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Pharmaceutical compound
Itasetron
Clinical data
Other namesDAU-6215; DAU6215; U-98079; U98079
Routes of
administration
Oral
Drug classSerotonin 5-HT3 receptor antagonist
ATC code
  • None
Pharmacokinetic data
Bioavailability68%
Elimination half-life10.6–12.4 hours
Identifiers
  • N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3H-benzimidazole-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H20N4O2
Molar mass300.362 g·mol−1
3D model (JSmol)
  • CN1[C@@H]2CC[C@H]1CC(C2)NC(=O)N3C4=CC=CC=C4NC3=O
  • InChI=1S/C16H20N4O2/c1-19-11-6-7-12(19)9-10(8-11)17-15(21)20-14-5-3-2-4-13(14)18-16(20)22/h2-5,10-12H,6-9H2,1H3,(H,17,21)(H,18,22)/t10?,11-,12+
  • Key:RWXRJSRJIITQAK-YOGCLGLASA-N

Itasetron (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names DAU-6215 and U-98079) is a selective serotonin 5-HT3 receptor antagonist which was under development for the treatment of anxiety disorders, cognition disorders, nausea and vomiting, and psychotic disorders but was never marketed.[3] It is taken orally. Itasetron was first described in the scientific literature by 1990.[5] The drug was under development by Boehringer Ingelheim.[3] It reached phase 3 clinical trials for nausea and vomiting and phase 2 trials for anxiety disorders.

See also

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References

[edit]
  1. 1 2 "Delving into the Latest Updates on Itasetron with Synapse". Synapse. 16 May 2026. Retrieved 5 June 2026.
  2. Turconi M, Nicola M, Quintero MG, Maiocchi L, Micheletti R, Giraldo E, et al. (August 1990). "Synthesis of a new class of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives as highly potent 5-HT3 receptor antagonists". Journal of Medicinal Chemistry. 33 (8): 2101–2108. doi:10.1021/jm00170a009. PMID 1695682.