Alosetron

Alosetron
Clinical data
Trade namesLotronex
AHFS/Drugs.comMonograph
MedlinePlusa601230
Routes of
administration		Oral (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability50–60%
Protein binding82%
MetabolismHepatic (including CYP2C9, CYP3A4 and CYP1A2)
Elimination half-life1.5–1.7 hours
ExcretionRenal 73%, faecal 24%
Identifiers
  • 5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H18N4O
Molar mass294.358 g·mol−1
3D model (JSmol)
  • Cc1nc[nH]c1CN2CCc4c(C2=O)c3ccccc3n4C
  • 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) checkY
  • Key:JSWZEAMFRNKZNL-UHFFFAOYSA-N checkY
  (verify)

Alosetron, sold under the brand name Lotronex among others, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in females only.

It was patented in 1987 and approved for medical use in 2002.[2] It is currently marketed by Prometheus Laboratories Inc. (San Diego). Alosetron was withdrawn from the market in 2000 owing to the occurrence of serious life-threatening gastrointestinal adverse effects, but was reintroduced in 2002 with availability and use restricted.

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  2. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495.