FUNDAMENTAL AND CLINICAL STUDIES OF AT-2266 IN THE UROLOGICAL FIELD

• Published in: CHEMOTHERAPY Vol. 32; no. Supplement3; pp. 776 - 795
• Main Authors: ARAKAWA, SOICHI, FUJII, AKIRA, KITANO, YOSHIHIKO, TADERA, SHIGENORI, HARADA, MASUYOSHI, KATAOKA, NOBUMASA, MITA, TOSHIHIKO, KAMIDONO, SADAO, ISHIGAMI, JOJI
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1984
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.32.Supplement3_776

We performed fundamental and clinical studies of AT-2266, a new synthetic pyridonecarboxylic acid antibacterial agent. The results obtained were as follows. 1) Antibacterial activity: The MIC distribution of AT-2266 against 9 species, each of 54 strains, of gramnegative clinical isolates was compared with that of NFLX, PPA and NA. AT-2266 was superior by a few tubes against all species to PPA and NA. AT-2266 was slightly inferior to NFLX against Proteus but equal to it against the other species. This drug had MICs of 100μg/ml or less against all strains. 2) Pharmacokinetics: The time courses of blood and urinary concentrations after administration of a single dose of 200mg were compared in normal subjects (Ccr>80ml/ min) and patients with chronic renal failure on hemodialysis (Ccr<10ml/ min). The blood half-life was 3.9 hours in the former and 10.6 hours in the latter. The peak urinary concentration was 325μg/ ml in the former and 12.3μg/ ml in the latter. 3) Clinical study: AT-2266 was effective in 95% of 131 patients with acute uncomplicated cystitis (according to the Criteria for Evaluation of the Drug Efficacy for UTI, the success rate was 100% in 70 patients.) and 72% of 50 patients with chronic urinary tract infections (according to the abovementioned Criteria, the success rate was 71% in 21 patients). The rate of bacterial elimination was 100% in the former and 88% in the latter. All 6 strains of P. aeruginosa were eradicated. The drug was effective in 79% of 14 patients with gonorrheal urethritis. The elimination rate of gonococci was 93%. Side effects obtained were transient but mild gastrointestinal disorders occurred in 2 out of 198 patients.