A multicenter clinical trial of 274 patients compared the efficacy and safety of a new vaginal antifungal compound, butoconazole nitrate cream 2% (butoconazole), to clotrimazole vaginal tablets 200 mg/day (clotrimazole). Both drugs were administered for three days. The patients were randomly assigned to one or the other treatment regimen. Eight days after treatment completion, Candida albicans was absent in vaginal cultures of 95% of patients receiving butoconazole and of 91% of patients receiving clotrimazole; 30 days after treatment completion, 80% of patients receiving butoconazole were free of the fungal infection; the corresponding number for clotrimazole was 74%. Complete absence of the entrance signs and symptoms of vulvovaginal candidiasis was noted in 82% of patients receiving butoconazole and 72% of patients receiving clotrimazole. The phamacokinetic parameters were studied in three women volunteers who received one dose of radiolabeled butoconazole nitrate vaginal cream 2%. Measurable levels of radioactivity were not detected until two to eight hours after vaginal administration of the compound. Maximum plasma levels of radioactivity were achieved 24 hours after dosing and ranged from 19 to 44 ng/mL and fell to background levels after 96 to 120 hours. Total radioactivity was excreted to an equal extent in urine (2.7%) and in feces (2.8%).