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 inJapanese Journal of Chemotherapy Vol. 44; no. Supplement1; pp. 289 - 294
Main Authors Sato, Yasunobu, Ishida, Yuichiro, Takahashi, Takayuki, Matsumoto, Fumio, Shimada, Jingoro, Sakurai, Iwao, Nakamura, Toru, Morita, Masayuki, Imai, Takeo
Format Journal Article
LanguageJapanese
Published Japanese Society of Chemotherapy 1996
公益社団法人 日本化学療法学会
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ISSN1340-7007
1884-5886
DOI10.11250/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.
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
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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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Snippet We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained....
We investigated the antibacterial activities and clinical efficacy of NM441, a newly-developed quinolone antibiotic, and the following results were obtained.1)...
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抗菌力
臨床効果
Title Basic and clinical studies on NM441
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