itasetron

Itasetron is a small molecule antiemetic that acts as a selective antagonist of the serotonin 5-hydroxytryptamine 3 (5‑HT₃) receptor. It was developed for the prevention and treatment of nausea and vomiting, particularly chemotherapy-induced emesis. The drug demonstrated potent antagonistic activity at the 5‑HT₃ receptor in preclinical studies and advanced to phase II/III clinical trials for indications including nausea and vomiting as well as anxiety disorders and psychotic disorders. However, development was discontinued before approval[3][5]. The originator company was Boehringer Ingelheim.

Other names

itasetron hydrochlorideItasetron < Rec INN>N-(endo-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-2,3-dihydro-1H-benzimidazole-1-carboxamide2-Oxo-N-(1alphaH,5alphaH-tropan-3alpha-yl)-1-benzimidazoline-1-carboxamide