Vol.68 No.S-1 November 2020
Open-label study of lascufloxacin in patients with otorhinolaryngological infections -Efficacy, Safety and Tissue Penetration-
1)Department of Otorhinolaryngology, Shimane University Faculty of Medicine, 89-1 Enyacho, Izumo, Shimane, Japan
2)Department of Otolaryngology, Head and Neck Surgery, Kagoshima University Graduate School of Medical and Dental Sciences
3)Department of Infecion Control, Jikei University Hospital
4)Department of Microbiology and Infectious Disease, Toho University School of Medicine
5)Department of Internal Medicine, Kita-tama Hospital
6)Clinical Development Center, Kyorin Pharmaceutical
7)Department of Otolaryngology, Yonaha General Hospital
Abstract
An open-label, non-comparative study of lascufloxacin (LSFX) was conducted in patients with otorhinolaryngological infections, and its efficacy and safety were investigated. The target diseases in this study were otitis media, tonsillitis, and laryngopharyngitis; LSFX 75 mg was administered orally once daily for 7 to 14 days. In addition, we examined the drug penetration ratios of LSFX into the otorhinolaryngologic tissues.
The overall clinical efficacy rate at the end of treatment (EOT) as the primary endpoint was 90.9% (60/66). The efficacy rates by the target disease were 92.9% (13/14) in the patients with otitis media, 89.3% (25/28) in the patients with tonsillitis, and 91.7% (22/24) in the patients with laryngopharyngitis. In regard to the secondary endpoints, the clinical efficacy rates on Day 3 and on Day 7 after EOT were 14.3% (2/14) and 100.0% (13/13) in the patients with otitis media, 25.0% (7/28) and 84.6% (22/26) in the patients with tonsillitis, 20.8% (5/24) and 95.5% (21/22) in the patients with laryngopharyngitis, respectively. The microbiological effects (eradication rates) were 98.1% (53/54) overall, 100.0% (7/7) in the patients with otitis media, 96.2% (25/26) in the patients with tonsillitis, and 100.0% (21/21) in the patients with laryngopharyngitis. LSFX yielded high eradication rates for all the causative microorganism isolated, regardless of the bacterial species. The incidence of adverse events (AEs) was 24.3% (17/70). The incidence of AEs for which a causal relationship could not be ruled out was 8.6% (6/70). Single administration of LSFX 75 mg was confirmed to have favorable tissue penetration, since the tissue-plasma concentration ratios exceeded 2 in all of the tissues, including the sinus mucosa, middle ear mucosa and palatine tonsil.
From the above results, including the highly favorable clinical and microbiological effects, good safety results without major problems, and good tissue permeability, it is considered that LSFX is a useful agent for the treatment of otorhinolaryngologic infections.
Key word
lascufloxacin, otolaryngological infection, clinical trial
Received
October 30, 2019
Accepted
June 22, 2020
Jpn. J. Chemother. 68 (S-1): 81-95, 2020
