BASIC AND CLINICAL STUDIES ON KW-1062 AT DAILY DOSE OF 240 AND 360mg IN THE FIELD OF UROLOGY

Abstract

Clinical trials with KW-1062, a new aminoglycoside antibiotic, were carried out on the basis of the pre-clinical studies.
Absorption and excretion of KW-1062 were studied in the healthy adults after single and multiple intramuscular administration. The blood concentration at single administration of 120 and 180mg of KW-1062 reached the peak of 7 and 12μ/ml respectively 30 minutes after administration.The half life was constantly about 2 hours. The 10-hour urinary recovery rate was 55.6% and 60.8% at each of the above doses.No accumulation of KW-1062 in plasma was observed with multiple administration of 180 mg twice a day for 5 days.No adverse reactions (on blood, renal function and hearing) were observed.From these results, the dose of 360mg/day proved to be as safe as that of 240mg/day.
KW-1062 was administered to 155 patients at daily dose of 240mg and 360mg for 1-11 days. The cases collected and analyzed consisted of 105 patients with complicated U.T.I., 10 with acute and uncomplicated pyelonephritis, 16 with infection of neurogenic bladder after spinal cord injury and others.Of 105 patients with complicated U.T.I., 65 were administered KW-1062 at 360 mg daily, and 40 at 240mg.KW-1062 was found to be effective in 52.5% of the 240mg/day group, in 40% of the 360mg/day group of complicated U.T.I., when evaluated on the basis of the criteria by the U.T.I.study group, and in 90% of patients with acute and uncomplicated pyelonephritis.
Of 155 patients subjected to KW-1062 treatment, only one experienced tinnitus and nausea, and 17 had abnormal values in their laboratory findings.