Droperidol

Summary

Droperidol (CHEMBL1108) is an approved small-molecule dopaminergic antagonist (ATC N05AD08); indicated across 4 conditions including psychotic disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AD08
• Indications: 4 conditions
• Clinical trials: 22
• Chemistry: 379.4 Da · C22H22FN3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1108
Name	Droperidol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3168
ChEBI	CHEBI:4717
ATC	N05AD08
Molecular formula	C22H22FN3O2
Molecular weight	379.4
InChIKey	RMEDXOLNCUSCGS-UHFFFAOYSA-N

SMILES: C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F

IUPAC name: 3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one

ChEBI definition: An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.

Pharmacological roles (ChEBI): antiemetic, dopaminergic antagonist, first generation antipsychotic, anaesthesia adjuvant.

Also known as: Droleptan, Droperidol, Droperidol component of innovar, Dridol, Inapsine, MCN-JR-4749, NSC-169874, R-4749, SID11112409, SID26719691, SID26748461, SID855921

Patent coverage: 4,407 distinct patent families (16,888 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 16,336 (97%) 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: 35 (assay-derived). Sample: Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Prelamin-A/C, Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Sodium channel protein type 5 subunit alpha.

Bioactivity

ChEMBL activities: 58 potent at pChembl ≥ 5 of 69 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P43140	9.18	Ki	0.67	nM	CHEMBL_ACT_7673224
HTR2A	9.13	Ki	0.74	nM	CHEMBL_ACT_7675453
DRD2	9.1	Ki	0.8	nM	CHEMBL_ACT_7673300
DRD3	9.03	Ki	0.94	nM	CHEMBL_ACT_7673302
P43140	8.78	IC50	1.65	nM	CHEMBL_ACT_7673223
DRD2	8.62	IC50	2.41	nM	CHEMBL_ACT_7673299
HTR2A	8.59	IC50	2.58	nM	CHEMBL_ACT_7675452
DRD3	8.56	IC50	2.77	nM	CHEMBL_ACT_7673301
P15823	8.01	Ki	9.78	nM	CHEMBL_ACT_7673226
P15823	7.75	IC50	18	nM	CHEMBL_ACT_7673225
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_1055549
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_1427116
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_1523564
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_2358272
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_2616647
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_2645526
KCNH2	7.49	IC50	32.2	nM	CHEMBL_ACT_305244
KCNH2	7.49	IC50	32.36	nM	CHEMBL_ACT_5219049
ADRA1D	7.39	Ki	41	nM	CHEMBL_ACT_7673228
ADRA1D	7.08	IC50	83	nM	CHEMBL_ACT_7673227
ADRA2B	7	Ki	101	nM	CHEMBL_ACT_7673232
P19327	6.86	Ki	138	nM	CHEMBL_ACT_7675449
ADRA2B	6.66	IC50	220	nM	CHEMBL_ACT_7673231
P19327	6.62	IC50	242	nM	CHEMBL_ACT_7675448
HTR2C	6.62	Ki	238	nM	CHEMBL_ACT_7675457
ADRA2C	6.59	Ki	256	nM	CHEMBL_ACT_7673234
KCNH2	6.55	AC50	280	nM	CHEMBL_ACT_25117583
HTR2C	6.34	IC50	454	nM	CHEMBL_ACT_7675456
HRH1	6.28	Ki	525	nM	CHEMBL_ACT_7675343
CHRM4	6.27	Ki	537	nM	CHEMBL_ACT_7675377

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 indications (3 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	4	MONDO:0005485	EFO:0005407

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

Clinical trials

Total trials: 22.

Phase distribution

Phase	Trials
Not specified	9
PHASE4	5
PHASE3	5
PHASE1/PHASE2	1
PHASE2	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00209885	PHASE4	UNKNOWN	Optimal Multimodal Analgesia in Laparoscopic Cholecystectomy
NCT00445055	PHASE4	TERMINATED	Evaluation of 2 Doses of Intravenous Droperidol in the Prevention of Postoperative Nausea
NCT00702442	PHASE4	COMPLETED	Role of Droperidol in Postoperative Vomiting
NCT01434017	PHASE4	COMPLETED	Comparison of Three Different Prophylactic Treatments of Postoperative Nausea and Vomiting (PONV) in Children
NCT02282956	PHASE4	UNKNOWN	Ultrasound Guided Single Shot Block of Posterior Tibial Nerve for Postoperative Pain Relief After Hallux Valgus Surgery
NCT01432977	PHASE3	COMPLETED	Drug Interactions Between Paracetamol and Setrons in Pain Management
NCT01679093	PHASE3	COMPLETED	Antagonism Research Between Antiemetics Agents and Acetaminophen in Thyroidectomy’s Post-operative Analgesia.
NCT01942343	PHASE3	COMPLETED	Akathisia in Post Operative Outpatients Surgery
NCT02744495	PHASE3	COMPLETED	Prophylaxis of Postoperative Nausea and Vomiting After Cardiac Surgery
NCT05065567	PHASE3	TERMINATED	Haloperidol, Droperidol, Ondansetron in Cannabis Hyperemesis
NCT02858310	PHASE1/PHASE2	COMPLETED	E7 TCR T Cells for Human Papillomavirus-Associated Cancers
NCT04411069	PHASE2	COMPLETED	Simplified Algorithm for the Prevention of Postoperative Nausea and Vomiting in an Oncological Hospital
NCT07015528	EARLY_PHASE1	ENROLLING_BY_INVITATION	Assessment of Drug Liking In Peri-procedural Clinical Settings
NCT06726811	Not specified	RECRUITING	Droperidol and QTc Interval Changes in ED Patients
NCT00624208	Not specified	COMPLETED	The Effects of the Anti Nausea Drugs Droperidol and Ondansetron on the Way the Heart Recovers Between Beats
NCT01406860	Not specified	TERMINATED	Droperidol Versus Metoclopramide + Diphenhydramine for the Treatment of Primary Headaches
NCT01739985	Not specified	COMPLETED	Postoperative Vomiting in Children: Comparison Tri - Versus bi -Prophylaxis
NCT02600741	Not specified	COMPLETED	Family Intervention in Recent Onset Schizophrenia Treatment (FIRST)
NCT02625181	Not specified	COMPLETED	Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis
NCT03023462	Not specified	COMPLETED	Efficacy of an Anterior Quadratus Lumborum Block vs. a TAP-block for Inguinal Hernia Repair
NCT03677323	Not specified	COMPLETED	Evaluation of the Efficacy of VR on Pain and Anxiety When Performing an Ultrasound-controlled Ankle Block.
NCT05401058	Not specified	UNKNOWN	Low-dose Droperidol for Prevention of Postoperative Delirium in Elderly Patients After Non-cardiac Surgery

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).