&NA;Itasetron (DAU 6215, U 98079) is a potent and selective serotonin 5-HT3receptor antagonist currently in phase II/III clinical trials in Germany, the US and Japan with Boehringer Ingelheim as a potential oral antiemetic agent for use in cancer patients. Itasetron is also in early phase II clinical trials as an anxiolytic agent in Germany and is undergoing preclinical investigation in Italy for anxiety and as a potential cognition enhancing agent. It may also have potential as an antipsychotic agent. Pharmacia & Upjohn has licensed itasetron for joint development and marketing worldwide.Itasetron has a favourable pharmacokinetic profile compared with other currently available 5-HT3antagonist antiemetic agents.