Dolasetron

Summary

Dolasetron (CHEMBL2368925) is an approved small molecule (ATC A04AA04); indicated across 3 conditions including fibromyalgia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A04AA04
• Indications: 3 conditions
• Clinical trials: 5
• Chemistry: 324.4 Da · C19H20N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2368925
Name	Dolasetron
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3033818
ATC	A04AA04
Molecular formula	C19H20N2O3
Molecular weight	324.4
InChIKey	UKTAZPQNNNJVKR-AKJUYKBHSA-N

SMILES: C1[C@@H]2CC(C[C@H]3N2CC(=O)C1C3)OC(=O)C4=CNC5=CC=CC=C54

IUPAC name: [(3S,7R)-10-oxo-8-azatricyclo[5.3.1.03,8]undecan-5-yl] 1H-indole-3-carboxylate

Also known as: Dolasetron, dolasetron, DOLASETRON

Parent form; salt/anhydrous children: CHEMBL2368924, CHEMBL2373322

Patent coverage: 9 distinct patent families (9 SureChEMBL compound mentions), from 1 matched compound structure(s). 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: 3 (assay-derived). Sample: 5-hydroxytryptamine receptor 3A, Sodium-dependent serotonin transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR3A	6.02	AC50	950	nM	CHEMBL_ACT_25149497
KCNH2	5.22	IC50	6026	nM	CHEMBL_ACT_1427114
KCNH2	5.22	IC50	6026	nM	CHEMBL_ACT_2645512
KCNH2	5.22	IC50	5950	nM	CHEMBL_ACT_305245
SLC6A4	5.03	AC50	9306	nM	CHEMBL_ACT_25151723

Target pathways

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

Indications & clinical

Indications

3 indications (2 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
fibromyalgia	3	MONDO:0005546	EFO:0005687

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

Clinical trials

Total trials: 5.

Phase distribution

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

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01636947	PHASE4	COMPLETED	A 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)
NCT00820326	PHASE3	COMPLETED	Efficacy of Dolasetron in Patients With Fibromyalgia
NCT06593782	PHASE2	NOT_YET_RECRUITING	Evaluating the Efficacy and Safety of HSK21542 Injection in Chemotherapy-induced Nausea and Vomiting
NCT00511823	PHASE1	COMPLETED	The Pharmacokinetic Interaction Between Oral Casopitant and Oral Dolasetron, Granisetron or Rosiglitazone in Subjects
NCT07515027	Not specified	RECRUITING	Electroacupuncture Plus 5-HT3 Receptor Inhibitor for PONV Prevention in High-Risk Patients Undergoing Thoracoscopic Lung Cancer Surgery

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

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