Fabesetron (FK1052) is an orally active compound that acts as a dual antagonist of 5-HT3 and 5-HT4 receptors, demonstrating efficacy in managing emesis induced by cancer chemotherapy and showing potential for addressing both acute and delayed symptoms.

Fabesetron (FK1052) at a dose of 0.1 mg/kg when administered orally, effectively inhibits the increase in colonic transit in male Sprague-Dawley rats (220 to 330 g) and also completely prevents cisplatin (18 mg/kg, i.p.)-induced emesis in Suncus murinus (either sex, >10-week-old, 30-70 g). The study utilized male Sprague-Dawley rats and ddy mice for evaluating its effect on colonic transit, reporting a significant delay and inhibition degree of 33.8 ± 4.8% following a 0.1 mg/kg oral dose. In a dose-dependent manner, FK1052, administered orally 30 minutes before cisplatin, showed inhibited emesis in Suncus murinus, with no emesis observed at 100 μg/kg, indicating its potential for managing chemotherapy-induced side effects.