ALOSETRON

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H18N4O
Molecular Weight	294.351
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1C2=CC=CC=C2C3=C1CCN(CC4=C(C)N=CN4)C3=O

InChI

InChIKey=JSWZEAMFRNKZNL-UHFFFAOYSA-N

InChI=1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19)

HIDE SMILES / InChI

Molecular Formula	C17H18N4O
Molecular Weight	294.351
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21107s5lbl.pdf | https://www.drugs.com/cdi/alosetron.html | https://www.ncbi.nlm.nih.gov/pubmed/10776833

Alosetron, marketed under the brand name Lotronex, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only. Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of the enteric nervous system. Alosetron is used for the treating women with severe irritable bowel syndrome (IBS) accompanied by severe diarrhea (usually lasting for 6 months or more). It is only prescribed to women who do not respond to other medicines and is not to be used by women whose main IBS problem is constipation.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 3a (5-HT3a) receptor 48 Target ID: CHEMBL1899 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21107s5lbl.pdf	Antagonist 2849		0.29 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Irritable bowel syndrome 61 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21107s5lbl.pdf	Primary		Approved 8583	LOTRONEX Approved Use LOTRONEX is indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of the gastrointestinal tract excluded, and not responded adequately to conventional therapy. Diarrhea-predominant IBS is severe if it includes diarrhea and one or more of the following: frequent and severe abdominal pain/discomfort, frequent bowel urgency or fecal incontinence, disability or restriction of daily activities due to IBS. Because of infrequent but serious gastrointestinal adverse reactions associated with LOTRONEX, the indication is restricted to those patients for whom the benefit-to-risk balance is most favorable. Clinical studies have not been performed to adequately confirm the benefits of LOTRONEX in men. LOTRONEX is a selective serotonin 5-HT3 antagonist indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of the gastrointestinal tract excluded, and not responded adequately to conventional therapy. (1) Severe IBS includes diarrhea and 1 or more of the following: frequent and severe abdominal pain/discomfort, frequent bowel urgency or fecal incontinence, disability or restriction of daily activities due to IBS. (1) Launch Date 2000

C_max

Value	Dose	Analyte	Population
43.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
14.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
40.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.35 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021107s013lbl.pdf	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021107s013lbl.pdf	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
66.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
36.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
49.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.65 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1.44 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1.52 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.45 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11874386	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ALOSETRON serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
18% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021107s013lbl.pdf			ALOSETRON plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	Disc. AE: Constipation, Gastrointestinal discomfort... AEs leading to discontinuation/dose reduction: Constipation (20%) Gastrointestinal discomfort (3%) Abdominal pain (8%) Nausea (9%) Vomiting (3%) Diarrhea (5%) Headaches (7%) Malaise and fatigue (3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf

AEs

AE	Significance	Dose	Population
Constipation	20% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Gastrointestinal discomfort	3% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Malaise and fatigue	3% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Vomiting	3% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Diarrhea	5% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Headaches	7% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Abdominal pain	8% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf
Nausea	9% Disc. AE	8 mg 2 times / day multiple, oral MTD Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf	unhealthy, 45 Health Status: unhealthy Age Group: 45 Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	substrate 1193 inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2C19 2057 CYP2E1 1060	CYP1A2 1197 CYP2C8 810 CYP2C19 1119 CYP2E1 729	CYP3A 142 CYP2E1 131 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	inconclusive
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2E1 1146	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP3A 317	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	yes
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2E1 729	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	yes	unlikely (co-administration study) Comment: Ketoconazole is a known strong inhibitor of CYP3A4. In a pharmacokinetic study, 38 healthy female subjects received ketoconazole 200 mg twice daily for 7 days, with coadministration of alosetron 1 mg on the last day. Ketoconazole increased mean alosetron plasma concentrations (AUC) by 29%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	yes	yes (co-administration study) Comment: Fluvoxamine is a known strong inhibitor of CYP1A2 and also inhibits CYP3A4, CYP2C9, and CYP2C19. In a pharmacokinetic study, 40 healthy female subjects received fluvoxamine in escalating doses from 50 to 200 mg/day for 16 days, with coadministration of alosetron 1 mg on the last day. Fluvoxamine increased mean alosetron plasma concentrations (AUC) approximately 6-fold and prolonged the half-life by approximately 3-fold. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/12873512/ Page: -

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:53783	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:53783
ChemicalBook	CB3107074	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3107074
eMolecules	10222191	https://www.emolecules.com/cgi-bin/more?vid=10222191
eMolecules	14090089	https://www.emolecules.com/cgi-bin/more?vid=14090089

PubMed

Title	Date	PubMed
Treating irritable bowel syndrome: overview, perspective and future therapies.	2004-04	15037521
Therapy for irritable bowel syndrome.	2004-03-18	15031865
Occurrence of colon ischemia in relation to irritable bowel syndrome.	2004-03	15056090
New options for soothing an irritable bowel.	2004-03	15029867
Safety and tolerability of tegaserod in irritable bowel syndrome management.	2004-02-18	14965152
Study design issues in irritable bowel syndrome.	2004-01-01	14687176
5-HT3-receptor antagonist inhibits visceral pain differently in chemical and mechanical stimuli in rats.	2004-01	14745121
Platelet serotonin transporter in patients with diarrhea-predominant irritable bowel syndrome both before and after treatment with alosetron.	2003-12	14687821
Advances in the management of irritable bowel syndrome.	2003-12	14602054
Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia.	2003-11-17	14612892
Alosetron and irritable bowel syndrome.	2003-11	14596662
Gateways to clinical trials.	2003-10	14671684
Evaluation of drug treatment in irritable bowel syndrome.	2003-10	12968980
Re: Brandt et al.--An evidence-based approach to the management of irritable bowel syndrome in North America.	2003-09	14499800
Irritable bowel syndrome: an overview of diagnosis and pharmacologic treatment.	2003-06	12825862
Incidence of colonic ischemia, hospitalized complications of constipation, and bowel surgery in relation to use of alosetron hydrochloride.	2003-05	12809837
Regulatory role of 5-HT and muscarinic receptor antagonists on the migrating myoelectric complex in rats.	2003-04-25	12706477
Gateways to clinical trials.	2003-04-15	12690708
Safety, efficacy and costs of pharmacotherapy for functional gastrointestinal disorders: the case of alosetron and its implications.	2003-04	12694084
Review: tegaserod or alosetron is effective for the irritable bowel syndrome.	2003-03-05	12614135
Efficacy of alosetron in irritable bowel syndrome: a meta-analysis of randomized controlled trials.	2003-02	12588472
Bad medicine. Why data from drug companies may be hard to swallow.	2003-02	12561450
Alosetron for irritable bowel syndrome. Risks of using alosetron are still unknown.	2003-01-04	12518769
Alosetron for irritable bowel syndrome. Senior vice president of GlaxoSmithKline responds.	2003-01-04	12511473
[Visceral hypersensitivity: a concept within our reach].	2003-01	12643225
Alosetron (Lotronex) is back: should I use it to treat my patients with irritable bowel syndrome?	2003-01	12549728
Lipid-induced colonic hypersensitivity in irritable bowel syndrome: the role of 5-HT3 receptors.	2003-01	12534414
Alosetron in irritable bowel syndrome: strategies for its use in a common gastrointestinal disorder.	2003	12930162
Tegaserod and other serotonergic agents: what is the evidence?	2003	12776001
Irritable bowel syndrome genophenomics: correlation of serotonin-transporter polymorphisms and alosetron response.	2003	12746730
Patient satisfaction with alosetron for the treatment of women with diarrhea-predominant irritable bowel syndrome.	2002-12	12492201
Excitation of rat colonic afferent fibres by 5-HT(3) receptors.	2002-11-01	12411529
Systematic review on the management of irritable bowel syndrome in North America.	2002-11	12425586
Evidence-based position statement on the management of irritable bowel syndrome in North America.	2002-11	12425585
Gateways to clinical trials.	2002-10	12500432
FDA OK's two drugs for irritable bowel syndrome. The arsenal of IBS drugs is growing, but diagnosis is tricky.	2002-10	12416480
Condition-specific deactivation of brain regions by 5-HT3 receptor antagonist Alosetron.	2002-10	12360456
New developments in the diagnosis and treatment of irritable bowel syndrome.	2002-10	12228046
Alosetron: a case study in regulatory capture, or a victory for patients' rights?	2002-09-14	12228140
FDA advisers warn of more deaths if drug is relaunched.	2002-09-14	12228121
Alosetron for irritable bowel syndrome.	2002-09-14	12228116
FDA approves restricted marketing of Lotronex.	2002-08-20	12184306
From the Food and Drug Administration.	2002-08-14	12169049
Alosetron (lotronex) revisited.	2002-08-05	12163838
Contemporary thoughts on the treatment of irritable bowel syndrome.	2002-08	12229060
The treatment of irritable bowel syndrome.	2002-08	12182740
Serotonin-transporter polymorphism pharmacogenetics in diarrhea-predominant irritable bowel syndrome.	2002-08	12145795
Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds.	2002-07	12184141
Return of alosetron.	2002-05	12904154
Adverse drug reaction update.	2002	12503258

Patents

Sample Use Guides

In Vivo Use Guide

Usual Adult Dose for Irritable Bowel Syndrome -Initial dose: 0.5 mg orally twice a day -Maintenance dose: 0.5 mg orally once or twice a day; can be increased up to 1 mg orally twice a day after 4 weeks of treatment.

Route of Administration: Oral

In Vitro Use Guide

Alosetron blocked the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons in vitro, with half-maximal inhibition at approximately 55 nmol/L.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:14:17 GMT 2025` Edited by `admin` on `Mon Mar 31 18:14:17 GMT 2025`
Record UNII	13Z9HTH115
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

A03AE01

Preferred Name

English

ALOSETRON

Official Name

English

ALOSETRON [MI]

Common Name

English

Alosetron [WHO-DD]

Common Name

English

ALOSETRON [VANDF]

Common Name

English

alosetron [INN]

Common Name

English

1H-PYRIDO(4,3-B)INDOL-1-ONE, 2,3,4,5-TETRAHYDRO-5-METHYL-2-((5-METHYL-1H-IMIDAZOL-4-YL)METHYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C94726