Vol.68 No.S-1 November 2020

Open-label study of lascufloxacin for secondary infections in patients with chronic pulmonary diseases and patients with acute bronchitis

Makoto Miki¹⁾, Keiichi Mikasa²⁾, Junichi Kadota³⁾, Hiroshi Mukae⁴⁾, Jiro Fujita⁵⁾, Seiji Hori⁶⁾, Katsunori Yanagihara⁷⁾, Kazuhiro Tateda⁸⁾, Kyoichi Totsuka⁹⁾, Tomohiko Eiraku¹⁰⁾ and Shigeru Kohno¹¹⁾

¹⁾Department of Respiratory Medicine, Japanese Red Cross Sendai Hospital, 2-43-3 Yagiyamahoncho,Taihaku-ku, Sendai, Miyagi, Japan
²⁾Nara Koseikai Hospital
(Past: Center for Infectious Diseases, Nara Medical University)
³⁾Oita University Hospital
⁴⁾Department of Respiratory Medicine, Unit of Basic Medical Sciences, Nagasaki University Graduate School of Biomedical Sciences
⁵⁾Department of Infectious, Respiratory, and Digestive Medicine, Graduate School of Medicine, University of the Ryukyus
⁶⁾Department of Infecion Control, Jikei University Hospital
⁷⁾Department of Laboratory Medicine, Nagasaki University Graduate School of Biomedical Sciences
⁸⁾Department of Microbiology and Infectious Disease, Toho University School of Medicine
⁹⁾Department of Internal Medicine, Kita-tama Hospital
¹⁰⁾Clinical Development Center, Kyorin Pharmaceutical
¹¹⁾Nagasaki University

Abstract

To investigate the efficacy and safety of lascufloxacin (LSFX) for secondary infections in patients with chronic pulmonary diseases and for acute bronchitis, we conducted this multicenter, open-label, non-comparative study. Oral LSFX 75 mg was prescribed once daily for 7 days.
Clinical efficacy: For secondary infections in patients with chronic pulmonary diseases, the cure rate at test-of-cure (TOC) as the primary endpoint was 86.8% (33/38). In regard to the secondary endpoints, the clinical efficacy rates on Day 3 and at end-of-treatment (EOT) were 86.8% (33/38) and 92.1% (35/38), respectively. For acute bronchitis, the cure rate at TOC as the primary endpoint was 92.3% (12/13) and the clinical efficacy rates on Day 3 and at EOT as the secondary endpoints were 69.2% (9/13) and 92.3% (12/13), respectively.
Microbiological effect: Microbiological effect by subject (bacterial eradication rate) was achieved in 84.0% (21/25) of patients of chronic pulmonary diseases with secondary infections and in 6 out of 8 patients with acute bronchitis.
Drug concentrations in the sputum: The LSFX concentrations in sputum reached 0.167-2.01 μg/g (n=36) at 1.00-2.67 hours after the intake of the antibiotic, and the sputum-to-plasma penetration ratio was 0.613±0.289. It was confirmed that the concentrations in the sputum exceeded the MIC₉₀ for the principal isolates of the causative microorganisms in this study.
Safety: The incidences of adverse events (AEs) and adverse drug reactions were 30.2% (16/53) and 9.4% (5/53), respectively. There were no cases of death or serious AEs.
From these results, we concluded that LSFX is effective for respiratory infections, such as secondary infections in patients with chronic pulmonary diseases and acute bronchitis; no major safety problems associated with the use of the drug were identified either.

Key word

lascufloxacin, respiratory tract infection, secondary infection, chronic respiratory disease, acute bronchitis

Received

October 30, 2019

Accepted

January 24, 2020

Jpn. J. Chemother. 68 (S-1): 55-67, 2020