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 46 Target ID: CHEMBL1899 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21107s5lbl.pdf	Antagonist 2778		0.29 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Irritable bowel syndrome 60 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21107s5lbl.pdf	Primary		Approved 8429	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
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
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
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
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
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
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
1.65 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

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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001	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 Page: S3BA2001

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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001
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 Page: S3BA2001	unhealthy, 45 n = 68 Health Status: unhealthy Condition: irritable bowel syndrome Age Group: 45 Sex: M+F Population Size: 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_medr_P15.pdf Page: S3BA2001

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2C19 1478 CYP2E1 882	CYP1A2 1054 CYP2C8 693 CYP2C19 991 CYP2E1 667	CYP3A 129 CYP2E1 128 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	inconclusive
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	no
CYP2E1 970	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf#page=5 Page: 5.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P4.pdf#page=8 Page: 8.0	yes
CYP2E1 970	inhibitor 3277 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 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2E1 667	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21107a_Lotronex_clinphrmr_P3.pdf#page=8 Page: 8.0	yes
CYP3A4 1737	substrate 3367 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 1054	substrate 3367 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 1647	inhibitor 1626 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
The FDA and The Lancet: an exchange.	2001 Aug 4	11503622
The FDA and The Lancet: an exchange.	2001 Aug 4	11503621
The FDA and The Lancet: an exchange.	2001 Aug 4	11503620
The FDA and The Lancet: an exchange.	2001 Aug 4	11503619
Possible mechanisms for ischemic colitis during alosetron therapy.	2001 Jul	11441889
Irritable bowel syndrome. A poorly understood disorder.	2001 Jul-Aug	11692885
Lotronex and the FDA: a fatal erosion of integrity.	2001 May 19	11377636
Effect of alosetron on theophylline pharmacokinetics.	2001 Nov	11736869
[Irritable bowel syndrome: diagnostic criteria and recent advancement of its pharmacological management].	2001 Oct	11680988
The short, sad history of alosetron.	2001 Oct	11560794
Effects of alosetron on spontaneous migrating motor complexes in murine small and large bowel in vitro.	2001 Oct	11557518
Gender-related differences in slowing colonic transit by a 5-HT3 antagonist in subjects with diarrhea-predominant irritable bowel syndrome.	2001 Sep	11569693
Alosetron controls bowel urgency and provides global symptom improvement in women with diarrhea-predominant irritable bowel syndrome.	2001 Sep	11569692
The treatment of irritable bowel syndrome.	2002 Aug	12182740
Serotonin-transporter polymorphism pharmacogenetics in diarrhea-predominant irritable bowel syndrome.	2002 Aug	12145795
From the Food and Drug Administration.	2002 Aug 14	12169049
Emerging treatments for irritable bowel syndrome.	2002 Jan	11772329
Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds.	2002 Jul	12184141
The effect of the 5-HT3 receptor antagonist, alosetron, on brain responses to visceral stimulation in irritable bowel syndrome patients.	2002 Jul	12144587
Alosetron to return to market.	2002 Jul 15	12132555
FDA approves restricted marketing of Lotronex.	2002 Jul-Aug	12184306
FDA allows controversial bowel drug back on to market.	2002 Jun 15	12086774
Review article: the complexity of drug development for irritable bowel syndrome.	2002 Mar	11876686
Sex and age differences in the pharmacokinetics of alosetron.	2002 Mar	11874386
Return of alosetron.	2002 May	12904154
FDA advisory panels recommend Lotronex be put back on market.	2002 May 4	11993482
Gateways to clinical trials.	2002 Oct	12500432
New developments in the diagnosis and treatment of irritable bowel syndrome.	2002 Oct	12228046
Alosetron: a case study in regulatory capture, or a victory for patients' rights?	2002 Sep 14	12228140
Regulatory role of 5-HT and muscarinic receptor antagonists on the migrating myoelectric complex in rats.	2003 Apr 25	12706477
Platelet serotonin transporter in patients with diarrhea-predominant irritable bowel syndrome both before and after treatment with alosetron.	2003 Dec	14687821
Advances in the management of irritable bowel syndrome.	2003 Dec	14602054
Efficacy of alosetron in irritable bowel syndrome: a meta-analysis of randomized controlled trials.	2003 Feb	12588472
[Visceral hypersensitivity: a concept within our reach].	2003 Jan	12643225
Lipid-induced colonic hypersensitivity in irritable bowel syndrome: the role of 5-HT3 receptors.	2003 Jan	12534414
Alosetron for irritable bowel syndrome. Risks of using alosetron are still unknown.	2003 Jan 4	12518769
Alosetron for irritable bowel syndrome. Senior vice president of GlaxoSmithKline responds.	2003 Jan 4	12511473
Gateways to clinical trials.	2003 Jan-Feb	12690708
Irritable bowel syndrome: an overview of diagnosis and pharmacologic treatment.	2003 Jun	12825862
Incidence of colonic ischemia, hospitalized complications of constipation, and bowel surgery in relation to use of alosetron hydrochloride.	2003 May	12809837
Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia.	2003 Nov 17	14612892
Gateways to clinical trials.	2003 Oct	14671684
Evaluation of drug treatment in irritable bowel syndrome.	2003 Oct	12968980
Treating irritable bowel syndrome: overview, perspective and future therapies.	2004 Apr	15037521
5-HT3-receptor antagonist inhibits visceral pain differently in chemical and mechanical stimuli in rats.	2004 Jan	14745121
Study design issues in irritable bowel syndrome.	2004 Jan 1	14687176
Safety and tolerability of tegaserod in irritable bowel syndrome management.	2004 Jan-Feb	14965152
Occurrence of colon ischemia in relation to irritable bowel syndrome.	2004 Mar	15056090
New options for soothing an irritable bowel.	2004 Mar	15029867
Therapy for irritable bowel syndrome.	2004 Mar 18	15031865

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 `Fri Dec 15 15:57:00 GMT 2023` Edited by `admin` on `Fri Dec 15 15:57:00 GMT 2023`
Record UNII	13Z9HTH115
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ALOSETRON

Official Name

English

ALOSETRON [MI]

Common Name

English

Alosetron [WHO-DD]

Common Name

English

ALOSETRON [VANDF]

Common Name

English

A03AE01

Code

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