A phase I antiemetic study of MDL 73,147EF, a novel 5-hydroxytryptamine antagonist in cancer patients receiving emetogenic chemotherapy.

BACKGROUND

We conducted a phase I study with MDL 73,147EF, a new 5 hydroxytryptamine 3 (5-HT3) receptor antagonist, in 25 patients requiring emetogenic chemotherapy.

PATIENTS AND METHODS

5 groups of 5 patients received rising unit doses of MDL 73,147EF (10 to 50 mg) intravenously before chemotherapy, with two additional doses per day if needed. Nausea was assessed by a patient-completed visual analogue scale and episodes of vomiting were recorded by an independent observer.

RESULTS

42% of the patients were complete or major responders on day one. Five patients were given other rescue antiemetic therapy. Adverse effects included headache (16%) diarrhea (8%) and other minor events. The best results were obtained with the 30, 40 and 50 mg doses.

CONCLUSIONS

MDL 73,147EF is a well-tolerated and probably effective antiemetic agent which requires further evaluation in randomised controlled clinical studies.