Basic and clinical studies on NM441
We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained. 1) Antibacterial activities The antibacterial activities of NM394 (active form of NM441) against 150 strains of 6 species were measured. MIC90...
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| Published in | Japanese Journal of Chemotherapy Vol. 44; no. Supplement1; pp. 289 - 294 |
|---|---|
| Main Authors | , , , , , , , , |
| Format | Journal Article |
| Language | Japanese |
| Published |
Japanese Society of Chemotherapy
1996
公益社団法人 日本化学療法学会 |
| Subjects | |
| Online Access | Get full text |
| ISSN | 1340-7007 1884-5886 |
| DOI | 10.11250/chemotherapy1995.44.Supplement1_289 |
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| Abstract | We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained. 1) Antibacterial activities The antibacterial activities of NM394 (active form of NM441) against 150 strains of 6 species were measured. MIC90s of NM394 against methicillin-susceptible Staphylococcus aureus (MSSA), methicillinresistant S. aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Pseudomonas aeruginosa were 3.13, 6.25, 0.1, 0.2, 0.39 and 3.13μg/ml, respectively. 2) Clinical results Subjects in the clinical study were a total of 10 patients including 5 cases with bacterial pneumonia, 1 with acute bronchitis, 1 with chronic bronchitis, 1 with acute pharyngolaryngitis, 1 with tonsillitis and 1 with acute cystitis. The clinical response was good in 8 cases and fair in 1 of the 9 patients able to be evaluated, and the efficacy rate was 88.9%. In the bacteriological efficacy, S.aureus and α-Streptococcus were isolated from 2 patients with bacterial pneumonia, K.pneumoniae from 1 with acute bronchitis, S.aureus from 1 with chronic bronchitis, Streptococcus pyogenes from 1 with tonsillitis and E. coli from 1 with cystitis, and all isolated organisms were eradicated except S.aureus in bacterial pneumonia and unknown in tonsillitis. Subjective and objective side effects were observed eruption in a patient with tonsillitis, and blister with glossitis in a patient with acute cystitis. From the above results, NM441 showed a wide antibacterial spectrum and good clinical response, and it was considered a useful drug for use in internal medical infections. |
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| AbstractList | We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained.1) Antibacterial activitiesThe antibacterial activities of NM394 (active form of NM441) against 150 strains of 6 species were measured. MIC90s of NM394 against methicillin-susceptible Staphylococcus aureus (MSSA), methicillinresistant S. aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Pseudomonas aeruginosa were 3.13, 6.25, 0.1, 0.2, 0.39 and 3.13μg/ml, respectively.2) Clinical resultsSubjects in the clinical study were a total of 10 patients including 5 cases with bacterial pneumonia, 1 with acute bronchitis, 1 with chronic bronchitis, 1 with acute pharyngolaryngitis, 1 with tonsillitis and 1 with acute cystitis. The clinical response was good in 8 cases and fair in 1 of the 9 patients able to be evaluated, and the efficacy rate was 88.9%. In the bacteriological efficacy, S.aureus and α-Streptococcus were isolated from 2 patients with bacterial pneumonia, K.pneumoniae from 1 with acute bronchitis, S.aureus from 1 with chronic bronchitis, Streptococcus pyogenes from 1 with tonsillitis and E. coli from 1 with cystitis, and all isolated organisms were eradicated except S.aureus in bacterial pneumonia and unknown in tonsillitis. Subjective and objective side effects were observed eruption in a patient with tonsillitis, and blister with glossitis in a patient with acute cystitis.From the above results, NM441 showed a wide antibacterial spectrum and good clinical response, and it was considered a useful drug for use in internal medical infections.
新しく開発されたキノロン系抗菌薬NM441の抗菌活性本体であるNM394の抗菌力および各種呼吸器感染症に対してNM441を経口投与した時の臨床効果を検討したところ, 以下のごとき成績を得た。1) 抗菌力臨床分離の6菌種, 150株に対するNM394のMIC90値はmethicillin-susceptible Staphylococcus aurezcs (MSSA) 3.13μg/ml, methicillin-resistant S.aureus (MRSA) 6.25μg/ml, Escherichia coli 0.1μg/ml, Klebsiella pneumoniae 0.2μg/ml, Proteus mirabilis 0.39μg/ml, Pseudomonas aemginosa 3.13μg/mlであった。2) 臨床成績細菌性肺炎5例, 急性気管支炎1例, 慢性気管支炎1例, 急性咽喉頭炎1例, 急性扁桃腺炎1例, 急性膀胱炎1例計10例の臨床効果は, 判定可能であった9例のうち8例で「有効」の結果を得, 1例が「やや有効」であった。細菌性肺炎2例よりS.aurezcs (MRSA), α-Streptococcus, 急性気管支炎1例よりK.pneumonine, 慢性気管支炎1例よりS.aureus (MSSA), 急性扁桃腺炎l例よりStreptococczts pyogenes, 急性膀胱炎1例よりE.coliが分離された。細菌性肺炎例のS.aureusは存続し, 急性扁桃腺炎では使用後細菌培養未実施により「判定不能」であったが, それら以外の症例の分離菌はいずれも除菌された。自他覚的副作用としては, 発疹 (1例), 舌炎・水庖 (1例) がみられた。臨床検査値の異常変動は細菌性肺炎の1例で好酸球の増多が認められた。以上の成績から, 本剤は幅広い抗菌スペクトルと良好な臨床成績を示し, 内科領域感染症に対して有用な薬剤の一つと考えられた。 We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained. 1) Antibacterial activities The antibacterial activities of NM394 (active form of NM441) against 150 strains of 6 species were measured. MIC90s of NM394 against methicillin-susceptible Staphylococcus aureus (MSSA), methicillinresistant S. aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Pseudomonas aeruginosa were 3.13, 6.25, 0.1, 0.2, 0.39 and 3.13μg/ml, respectively. 2) Clinical results Subjects in the clinical study were a total of 10 patients including 5 cases with bacterial pneumonia, 1 with acute bronchitis, 1 with chronic bronchitis, 1 with acute pharyngolaryngitis, 1 with tonsillitis and 1 with acute cystitis. The clinical response was good in 8 cases and fair in 1 of the 9 patients able to be evaluated, and the efficacy rate was 88.9%. In the bacteriological efficacy, S.aureus and α-Streptococcus were isolated from 2 patients with bacterial pneumonia, K.pneumoniae from 1 with acute bronchitis, S.aureus from 1 with chronic bronchitis, Streptococcus pyogenes from 1 with tonsillitis and E. coli from 1 with cystitis, and all isolated organisms were eradicated except S.aureus in bacterial pneumonia and unknown in tonsillitis. Subjective and objective side effects were observed eruption in a patient with tonsillitis, and blister with glossitis in a patient with acute cystitis. From the above results, NM441 showed a wide antibacterial spectrum and good clinical response, and it was considered a useful drug for use in internal medical infections. |
| Author | Sato, Yasunobu Shimada, Jingoro Sakurai, Iwao Imai, Takeo Morita, Masayuki Matsumoto, Fumio Ishida, Yuichiro Nakamura, Toru Takahashi, Takayuki |
| Author_FL | 中村 徹 松本 文夫 今井 健郎 佐藤 康信 石田 裕一郎 高橋 孝行 森田 雅之 嶋田 甚五郎 桜井 磐 |
| Author_FL_xml | – sequence: 1 fullname: 松本 文夫 – sequence: 2 fullname: 桜井 磐 – sequence: 3 fullname: 今井 健郎 – sequence: 4 fullname: 石田 裕一郎 – sequence: 5 fullname: 高橋 孝行 – sequence: 6 fullname: 森田 雅之 – sequence: 7 fullname: 佐藤 康信 – sequence: 8 fullname: 嶋田 甚五郎 – sequence: 9 fullname: 中村 徹 |
| Author_xml | – sequence: 1 fullname: Sato, Yasunobu organization: Pharmacy, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Ishida, Yuichiro organization: Department of Internal Medicine, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Takahashi, Takayuki organization: Clinical Laboratory, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Matsumoto, Fumio organization: Department of Internal Medicine, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Shimada, Jingoro organization: Insutitute of Medical Sceience, St. Marianna University School of Medicine – sequence: 1 fullname: Sakurai, Iwao organization: Department of Internal Medicine, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Nakamura, Toru organization: Department of Internal Medicine, Yokohama General Hospital – sequence: 1 fullname: Morita, Masayuki organization: Pharmacy, Kanagawa Prefecture Midwives and Nurses Training School Hospital – sequence: 1 fullname: Imai, Takeo organization: Department of Internal Medicine, Kanagawa Prefecture Midwives and Nurses Training School Hospital |
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| References | 1) Segawa J, Kitano M, Kazuno K, Matsuoka M, Shirahase I, Ozaki M, Matsuda M, Tomii Y, Kise M: Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1, 3] thiazeto [3, 2-a] quinoline-3-carboxylic acids. J Med Chem 35: 4727-4738, 1992 3) 名出頼男, 副島林造: 第42回日本化学療法学会西日本支部総会, 新薬シンポジウム. NM441, 名古屋, 1994 2) Yoshida T, Mitsuhashi S: Antibacterial activity of NM394 the active form of prodrug NM441, a new quinolone. Antimicrob Agents Chemother 37: 793-800, 1993 4) 日本化学療法学会: 最小発育阻止濃度 (MIC) 測定法再改訂について. Chemotherapy 29: 76-79, 1981 |
| References_xml | – reference: 3) 名出頼男, 副島林造: 第42回日本化学療法学会西日本支部総会, 新薬シンポジウム. NM441, 名古屋, 1994 – reference: 1) Segawa J, Kitano M, Kazuno K, Matsuoka M, Shirahase I, Ozaki M, Matsuda M, Tomii Y, Kise M: Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1, 3] thiazeto [3, 2-a] quinoline-3-carboxylic acids. J Med Chem 35: 4727-4738, 1992 – reference: 4) 日本化学療法学会: 最小発育阻止濃度 (MIC) 測定法再改訂について. Chemotherapy 29: 76-79, 1981 – reference: 2) Yoshida T, Mitsuhashi S: Antibacterial activity of NM394 the active form of prodrug NM441, a new quinolone. Antimicrob Agents Chemother 37: 793-800, 1993 |
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