Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic

Yoshiteru Shigeno, Miyako Masaki, Hiroko Nakazato, Hironobu Koga, Masao Nagasawa, Hiroshi Tomita, Koichi Watahabe, Yoshiaki Fukuda, Hikaru Tanaka, Akimitsu Tomonaga, Yoji Suzuyama, Kinichi Izumikawa, Atsushi Saito, Kohei Hara, Nobuchika Kusano, Mitsuo Kaku, Kazuyuki Sugawara, Chikako Mochida, Keizo Yamaguchi, Hlroyuki OkadaAkira Ikebe, Kazuhiro Okuno

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Laboratory and clinical studies on lenampicillin (KBT-1585), a newly developed ampicillin prodrug, were carried out with following results. 1) Antibacterial activity: The in vitro antibacterial activity of KBT-1585 was tested by the serial microbroth dilution method using MIC 2000 system (Dynatek Co.). The minimum inhibitory concentrations (MICs) of ABPC against total 433 strains consisting of 26 standard strains and 407 clinical isolates including Staphylococcus aureus 48, Staphylococcus epidermidis 42, Streptococcus pneumoniae 48, Streptococcus faecalis 44, Escherichia coli 52, Klebsiella aerogenes 49, Proteus mirabilis 47, Haemophilus influenzae 63 were compared with those of amoxicillin (AMPC), mecillinam (MPC) and piperacillin (PIPC). Antibacterial activities of ABPC against S. aureus, S. epidermidis and 5. faecalis were almost equal to those of AMPC, and more potent than those of PIPC and MPC. AMPC and PIPC were two times more active than ABPC against S. pneumoniae. On the other hand, antibacterial activities of ABPC and AMPC against Enterobacteriaceae such as K. aerogenes, E. coli and P. mirabilis were less potent than those of PIPC and MPC. PIPC was most active against H. influenzae and followed by ABPC and AMPC. 2) Serum and sputum levels in patients with chronic respiratory tract infection: Two patients with chronic respiratory tract infections were objected in this study. After a dose of 500 mg of KBT-1585 was given to them orally, their levels in sera and sputa were measured by bioassay method. As a result, peak serum levels were obtained at one hour after administration showing values of 6.39 to 10.64 μg/ml. On the other hand, concentrations of sputum reached its peak at 4 to 6 hours after administration in one case with purulent sputum and the value was 0.38 μg/ml. But in one case, the value was under the limit of measurement. 3) Clinical evaluation and adverse reaction: Forty patients with respiratory infections (pneumonia 16, chronic bronchitis 15, bronchiectasis 8, organizing pneumonia 1) were treated with 0.75 to 1.0 g of KBT-1585 daily for 3 to 21 days by oral administration. Twenty-nine of 39 patients responded satisfactorily to the treatment and the efficacy rate was 74.4% (excellent 9, good 20, fair 5, poor 5, unknown 1). Subjective and objective symptoms, hematological and biochemical data and renal functions were checked up before and after administration of KBT-1585. Abnormal laboratory findings were observed in 3 cases: elevation of S-GOT in 1, BUN in 1 and Al-Pase in 1.

Original languageEnglish
Pages (from-to)382-396
Number of pages15
JournalChemotherapy
Volume32
Issue numberSupplement
DOIs
Publication statusPublished - 1984
Externally publishedYes

Fingerprint

Piperacillin
Penicillins
Sputum
Respiratory Tract Infections
Enterobacter aerogenes
Proteus mirabilis
Staphylococcus epidermidis
Haemophilus influenzae
Microbial Sensitivity Tests
Streptococcus pneumoniae
Staphylococcus aureus
Pneumonia
Amdinocillin
Serum
Escherichia coli
Bronchiectasis
Enterococcus faecalis
Blood Urea Nitrogen
Chronic Bronchitis
Amoxicillin

ASJC Scopus subject areas

  • Oncology
  • Pharmacology
  • Drug Discovery
  • Pharmacology (medical)
  • Infectious Diseases

Cite this

Shigeno, Y., Masaki, M., Nakazato, H., Koga, H., Nagasawa, M., Tomita, H., ... Okuno, K. (1984). Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic. Chemotherapy, 32(Supplement), 382-396. https://doi.org/10.11250/chemotherapy1953.32.Supplement8_382

Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic. / Shigeno, Yoshiteru; Masaki, Miyako; Nakazato, Hiroko; Koga, Hironobu; Nagasawa, Masao; Tomita, Hiroshi; Watahabe, Koichi; Fukuda, Yoshiaki; Tanaka, Hikaru; Tomonaga, Akimitsu; Suzuyama, Yoji; Izumikawa, Kinichi; Saito, Atsushi; Hara, Kohei; Kusano, Nobuchika; Kaku, Mitsuo; Sugawara, Kazuyuki; Mochida, Chikako; Yamaguchi, Keizo; Okada, Hlroyuki; Ikebe, Akira; Okuno, Kazuhiro.

In: Chemotherapy, Vol. 32, No. Supplement, 1984, p. 382-396.

Research output: Contribution to journalArticle

Shigeno, Y, Masaki, M, Nakazato, H, Koga, H, Nagasawa, M, Tomita, H, Watahabe, K, Fukuda, Y, Tanaka, H, Tomonaga, A, Suzuyama, Y, Izumikawa, K, Saito, A, Hara, K, Kusano, N, Kaku, M, Sugawara, K, Mochida, C, Yamaguchi, K, Okada, H, Ikebe, A & Okuno, K 1984, 'Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic', Chemotherapy, vol. 32, no. Supplement, pp. 382-396. https://doi.org/10.11250/chemotherapy1953.32.Supplement8_382
Shigeno, Yoshiteru ; Masaki, Miyako ; Nakazato, Hiroko ; Koga, Hironobu ; Nagasawa, Masao ; Tomita, Hiroshi ; Watahabe, Koichi ; Fukuda, Yoshiaki ; Tanaka, Hikaru ; Tomonaga, Akimitsu ; Suzuyama, Yoji ; Izumikawa, Kinichi ; Saito, Atsushi ; Hara, Kohei ; Kusano, Nobuchika ; Kaku, Mitsuo ; Sugawara, Kazuyuki ; Mochida, Chikako ; Yamaguchi, Keizo ; Okada, Hlroyuki ; Ikebe, Akira ; Okuno, Kazuhiro. / Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic. In: Chemotherapy. 1984 ; Vol. 32, No. Supplement. pp. 382-396.
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T1 - Laboratory and clinical studies on lenampicillin (kbt-1585) A new penicillin antibiotic

AU - Shigeno, Yoshiteru

AU - Masaki, Miyako

AU - Nakazato, Hiroko

AU - Koga, Hironobu

AU - Nagasawa, Masao

AU - Tomita, Hiroshi

AU - Watahabe, Koichi

AU - Fukuda, Yoshiaki

AU - Tanaka, Hikaru

AU - Tomonaga, Akimitsu

AU - Suzuyama, Yoji

AU - Izumikawa, Kinichi

AU - Saito, Atsushi

AU - Hara, Kohei

AU - Kusano, Nobuchika

AU - Kaku, Mitsuo

AU - Sugawara, Kazuyuki

AU - Mochida, Chikako

AU - Yamaguchi, Keizo

AU - Okada, Hlroyuki

AU - Ikebe, Akira

AU - Okuno, Kazuhiro

PY - 1984

Y1 - 1984

N2 - Laboratory and clinical studies on lenampicillin (KBT-1585), a newly developed ampicillin prodrug, were carried out with following results. 1) Antibacterial activity: The in vitro antibacterial activity of KBT-1585 was tested by the serial microbroth dilution method using MIC 2000 system (Dynatek Co.). The minimum inhibitory concentrations (MICs) of ABPC against total 433 strains consisting of 26 standard strains and 407 clinical isolates including Staphylococcus aureus 48, Staphylococcus epidermidis 42, Streptococcus pneumoniae 48, Streptococcus faecalis 44, Escherichia coli 52, Klebsiella aerogenes 49, Proteus mirabilis 47, Haemophilus influenzae 63 were compared with those of amoxicillin (AMPC), mecillinam (MPC) and piperacillin (PIPC). Antibacterial activities of ABPC against S. aureus, S. epidermidis and 5. faecalis were almost equal to those of AMPC, and more potent than those of PIPC and MPC. AMPC and PIPC were two times more active than ABPC against S. pneumoniae. On the other hand, antibacterial activities of ABPC and AMPC against Enterobacteriaceae such as K. aerogenes, E. coli and P. mirabilis were less potent than those of PIPC and MPC. PIPC was most active against H. influenzae and followed by ABPC and AMPC. 2) Serum and sputum levels in patients with chronic respiratory tract infection: Two patients with chronic respiratory tract infections were objected in this study. After a dose of 500 mg of KBT-1585 was given to them orally, their levels in sera and sputa were measured by bioassay method. As a result, peak serum levels were obtained at one hour after administration showing values of 6.39 to 10.64 μg/ml. On the other hand, concentrations of sputum reached its peak at 4 to 6 hours after administration in one case with purulent sputum and the value was 0.38 μg/ml. But in one case, the value was under the limit of measurement. 3) Clinical evaluation and adverse reaction: Forty patients with respiratory infections (pneumonia 16, chronic bronchitis 15, bronchiectasis 8, organizing pneumonia 1) were treated with 0.75 to 1.0 g of KBT-1585 daily for 3 to 21 days by oral administration. Twenty-nine of 39 patients responded satisfactorily to the treatment and the efficacy rate was 74.4% (excellent 9, good 20, fair 5, poor 5, unknown 1). Subjective and objective symptoms, hematological and biochemical data and renal functions were checked up before and after administration of KBT-1585. Abnormal laboratory findings were observed in 3 cases: elevation of S-GOT in 1, BUN in 1 and Al-Pase in 1.

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