Itasetron

Itasetron
Clinical data
Other namesDAU-6215; DAU6215; U-98079; U98079
Routes of
administration		Oral[1][2]
Drug classSerotonin 5-HT3 receptor antagonist
ATC code
  • None
Pharmacokinetic data
Bioavailability68%[2]
Elimination half-life10.6–12.4 hours[2]
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.[1][3][2][4] It is taken orally.[1] Itasetron was first described in the scientific literature by 1990.[5] The drug was under development by Boehringer Ingelheim.[1][3][2] It reached phase 3 clinical trials for nausea and vomiting and phase 2 trials for anxiety disorders.[1][2]

See also

References

  1. ^ a b c d e "Itasetron". AdisInsight. 22 July 2011. Retrieved 5 June 2026.
  2. ^ a b c d e f "Itasetron. DAU 6215, U 98079". Drugs in R&D. 2 (4): 243–244. October 1999. doi:10.2165/00126839-199902040-00003. PMID 10659399.
  3. ^ a b "Delving into the Latest Updates on Itasetron with Synapse". Synapse. 16 May 2026. Retrieved 5 June 2026.
  4. ^ Sagrada A, Turconi M, Bonali P, Schiantarelli P, Micheletti R, Montagna E, et al. (1991). "Antiemetic activity of the new 5-HT3 antagonist DAU 6215 in animal models of cancer chemotherapy and radiation". Cancer Chemotherapy and Pharmacology. 28 (6): 470–474. doi:10.1007/BF00685825. PMID 1834359.
  5. ^ 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.
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