PHASE I CLINICAL STUDIES ON A NOVEL ORAL CEPHEM ANTIBIOTIC, ME 1207

• Published in: CHEMOTHERAPY Vol. 40; no. Supplement2; pp. 105 - 119
• Main Authors: Shimada, Kaoru, Matsumoto, Takashi, Komiya, Izumi, Shinkai, Sachihiko
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1992
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.40.Supplement2_105

ME 1207, a novel oral cephem antibiotic, is a prodrug of ME1206 which has a potent activity againsta broad spectrum of bacteria.Our preclinical animal studies showed that ME 1207 is a safe antibioticand also has a potent antibacterial effect in in vivo experimental infections. We performed a phase I clinical study in 28 healthy volunteers to determine the safety, tolerance and pharmacokineticprofile of ME 1207. The results obtained were as follows: 1. No alterations attributable to ME 1207 were observed regarding subjective or objective signs, physical examinations or clinical laboratory findings, except for one subject who developed a slightheadache once after a postprandial oral dose of 200mg of ME 1207, which disappeared within 45minutes. 2. Two hours after a postprandial single dose of 100, 200 or 300mg, the mean serum concentrationof ME 1206 reached a peak value at 1.48, 3.17 and 4.42μg/ml, respectively. The half-life rangedbetween 0.80-1.11h and the cumulative urinary excretion ratio was about 20%. 3. Absorpion of ME 1207 was affected by food intake, namely, the absorption underpostprandialconditions was rather higher than under fasting conditions. 4. No accumulation of ME1206 in serum was observed after multiple postprandial administrationof ME 1207 (200mg, t.i.d.) for 8 days.