Indisetron dihydrochloride (N-3389) was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004. It was co-developed and co-marketed as Sinseron by Kyorin & Yakult Honsha in Japan. Indisetron is a dual serotonin 5-HT3 and 5-HT4 receptor antagonist. It is indicated for the treatment of prophylaxis of chemotherapy-induced nausea and vomiting, it’s administered once daily. Indisetron is metabolized in the liver, and CYP1A1, CYP2C9, CYP2D6, and CYP3A4 are involved in its metabolism. However, indisetron is unlikely to cause drug interactions at clinical doses because the effective plasma concentrations are lower than those necessary for inhibiting the metabolic enzymes. No drug interaction has been reported. Indisetron antagonizes 5-HT4 receptors, as well as 5-HT3 receptors, and this characteristic is expected to contribute to its clinical efficacy.