The effect of TZP-4238, an antiandrogen drug, on renal function was examined. Single administration test: Patients with prostatic hypertrophy were divided according to creatinine clearance (CCr) into group A (CCr < 50 ml/min) and group B (CCr > or = 50 ml/min), and hemodynamics after a single administration of TZP-4238 were compared between the two groups. Groups A and B showed similar TZP-4238 hemodynamics, and there was no significant difference in pharmacokinetic parameters or the rate of serum protein binding between them. There was no difference in the hemodynamics of a major metabolite, 15-OH body, between the two groups. Neither was there any significant difference in the urinary excretion rate of TZP-4238 or 15-OH body. There were no findings of adverse clinical significance, and there were no problems with safety. Consecutive administration test: A 16-week consecutive administration study was performed on patients with prostatic hypertrophy associated with relative renal hypofunction. The blood levels determined in 5 patients were in good accordance with the simulation curve drawn from the results of group A. The rates of efficacy, safety and usefulness were 71.4%, 90% and 71.4%, respectively. Mild side effects were observed in one patient, but the 16-week administration was completed in all patients, and no adverse effects on renal function were observed. Favorable blood levels of TZP-4238 were obtained even in patients with prostatic hypertrophy associated with renal hypofunction, and adequate efficacy and safety were achieved even with consecutive administration. Furthermore, the drug had no apparent adverse effect on renal function.
Nakatani T; Yasumoto R; Wada S; Maekawa T; Nishisaka N; Yamamoto K; Kishimoto T
Department of Urology, Osaka City University Medical School.
Hinyokika Kiyo, 40: 8, 1994 Aug, 735-43