呼吸器感染症に対するNM441の基礎的, 臨床的検討

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  • Basic and clinical studies on NM441 in respiratory tract infection

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Basic and clinical studies on NM441, a new prodrug type quinolone, were performed and the following results were obtained.<BR>1. In vitro antimicrobial activity<BR>The minimum inhibitory concentrations (MICs) of NM394, the active form of NM441 were measured for 101 strains of 5 clinically isolated species and compared to those of ofloxacin (OFLX), ciprofloxacin (CPFX), tosufloxacin (TFLX) and sparfloxacin (SPFX). The activity of NM394 against Streptococcus pneumoniae was equal to that of CPFX but less than that of OFLX, TFLX and SPFX. NM394 showed better activity against Klebsiella pneumoniae than OFLX and SPFX and the activity was equal to that of CPFX and TFLX. The activity of NM394 against Haemophilus spp. was equal to that of OFLX, TFLX and SPFX but less than that of CPFX. NM394 showed better anti-pseudomonal activity against Pseudomonas aeruginosa than OFLX and the activity was equal to that of SPFX but less than that of CPFX and TFLX. None of them showed meaningful activity against Staphylococcus aureus.<BR>2. The penetration into sputum and serum<BR>NM441 was orally administered to a chronic bronchitis patient at a dose of 300mg twice a day for 5 days. The serum and sputum levels of NM394 were determined on the first, 3rd and 5th day of the administrations. The maximum serum levels were obtained 4 h after each administration on the first, 3rd and 5th days and the values were 1.43, 3.45 and 2.86μg/ml, respectively. The maximum sputum levels were obtained 6 h after the first and 3rd day of the administrations, but on the 5th day the peak was obtained in the first sputum in the morning, which was 1 h prior to the administration. Those values were 2.64, 7.49 and 6.40μg/ml, respectively. The penetration rate to the sputum was 185-224% higher than that to the serum.<BR>3. Clinical efficacy<BR>NM441 was administered to a total of 12 patients with respiratory tract infections at 100-300mg twice a day for 5-14 days. The clinical efficacy was evaluated as excellent in 1 acute pneumonia, good in 7 cases (1 mycoplasma pneumonia, 3 chronic bronchitis and 3 secondary infections to bronchial asthma), fair in 1 chronic bronchitis and poor in 3 cases (3 bronchiectasis). The clinical efficacy rate was 66.7%. No side effects were observed but abnormal laboratory findings were observed in 1 case in GOT·GPT elevation and in 1 case in ALP·γ-GTP·LAP elevation.

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