroxytryptamine receptor 3A, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Adrenergic receptor alpha-2, Serotonin 2 (5-HT2) receptor, Serotonin 3 (5-HT3) receptor.

Bioactivity

ChEMBL activities: 77 potent at pChembl ≥ 5 of 87 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
O70528	8.24	EC50	5.7	nM	CHEMBL_ACT_417283
LMNA	8.15	Potency	7.1	nM	CHEMBL_ACT_3654438
DRD3	7.8	Ki	16	nM	CHEMBL_ACT_17705197
DRD3	7.8	Ki	16	nM	CHEMBL_ACT_26603614
DRD3	7.57	Ki	27	nM	CHEMBL_ACT_712466
P08482	7.45	Potency	35.5	nM	CHEMBL_ACT_4807502
DRD2	7.38	Ki	42	nM	CHEMBL_ACT_7751768
HTR3E	7.3	Kd	50.12	nM	CHEMBL_ACT_788615
HTR3E	7.3	Kd	50.12	nM	CHEMBL_ACT_937810
P19020	7.21	IC50	61.3	nM	CHEMBL_ACT_1224050
DRD2	7.19	Ki	64	nM	CHEMBL_ACT_17705193
DRD3	7.17	Ki	68	nM	CHEMBL_ACT_7751770
DRD3	7.12	AC50	76	nM	CHEMBL_ACT_25194199
P20288	7.1	Ki	80	nM	CHEMBL_ACT_1035145
HTR3E	7.1	Kd	79.43	nM	CHEMBL_ACT_937811
P61169	6.98	Ki	104	nM	CHEMBL_ACT_959236
DRD2	6.96	AC50	110	nM	CHEMBL_ACT_25141016
P61169	6.95	Ki	113	nM	CHEMBL_ACT_1267358
DRD2	6.9	IC50	127	nM	CHEMBL_ACT_7751767
P35563	6.8	Ki	158.5	nM	CHEMBL_ACT_535898
P23979	6.7	Ki	200	nM	CHEMBL_ACT_1035144
DRD3	6.7	IC50	200	nM	CHEMBL_ACT_7751769
P35563	6.7	Ki	199.5	nM	CHEMBL_ACT_788618
P35563	6.68	Ki	210	nM	CHEMBL_ACT_1224043
P35563	6.64	IC50	228	nM	CHEMBL_ACT_1224047
P35563	6.64	Ki	229.1	nM	CHEMBL_ACT_788617
P61169	6.63	Ki	235	nM	CHEMBL_ACT_959237
P35563	6.62	Ki	240	nM	CHEMBL_ACT_1267357
P61169	6.54	Ki	285	nM	CHEMBL_ACT_772166
P61169	6.52	Ki	303	nM	CHEMBL_ACT_1224045

Target pathways

Aggregated over 2 target gene(s): DRD2, HTR4.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	HTR4
Signaling by GPCR	1	HTR4
Class A/1 (Rhodopsin-like receptors)	1	HTR4
Amine ligand-binding receptors	1	HTR4
GPCR downstream signalling	1	HTR4
Dopamine receptors	1	DRD2
Serotonin receptors	1	HTR4
G alpha (s) signalling events	1	HTR4
GPCR ligand binding	1	HTR4

Dominant GO biological processes

GO term	Targets
signal transduction	2
G protein-coupled receptor signaling pathway	2
temperature homeostasis	1
response to hypoxia	1
response to amphetamine	1
nervous system process involved in regulation of systemic arterial blood pressure	1
regulation of heart rate	1
regulation of sodium ion transport	1
G protein-coupled receptor internalization	1
positive regulation of neuroblast proliferation	1
positive regulation of receptor internalization	1
intracellular calcium ion homeostasis	1
autophagy	1
adenylate cyclase-inhibiting dopamine receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1

Indications & clinical

Indications

22 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
neoplasm	3	MONDO:0005070	EFO:0000616
HIV infectious disease	3	MONDO:0005109	EFO:0000764
gastroparesis	3	MONDO:0006769	EFO:1000948
gastroschisis	3	MONDO:0009264	EFO:1000949
gastroenteritis	3	MONDO:0002269	EFO:1001463
migraine disorder	3	MONDO:0005277	MONDO:0005277
myelodysplastic syndrome	2	MONDO:0018881	EFO:0000198
injury	2	MONDO:0021178	EFO:0000546
hyperemesis gravidarum	2	MONDO:0006791	EFO:1000971
hypoglycemia	2	MONDO:0004946	HP:0001943
intestinal obstruction	2	MONDO:0004565	MONDO:0004565
orthostatic hypotension	1	MONDO:0005469	EFO:0005252
postural orthostatic tachycardia syndrome	1	MONDO:0011479	EFO:1000645

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

Clinical trials

Total trials: 123.

Phase distribution

Phase	Trials
PHASE4	42
Not specified	29
PHASE3	24
PHASE2	17
PHASE1	5
PHASE1/PHASE2	4
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05731960	PHASE4	RECRUITING	Evaluating the Effect of Intravenous Dexamethasone on the Duration of Spinal Anesthesia After Cesarean Delivery
NCT06148025	PHASE4	RECRUITING	Antibiotics and Vaccine Immune Responses Study
NCT06740812	PHASE4	NOT_YET_RECRUITING	Broadening Antiemetics Research by Comparing the Effectiveness of Fosaprepitant and Metoclopramide
NCT07100691	PHASE4	NOT_YET_RECRUITING	Gastric Emptying With Metoclopramide in GLP-1 Agonist Patients Undergoing Elective Surgery
NCT00242450	PHASE4	COMPLETED	Metoclopramide Use in Very Low Birth Weight Newborns
NCT00364806	PHASE4	COMPLETED	Prochlorperazine vs Metoclopramide
NCT00475306	PHASE4	COMPLETED	The Montefiore Metoclopramide Study
NCT00778011	PHASE4	COMPLETED	Uncomplicated Nausea and Vomiting in the Emergency Department
NCT01011673	PHASE4	COMPLETED	Metoclopramide Versus Ketorolac for Tension-type Headache
NCT01191645	PHASE4	COMPLETED	Opioid Effects on Swallowing and Esophageal Sphincter Pressure
NCT01267864	PHASE4	COMPLETED	Valproate Versus Ketorolac Versus Metoclopramide
NCT01596166	PHASE4	COMPLETED	Intravenous Ketorolac and Metoclopramide for Pediatric Migraine in the Emergency Department
NCT01630109	PHASE4	COMPLETED	Study of Metoclopramide in Small Bowel Capsule Endoscopy
NCT01781377	PHASE4	COMPLETED	Prophylactic Subhypnotic Propofol for Nausea and Vomiting During for Cesarean Section Under Subarachnoid Anesthesia.
NCT01825941	PHASE4	COMPLETED	Diphenhydramine for Acute Migraine
NCT01837394	PHASE4	COMPLETED	Ultrasound-guided Blocks for Ambulatory Knee Arthroscopy
NCT01937234	PHASE4	COMPLETED	Use of an Antiemetic to Shorten the Length of Labor in Nulliparous Women
NCT02098499	PHASE4	WITHDRAWN	Haldol/Diphenhydramine Versus Metoclopramide/Diphenhydramine for Treatment of Acute Headache in the ED: A RCT
NCT02253524	PHASE4	COMPLETED	Comparison of Efficacy Dimenhydrinate and Metoclopramide in the Treatment of Nausea Due to Vertigo
NCT02314351	PHASE4	COMPLETED	Intravenous Metoclopramide in the Acute Treatment of Migraine: A Double-blind, Randomized, Placebo-controlled Trial
NCT02441894	PHASE4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT02459275	PHASE4	TERMINATED	PEP uP Protocol in Surgical Patients
NCT02627950	PHASE4	COMPLETED	Impact of Morphine Treatment on Platelet Inhibition in Acute Myocardial Infarction
NCT02847494	PHASE4	COMPLETED	Corticosteroids for Acute Migraine in the Emergency Department
NCT02907632	PHASE4	COMPLETED	Methoclopramide for Gastroesophageal Reflux in Premature Infants
NCT02913469	PHASE4	UNKNOWN	Effects of Morphine on Loading-dose Ticagrelor in Patients With ST-segment Elevation Myocardial Infarction
NCT02939235	PHASE4	COMPLETED	Influence of Metoclopramide on Ticagrelor Pharmacokinetics and Pharmacodynamics in Patients With Unstable Angina Pectoris on Concomitant Treatment With Morphine
NCT02959840	PHASE4	COMPLETED	Acupuncture Point P6 Stimulation for Reduction of Nausea and Vomiting During Cesarean
NCT02972502	PHASE4	TERMINATED	Efficacy of Haloperidol vs. Metoclopramide for Treatment of Acute Headaches and Migraines in the Emergency Department
NCT03017391	PHASE4	UNKNOWN	Treatment Algorithm for Nausea and Vomiting in the Palliative Phase
NCT03269435	PHASE4	COMPLETED	Greater Occipital Nerve Block Versus Metoclopramide
NCT03778281	PHASE4	UNKNOWN	Treatment of Chemotherapy-related Hiccups With Baclofen
NCT03932578	PHASE4	COMPLETED	Intrathecal Atropine vs IV Metoclopramide for Nausea & Vomiting During CS
NCT04771481	PHASE4	COMPLETED	Metoclopramide for Acute Upper GI Bleeding
NCT04799015	PHASE4	COMPLETED	Dexamethasone for Post Traumatic Headache
NCT04873297	PHASE4	COMPLETED	Metoclopramide vs Placebo for Prevention of Pneumonia in Acute Stroke
NCT04969120	PHASE4	COMPLETED	Metoclopramide and the Length of First Stage of Labor , a Randomized Controlled Trial
NCT05533281	PHASE4	COMPLETED	Efficacy of Three Antiemetics in Preventing Nausea and Vomiting
NCT05641051	PHASE4	COMPLETED	Metoclopramide on Gastric Emptying in Mechanically Ventilated Patients
NCT05669781	PHASE4	COMPLETED	The Effects of Combined Gum-chewing and Parenteral Metoclopramide on Post-operative Ileus

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 9 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

Molecule	Source	Status	Shared targets
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR4
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR4
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR4
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	DRD2, HTR4
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD2, HTR4
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2
PRUCALOPRIDE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2
AMODIAQUINE	ChEMBL	Phase 4 (approved)	DRD2
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2
AMSACRINE	ChEMBL	Phase 4 (approved)	DRD2
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	DRD2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2
ARMODAFINIL	ChEMBL	Phase 4 (approved)	DRD2
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2
AZATADINE	ChEMBL	Phase 4 (approved)	DRD2
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD2
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	DRD2
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD2
BEPRIDIL	ChEMBL	Phase 4 (approved)	DRD2
BETAMETHASONE DIPROPIONATE	ChEMBL	Phase 4 (approved)	DRD2
BLONANSERIN	ChEMBL	Phase 4 (approved)	DRD2
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD2
BROMPERIDOL	ChEMBL	Phase 4 (approved)	DRD2
BUSPIRONE	ChEMBL	Phase 4 (approved)	DRD2
BUTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD2
CANNABIDIOL	ChEMBL	Phase 4 (approved)	DRD2
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD2
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD2
CEFEPIME	ChEMBL	Phase 4 (approved)	DRD2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	DRD2
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD2
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD2
CINACALCET	ChEMBL	Phase 4 (approved)	DRD2
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD2
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD2
CLOFAZIMINE	ChEMBL	Phase 4 (approved)	DRD2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD2
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD2
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	DRD2
DACOMITINIB	ChEMBL	Phase 4 (approved)	DRD2
DARIFENACIN	ChEMBL	Phase 4 (approved)	DRD2
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	DRD2
DESIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2
DESLORATADINE	ChEMBL	Phase 4 (approved)	DRD2
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD2
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD2
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD2