GR38032F, a 5HT3 receptor antagonist, in the prophylaxis of acute cisplatin-induced nausea and vomiting.

A total of 28 patients receiving cancer chemotherapy with cisplatin-containing regimens (70-120 mg/m2) participated in an evaluation of the efficacy and safety of GR38032F for the prevention of acute nausea and vomiting. GR38032F, a 5HT3 receptor antagonist, was given 30 min prior to cisplatin as an 8-mg loading dose by i.v. infusion over 15 min, followed by continuous infusion at a rate of 1 mg/h for 24 h. Efficacy was assessed by measurement of the number of episodes of retching and vomiting occurring in the 24 h after cisplatin administration and by an assessment of nausea during the same period. In all, 26 patients were evaluable for efficacy: overall, complete control was achieved in 12 patients (46%), major control (1-2 emetic episodes), in 6 (23%); minor control (3-5 episodes), in 1 (4%); control could not be achieved (failure; greater than 5 episodes) in 7 patients (27%). GR3832F was the tolerated, with no significant drug-related adverse events. These encouraging results should be confirmed in comparative trials.