alosetron

Trade name: lotronex

Small moleculeapproved

Approved

Feb 9, 2000

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. — NCATS

Clinical trial activity

6 trials · 5 clinical orgs · 15 marketing orgs

Phase 1
0
Phase 2
4
Phase 3
3
Phase 4
2

Earliest trial started Jun 1, 2003 (NCT00067561)

Timeline

2000s

  1. Feb 9, 2000

    Earliest FDA Approval

  2. Feb 9, 2000

    Sebela Pharmaceuticals — NDA Secondary Org

  3. Feb 9, 2000

    LEGACY PHARMA — Marketing Organization

  4. Feb 11, 2000

    Glaxo Wellcome — First NDA Organization

  5. Feb 11, 2000

    Glaxo Wellcome — NDA Organization

  6. Jan 1, 2003

    Earliest Phase 2 Sponsor(trial)

  7. Jan 1, 2003

    Earliest Phase 3 Sponsor(trial)

2010s

  1. May 4, 2015

    West-Ward Pharmaceutical — Marketing Organization

  2. May 4, 2015

    Hikma — Marketing Organization

  3. Dec 22, 2016

    Amneal Pharmaceuticals — Marketing Organization

  4. Feb 23, 2018

    Par Pharmaceuticals — Marketing Organization

  5. Feb 23, 2018

    Bristol-Myers Squibb — Marketing Organization

  6. Feb 23, 2018

    Endo Pharmaceuticals — Marketing Organization

  7. Feb 23, 2018

    PH HEALTH — Marketing Organization

  8. Jan 14, 2019

    Rising Pharmaceuticals — Marketing Organization

  9. Sep 16, 2019

    Eywa Pharma — Marketing Organization

  10. Sep 16, 2019

    HIBROW HLTHCARE — Marketing Organization

2020s

  1. Sep 9, 2020

    MannKind Corp — Marketing Organization

  2. Sep 9, 2020

    Mankind Pharma — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewFeb 9, 2000

Chemistry & pharmacology

Loading structure…

SMILES

Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O
Mol. weight
294.36 g/mol
Lipinski Ro5
Pass
Rule of 3
Yes
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one
  • 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one
  • 2,3,4,5-tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one monohydrochloride
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron
  • alosetron hcl
  • alosetron hcl
  • alosetron hcl
  • alosetron hydrochloride
  • alosetron hydrochloride
  • alosetron hydrochloride
  • alosetron hydrochloride
  • alosetron hydrochloride
  • alosetron hydrochloride
  • alosetron monohydrochloride
  • alosetron monohydrochloride
  • glaxosmithkline brand of alosetron hydrochloride
  • gr68755
  • gr68755
  • gr 68755
  • gr-68755c
  • gr-68755c
  • lotronex
  • lotronex
  • lotronex
  • lotronex

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05583266Phase 4Nov 1, 2022Capital Medical University, Yiling Pharmaceutical Inc.
NCT05284448Phase 3Feb 1, 2022Ain Shams University, Al Azhar University
NCT00370032Phase 4Dec 1, 2006GlaxoSmithKline
NCT01855711Phase 2Sep 18, 2003GlaxoSmithKline
NCT00067457Phase 3Jun 1, 2003GlaxoSmithKline
NCT00067561Phase 3Jun 1, 2003GlaxoSmithKline
Showing 6 of 6 trials
Page 1 / 1

Organizations

Research & Development (5)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GlaxoSmithKlineFor profit4432003
Ain Shams UniversityAcademic/Hospital1012022
Al Azhar UniversityAcademic/Hospital1112022
Capital Medical UniversityAcademic/Hospital1112022
Yiling Pharmaceutical Inc.For profit1012022
5 organizations
Page 1 / 1

Marketing (17)

OrganizationOrg typeRelationshipDate
Amneal PharmaceuticalsFor profitMKTGDec 22, 2016
Bristol-Myers SquibbFor profitMKTGFeb 23, 2018
Endo PharmaceuticalsFor profitMKTGFeb 23, 2018
Eywa PharmaFor profitMKTGSep 16, 2019
Glaxo WellcomeFor profitNDAFeb 11, 2000
HIBROW HLTHCAREFor profitMKTGSep 16, 2019
HikmaFor profitMKTGMay 4, 2015
HikmaFor profitSYNMay 4, 2015
LEGACY PHARMAFor profitMKTGFeb 9, 2000
Mankind PharmaFor profitMKTGSep 9, 2020
MannKind CorpFor profitMKTGSep 9, 2020
PH HEALTHFor profitMKTGFeb 23, 2018
Par PharmaceuticalsFor profitMKTGFeb 23, 2018
Rising PharmaceuticalsFor profitMKTGJan 14, 2019
Rising PharmaceuticalsFor profitSYNJan 14, 2019
Sebela PharmaceuticalsFor profitNDA2Feb 9, 2000
West-Ward PharmaceuticalFor profitMKTGMay 4, 2015