Vol.68 No.S-1 November 2020
An overview of oral lascufloxacin, a novel quinolone antibiotic
1)Department of Microbiology and Infectious Diseases, Toho University School of Medicine, 5-21-16 Omori-Nishi, Ota-ku, Tokyo, Japan
2)Discovery Research Management, Kyorin Pharmaceutical Co., Ltd.
3)Department of Internal Medicine, Kita-tama Hospital
4)Nagasaki University
Abstract
Lascufloxacin hydrochloride(lascufloxacin: LSFX) is a novel quinolone antibacterial agent that was discovered by Kyorin Pharmaceutical Co., Ltd., and is used as a new treatment agent for respiratory and otorhinolaryngological infections.
LSFX exhibited potent antibacterial activity against major causative organisms of respiratory tract infections, and showed better activity than conventional quinolones against oral streptococci and anaerobes which have recently been identified as the causative bacteria of community-acquired pneumonia(CAP). In a phase I clinical study conducted in healthy adult subjects, LSFX showed a favorable pharmacokinetic profile, with rapid and good gastrointestinal absorption, a half-life suitable for once-daily administration, and a much higher pulmonary distribution than the conventional quinolones. Based on the antimicrobial activities, pharmacokinetic profile, and results of the dose-finding study, the dosage and administration of LSFX was set at 75 mg orally once daily.
The clinical efficacy rate of LSFX 75 mg once daily was 92.1% for CAP, 86.8% for secondary infection in chronic respiratory diseases, 92.3% for acute bronchitis, 84.8% for sinusitis, 92.9% for otitis media, 89.3% for tonsillitis, and 91.7% for pharyngolaryngitis. Non-inferiority of LSFX 75 mg to levofloxacin 500 mg was demonstrated in all controlled studies of CAP and sinusitis. From the results of pharmacokinetics/pharmacodynamics analyses based on the results of these studies, the estimated target value of the AUC0-24/MIC to predict clinical efficacy was fAUC0-24/MIC >3.9, which is lower than that of the existing quinolones. In addition, no LSFX-specific adverse reactions were observed in the clinical studies, and the incidences of gastrointestinal and central nervous system disorders, which are the main adverse reactions of quinolones, tended to be lower than those observed for the control drug.
LSFX is considered as a novel-style antimicrobial drug use, as it allows satisfactory therapeutic effects to be obtained at a reasonably low dose as a result of its high distribution at the target sites of infections.
Key word
lascufloxacin, respiratory tract infection, otolaryngological infection
Received
October 30, 2019
Accepted
July 22, 2020
Jpn. J. Chemother. 68 (S-1): 1-15, 2020
