Lerisetron

Summary

Lerisetron (CHEMBL56900) is a phase-3 clinical-stage small molecule; indicated across 1 condition.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 292.4 Da · C18H20N4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL56900
Name	Lerisetron
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	65997
Molecular formula	C18H20N4
Molecular weight	292.4
InChIKey	PWWDCRQZITYKDV-UHFFFAOYSA-N

SMILES: C1CN(CCN1)C2=NC3=CC=CC=C3N2CC4=CC=CC=C4

IUPAC name: 1-benzyl-2-piperazin-1-ylbenzimidazole

Also known as: Lerisetron, LERISETRON, LerisetronÊ, LerisetronÂ

Patent coverage: 230 distinct patent families (860 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 858 (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

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: 5-hydroxytryptamine receptor 3A, Serotonin 3 (5-HT3) receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR3A	9.44	Ki	0.36	nM	CHEMBL_ACT_836214
P35563	9.21	Ki	0.62	nM	CHEMBL_ACT_449018
P35563	9.2	Ki	0.63	nM	CHEMBL_ACT_661404
P35563	9.2	Ki	0.63	nM	CHEMBL_ACT_833276

Target pathways

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

Indications & clinical

Indications

1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00004219	PHASE3	UNKNOWN	Lerisetron Compared With Granisetron in Preventing Nausea and Vomiting in Men Being Treated With Radiation Therapy for Stage I Seminoma

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).