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Lerisetron is a selective 5-HT3 receptor antagonist developed by Orion Corporation for the prevention and treatment of nausea and vomiting, particularly those induced by radiotherapy or chemotherapy. As a member of the "setron" class of antiemetics, it works by blocking serotonin (5-hydroxytryptamine) from binding to 5-HT3 receptors located on the vagal nerve terminals in the gastrointestinal tract and in the chemoreceptor trigger zone of the central nervous system. The drug reached Phase III clinical development, where it was evaluated for efficacy in patients with stage I seminoma receiving radiotherapy, comparing its performance to granisetron. However, development appears to have been discontinued, and the drug is not currently marketed.
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