Compounds > lerisetron
Page last updated: 2024-12-06

lerisetron

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Lerisetron is a selective 5-HT3 receptor antagonist. It is used to prevent nausea and vomiting associated with chemotherapy and radiation therapy. Lerisetron is effective in treating nausea and vomiting associated with chemotherapy and radiation therapy. It is thought to work by blocking the action of serotonin in the gastrointestinal tract, which helps to reduce nausea and vomiting. Lerisetron is well-tolerated and has a relatively low incidence of side effects. Lerisetron is important because it can help to improve the quality of life for patients undergoing chemotherapy and radiation therapy. It is studied to understand its mechanism of action and to develop new and more effective treatments for nausea and vomiting.'

Cross-References

ID SourceID
PubMed CID65997
CHEMBL ID56900
SCHEMBL ID141124
MeSH IDM0296522

Synonyms (30)

Synonym
lerisetron
CHEMBL56900 ,
1-benzyl-2-piperazin-1-ylbenzimidazole
bdbm50103072
1-benzyl-2-piperazin-1-yl-1h-benzoimidazole
q36r82sxrg ,
143257-98-1
1-benzyl-2-(1-piperazinyl)benzimidazole
lerisetron [inn]
unii-q36r82sxrg
AKOS015957715
lerisetron [who-dd]
S2644
SCHEMBL141124
PWWDCRQZITYKDV-UHFFFAOYSA-N
1-benzyl-2-(piperazin-1-yl)-1h-benzimidazole
DTXSID90162368
DB12964
Z2049693817
Q6528811
EX-A7543
BCP33052
1-benzyl-2-(piperazin-1-yl)-1h-benzo[d]imidazole
L-175
1-benzyl-2-piperazin-1-ylbenzimidazole.
trans-cyclohexane-1,3-diamine?hydrochloride
EN300-242559
CS-0024958
HY-105090
1-benzyl-2-(piperazin-1-yl)-1h-1,3-benzodiazole

Research Excerpts

Overview

Lerisetron is a 5-hydroxytryptamine3 receptor antagonist under development by FAES Farma. It is being developed for the potential treatment of emesis resulting from chemotherapy.

ExcerptReferenceRelevance
"Lerisetron is a 5-hydroxytryptamine3 receptor antagonist under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. "( Lerisetron. FAES.
Huckle, R, 2003)		3.2
"Lerisetron is a new 5-HT3 receptor antagonist chemically unrelated to other antagonists like Ondansetron."( Antiemetic effects of Lerisetron in radiation-induced emesis in the dog.
De Miguel, E; Gomez-de-Segura, IA; Grande, AG, 1998)		1.34

Pharmacokinetics

ExcerptReferenceRelevance
" Additionally, a pharmacodynamic study was performed."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E, )		0.37
"Both pharmacokinetic changes (decreased volume of distribution and clearance and increased elimination half-life) and pharmacodynamic alterations (decrease in total and unbound EC(50)) may be responsible for the different responses to lerisetron observed in old rats."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E, )		0.55

Dosage Studied

ExcerptRelevanceReference
" A mixed-effects population study was carried out in order to analyze the sparse data and to create covariate models which could be used to derive dosage recommendations."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E, )		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki1.00000.00010.601710.0000AID5322
DRattus norvegicus (Norway rat)Ki0.00060.00010.610010.0000AID6286
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.00060.00010.25675.8000AID6286
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki1.00000.00010.739610.0000AID4415
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.00060.00020.24622.0000AID6286
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.00060.00020.18872.0000AID6286
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.00060.00020.484110.0000AID5874; AID6286; AID6292
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00040.00000.74119.9000AID6379
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00010.54948.4000AID61535
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00060.00000.437510.0000AID6286
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.00060.00020.502310.0000AID5874; AID6286; AID6292
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID231268Ratio of binding affinity (Ki) of tryptophan tyrosine W89Y to Kd of wild type receptor.2001Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
AID4415In vitro by displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor on rat cortical membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID177157In vivo effective dose against Bezold-Jarisch reflex evoked by 5-HT in urethane-anesthetized rats1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID231266Ratio of binding affinity (Ki) of arginine alanine R91A to Kd of wild type receptor.2001Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
AID231267Ratio of binding affinity (Ki) of tryptophan phenylalanine W89F to Kd of wild type receptor.2001Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
AID6292In vitro by displacement of [3H]LY-278584 from 5-hydroxytryptamine 3 receptor on rat entorhinal cortex1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID5874Binding affinity towards rat 5-hydroxytryptamine 3 receptor was evaluated2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.
AID6160Binding affinity towards 5-hydroxytryptamine 4 receptor in striatum membranes of guinea-pig brain was evaluated2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.
AID6379Binding affinity against human 5-hydroxytryptamine 3A receptor2001Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
AID6194In vitro by displacement of [3H]GR-113808 from 5-hydroxytryptamine 4 receptor on guinea pig striatal membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID63797In vitro by displacement of [3H]raclopride from Dopamine receptor D2 on rat striatal membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID5322Binding affinity was evaluated in vitro by displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor on rat cortical membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
AID61535Binding affinity towards Dopamine receptor D2 in rat was evaluated2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT(3) ligands.
AID6286Rat 5-hydroxytryptamine 3 receptor (5-HT3) antagonist1998Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12
Arylpiperazines with serotonin-3 antagonist activity: a comparative molecular field analysis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (38.46)18.2507
2000's8 (61.54)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.39

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.39 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
8-hydroxy-2-(di-n-propylamino)tetralin
8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively		1.9910phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
granisetron
[no description available]		2.420aromatic amide;
indazoles
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		1.9910aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
ly 278584
LY 278584: structure given in first source; RN given refers to cpd without isomeric designation		1.9910aromatic amide;
indazoles
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		1.9910carbazoles
piperazine
[no description available]		2.0110azacycloalkane;
piperazines;
saturated organic heteromonocyclic parent		anthelminthic drug
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		1.9910organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.0110amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0110erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		2.0110arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		1.9910indazole
tropisetron
Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.		2.420indolyl carboxylic acid
sb 203186
[no description available]		1.9910indolyl carboxylic acid
granisetron
Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.. granisetron : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 1-methyl-1H-indazole-3-carboxylic acid with the primary amino group of (3-endo)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine. A selective 5-HT3 receptor antagonist, it is used (generally as the monohydrochloride salt) to manage nausea and vomiting caused by cancer chemotherapy and radiotherapy, and to prevent and treat postoperative nausea and vomiting.		2.0110aromatic amide;
indazoles
piperidines
Piperidines: A family of hexahydropyridines.		4.89110
ConditionIndicatedRelationship StrengthStudiesTrials
Emesis
[description not available]		03.6130
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		02.0110
Vomiting
The forcible expulsion of the contents of the STOMACH through the MOUTH.		03.6130
Benign Neoplasms
[description not available]		01.9910
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		01.9910
Bradyarrhythmia
[description not available]		02.4120
Bradycardia
Cardiac arrhythmias that are characterized by excessively slow HEART RATE, usually below 50 beats per minute in human adults. They can be classified broadly into SINOATRIAL NODE dysfunction and ATRIOVENTRICULAR BLOCK.		02.4120