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Ondansetron

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Also known as A04AA01DesmethylondansetronEUR-1025GR-38032NSC-757870Zofran odtZuplenzOndansetroneSID124893606SID144206599SID170464701C0164500

Summary

Ondansetron (CHEMBL46) is an approved small molecule (ATC A04AA01); indicated across 42 conditions including neoplasm and gastroenteritis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A04AA01
  • Indications: 42 conditions
  • Clinical trials: 332
  • Chemistry: 293.4 Da · C18H19N3O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL46
NameOndansetron
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4595
ATCA04AA01
Molecular formulaC18H19N3O
Molecular weight293.4
InChIKeyFELGMEQIXOGIFQ-UHFFFAOYSA-N

SMILES: CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C

IUPAC name: 9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one

Also known as: A04AA01, Desmethylondansetron, EUR-1025, GR-38032, NSC-757870, Ondansetron, Zofran odt, Zuplenz, ondansetron, Ondansetrone, ONDANSETRON, SID124893606

Parent form; salt/anhydrous children: CHEMBL1201111, CHEMBL1487310, CHEMBL3186492

Patent coverage: 10,632 distinct patent families (41,386 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 41,224 (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).

GeneTargetActionpAffinityCancer dependencyUniProt
5-HT3ABAntagonist7.8
5-HT3AAntagonist8.3

Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, 5-hydroxytryptamine receptor 2B, 5-hydroxytryptamine receptor 3A, Neuronal acetylcholine receptor; alpha4/beta2, Neuronal acetylcholine receptor; alpha3/beta4, GABA-A receptor; anion channel, Solute carrier family 22 member 3, Serotonin 2 (5-HT2) receptor.

Bioactivity

ChEMBL activities: 71 potent at pChembl ≥ 5 of 79 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HTR3E10.1Kd0.08nMCHEMBL_ACT_767123
HTR3E10.1Kd0.08nMCHEMBL_ACT_912501
HTR3A10.05IC500.09nMCHEMBL_ACT_12168379
P355639.8IC500.16nMCHEMBL_ACT_12168378
HTR3E9.4Kd0.4nMCHEMBL_ACT_767122
HTR3E9.2Kd0.63nMCHEMBL_ACT_912500
P355639.11Ki0.77nMCHEMBL_ACT_13457834
P355639.11Ki0.77nMCHEMBL_ACT_779355
P355639Ki1nMCHEMBL_ACT_1007868
P355638.92Ki1.2nMCHEMBL_ACT_574333
P355638.85IC501.4nMCHEMBL_ACT_214234
P355638.81IC501.54nMCHEMBL_ACT_1222618
P355638.8Ki1.6nMCHEMBL_ACT_773668
P355638.8Ki1.6nMCHEMBL_ACT_779165
P355638.71IC501.95nMCHEMBL_ACT_1093786
P355638.71IC501.95nMCHEMBL_ACT_152878
P355638.7Kd2nMCHEMBL_ACT_294196
P355638.61Ki2.46nMCHEMBL_ACT_305310
P355638.61Ki2.46nMCHEMBL_ACT_305311
HTR2B8.6Ki2.5nMCHEMBL_ACT_25553828
HTR3A8.55Ki2.8nMCHEMBL_ACT_12168555
P355638.5Ki3.16nMCHEMBL_ACT_416583
P355638.5Ki3.16nMCHEMBL_ACT_517291
P355638.48Ki3.3nMCHEMBL_ACT_648199
P355638.48Ki3.31nMCHEMBL_ACT_767126
HTR3A8.47Ki3.4nMCHEMBL_ACT_3523727
P355638.27Ki5.37nMCHEMBL_ACT_781923
P355638.21Ki6.16nMCHEMBL_ACT_599863
P355638.19Ki6.5nMCHEMBL_ACT_146279
P355638.17IC506.8nMCHEMBL_ACT_80409

Target pathways

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

Indications & clinical

Indications

42 indications (6 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).

IndicationTrial phaseMONDOEFO
neoplasm4MONDO:0005070MONDO:0004992
gastroenteritis3MONDO:0002269EFO:1001463
cervical carcinoma3MONDO:0005131EFO:0001061
HIV infectious disease3MONDO:0005109EFO:0000764
irritable bowel syndrome3MONDO:0005052EFO:0000555
hypotensive disorder3MONDO:0005468EFO:0005251
alcohol abuse3MONDO:0002046MONDO:0002046
female reproductive organ cancer3MONDO:0001416EFO:1001331
obsessive-compulsive disorder2MONDO:0008114EFO:0004242
cocaine dependence2MONDO:0005186EFO:0002610
neoplasm of mature B-cells2MONDO:0004949EFO:0000096
sarcoma2MONDO:0005089EFO:0000691
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
nicotine dependence2MONDO:0008575EFO:0003768
non-Hodgkin lymphoma2MONDO:0018908EFO:0005952
breast neoplasm2MONDO:0021100EFO:0003869
methamphetamine dependence2MONDO:0005419EFO:0004701
cholecystitis2MONDO:0002155HP:0001082
glioma2MONDO:0021042MONDO:0100342
gastroparesis2MONDO:0006769EFO:1000948
dementia2MONDO:0001627HP:0000726
tonsillitis2MONDO:0001039MONDO:0001039
brain disorder1MONDO:0005560EFO:0005774
neuralgia1MONDO:0021667EFO:0005762
brain injury1MONDO:0043510MONDO:0043510
opiate dependence1MONDO:0005530EFO:0005611
small cell lung carcinoma1MONDO:0008433EFO:0000702

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

Clinical trials

Total trials: 332.

Phase distribution

PhaseTrials
Not specified88
PHASE479
PHASE257
PHASE356
PHASE133
PHASE2/PHASE39
PHASE1/PHASE25
EARLY_PHASE15

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04150614PHASE4RECRUITINGBMT-08: A Comparative Effectiveness Study of Transdermal Granisetron to Ondansetron
NCT05844501PHASE4RECRUITINGOndansetron for the Management of Atrial Fibrillation
NCT06704139PHASE4NOT_YET_RECRUITINGRole of Prophylactic Antiemetics in Women Receiving Intrathecal Morphine and Lipophilic Opioids Added to Bupivacaine for Cesarean Section
NCT06729307PHASE4NOT_YET_RECRUITINGOndansetron Combined with Dyclonine Hydrochloride to Improve Patient Experience in Unsedated Esophagogastro-duodenoscopy
NCT06747975PHASE4NOT_YET_RECRUITINGPreventative Effect of Combining Dexamethasone with Ondansetron on Postoperative Nausea, Vomiting and Shivering in Children Undergoing Caudal Anesthesia on Hypospadias Surgery
NCT07088601PHASE4NOT_YET_RECRUITINGEfficacy of Oral Ondansetron Strips on Prevention of Post-Spinal Shivering
NCT07264738PHASE4ACTIVE_NOT_RECRUITINGOral Ondansetron to Improve Patient Experience of Unsedated Esophagogastroduodenoscopy Pilot Study
NCT07336680PHASE4NOT_YET_RECRUITINGEffect of Ondansetron on Patient Tolerance, Efficacy and Endoscopist Workload in Unsedated Endoscopy for Upper Gastrointestinal Bleeding
NCT00429832PHASE4COMPLETEDA RCT of Ondansetron and Promethazine in the Treatment of Nausea and Vomiting in the Emergency Department
NCT00674713PHASE4COMPLETEDEffect of Acupuncture on Postoperative Nausea and Vomiting
NCT00734929PHASE4COMPLETEDAprepitant With Dexamethasone Versus Ondansetron With Dexamethasone for PONV Prophylaxis in Patients Having Craniotomy
NCT00738621PHASE4COMPLETEDCombination Antiemetic Regimen for Prevention of PONV in Breast Surgery Patients
NCT00745004PHASE4COMPLETEDOndansetron for the Treatment of IBS With Diarrhoea (IBS-D)
NCT00778011PHASE4COMPLETEDUncomplicated Nausea and Vomiting in the Emergency Department
NCT00793663PHASE4COMPLETEDDepth of Hypnosis and Postoperative Nausea and Vomiting During Xenon Anaesthesia
NCT00796497PHASE4COMPLETEDOndansetron in Treatment Resistant Obsessive Compulsive Disorder (OCD)
NCT00825071PHASE4COMPLETEDDexamethasone for Postoperative Nausea and Vomiting
NCT00878228PHASE4COMPLETEDAntiemetic Prophylaxis for Postdischarge Nausea and Vomiting After Hip Arthroscopy
NCT01007500PHASE4COMPLETEDEffect of Dexamethasone Combined With Ondansetron on Postoperative Nausea and Vomiting in Patients With Patient-controlled Analgesia After Video-assisted Thoracoscopic Surgery
NCT01050270PHASE4COMPLETEDScottish and Newcastle Anti-emetic Pre-treatment for Paracetamol Poisoning Study (SNAP)
NCT01303536PHASE4COMPLETEDOndansetron Augmentation in Treatment-resistant OCD
NCT01352130PHASE4COMPLETEDGranisetron Versus Ondansetron: Comparative Effects on ECG, QTc
NCT01434017PHASE4COMPLETEDComparison of Three Different Prophylactic Treatments of Postoperative Nausea and Vomiting (PONV) in Children
NCT01474915PHASE4COMPLETEDAprepitant Versus Ondansetron in Preoperative Triple-therapy Treatment of Nausea and Vomiting
NCT01636947PHASE4COMPLETEDA Korean Study of Efficacy and Safety of Aprepitant-based Triple Regimen for the Prevention of Chemotherapy-Induced Nausea and Vomiting in the First Cycle of Moderately Emetogenic Chemotherapy (Non-doxorubicin Hydrochloride [Adriamycin] and Cyclophosphamide Regimens) (MK-0869-225) (KMEC)
NCT01837394PHASE4COMPLETEDUltrasound-guided Blocks for Ambulatory Knee Arthroscopy
NCT01870635PHASE4COMPLETEDOndansetron Administration to WELL Children With Gastroenteritis Associated Vomiting in EDs in Pakistan
NCT01870648PHASE4COMPLETEDOndansetron Administration to Children With Gastroenteritis, Vomiting and SOME Dehydration in EDs in Pakistan
NCT01876290PHASE4COMPLETEDDexamethasone and Ondansetron Versus Placebo for Postoperative Nausea and Vomiting
NCT01896440PHASE4WITHDRAWNHeart Safety Study of Ondansetron in Children Receiving Chemotherapy
NCT01913990PHASE4UNKNOWNPrevention of Chemotherapy Induced Nausea and Vomiting in Breast Cancer Patients.
NCT02021851PHASE4COMPLETEDPrevention of Nausea and Vomiting in Patients After Surgery
NCT02082678PHASE4COMPLETEDOndansetron for Bipolar Disorder and Alcohol Use Disorders
NCT02085577PHASE4COMPLETEDThe Effect of Intraoperative Ketamine on Opioid Consumption and Pain After Spine Surgery in Opioid-dependent Patients
NCT02296333PHASE4COMPLETEDOndansetron’s Opposite Effect on Postoperative Analgesia of Acetaminophen
NCT02327923PHASE4COMPLETEDIntraoperative Lidocaine Infusion vs. Esmolol Infusion for Postoperative Analgesia in Laparoscopic Cholecystectomy
NCT02382146PHASE4COMPLETEDPrevention of Postoperative Nausea and Vomiting
NCT02386059PHASE4UNKNOWNPrevention of Postoperative Nausea and Vomiting in Patients Undergoing Vitrectomy Under Local Anesthesia
NCT02468323PHASE4COMPLETEDProphylactic Antiemetic Efficacy of Palonosetron Versus Ondansetron for Cesarean Sections Under Regional Anesthesia
NCT02541019PHASE4COMPLETEDProphylactic Antiemetic Efficacy of Palonosetron Versus Ondansetron for the Prophylaxis of Postoperative Nausea and Vomiting (PONV) in Women Over 60 Years Undergoing Laparoscopic Cholecystectomy

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of CPIC Guideline for ondansetron and CYP2D6CPICCYP2D6yes

PharmGKB also curates 6 clinical and 22 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 18

This page pulls from 18 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclinical_trialsefogtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondopatent_compoundpharmgkbpharmgkb_guidelinepubchemuniprot