FUNDAMENTAL AND CLINICAL STUDIES OF AC-1370 IN URINARY TRACT INFECTION

• Published in: CHEMOTHERAPY Vol. 32; no. Supplement9; pp. 681 - 691
• Main Authors: ARAKAWA, SOICHI, FUJII, AKIRA, OGAWA, TAKAYOSHI, HARADA, MASUYOSHI, HAZAMA, MINORU, KATAOKA, NOBUMASA, 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.Supplement9_681

Preclinical and clinical studies of a new cephem antibiotic, AC-1370, were made; and the following were found: 1) In vitro antibacterial activity: the MICs of AC-1370 against 8 clinical isolates of gram-negative rods were measured in comparison with those of CPZ, LMOX, CTX, CTM and CEZ. The in vitro antibacterial activity of AC-1370 was superior to that of CEZ, and it was more potent against P. aeruginosa but less potent against the other isolates than that of CTM. Its in vitro antibacterial activity was generally inferior to those of CPZ, LMOX and CTX. 2) Pharmacokinetics: Three normal subjects were treated with 2g of AC-1370 by intravenous oneshot injection, respectively. The AC-1370 level in the blood reached 303.3μg/ml in 5 minutes, with a T1/2 of about 2 hours. Its excretion in the 0-2 hour urine amounted to 15, 400μg/ml, with 91.7% of the injected dose recovered from the urine in 8 hours. The level of AC-1370 in prostatic adenoma was 48.2 and 66.6 μg/g (30 minutes after intravenous one-shot injection of 1g), and its level in the effusion of hydrocele was 8.7 μg/g (90 minutes after intravenous one-shot injection of 1g). 3) Clinical findings: Thirty patients with complicated urinary tract infections were treated with AC-1370; and the treatment was evaluated as having exerted an “excellent” effect on 6, and “good” effect on 11 of the patients, with a response rate of 57%, and a (pathogen) eradication rate of 70%. Neither subjectivenor objective side effects were noted in any of the patients; however, laboratory studies revealed that GOT, GPT and ALP were transiently elevated in one of the patients.