A randomized, controlled, multicenter clinical trial to evaluate the efficacy and safety of oral sitafloxacin versus moxifloxacin in adult patients with community-acquired pneumonia

Abstract

Objectives: To evaluate the efficacy and safety of oral sitafloxacin versus oral moxifloxacin in the treatment of Chinese adults with community-acquired pneumonia (CAP). Patients and methods: This is a multicenter, randomized, open-label, positive-controlled clinical trial (chinadrugtrials.org.cn identifier: CTR20130046). CAP patients received sitafloxacin tablets 100mg once daily (qd) or 100mg twice daily (bid) to compare with moxifloxacin tablets 400mg qd, for 7-10 days. The primary outcome was non-inferiority of sitafloxacin to moxifloxacin in clinical cure rate at test of cure (TOC) visit in per-protocol set (PPS). Results: A total of 343 patients were randomized (sitafloxacin 100mg qd, n=117, sitafloxacin 100mg bid, n=116, moxifloxacin, n=110), 291 patients were included in PPS (sitafloxacin 100mg qd, n=96, sitafloxacin 100mg bid, n=94, moxifloxacin, n=101). The clinical cure rate was 94.8% in sitafloxacin 100mg qd group, 96.8% in sitafloxacin 100mg bid group, and 95.0% in moxifloxacin group. At TOC visit, the microbiological success rate was 97.0% (32/33) in sitafloxacin 100mg qd group, 97.1% (34/35) in sitafloxacin 100mg bid group, and 94.9% (37/39) in moxifloxacin group in microbiological evaluable set (MES). The incidence of study drug-related adverse events (AEs) was 23.3% (27/116) in sitafloxacin 100mg qd group, 29.8% (34/114) in sitafloxacin 100mg bid group, and 28.2% (31/110) in moxifloxacin group (P> 0.05). The common AEs related to study drug were dizziness, nausea, diarrhea, increased A c c e p t e d M a n u s c r i p t platelet count, and ALT elevation. All the AEs resolved completely after discontinuation of study drug. Conclusion: Sitafloxacin 100mg qd or 100mg bid for 7-10 days is not inferior to moxifloxacin 400mg qd for 7-10 days in the clinical efficacy for adult CAP patients. Sitafloxacin provides safety profile comparable to moxifloxacin.

Effectiveness of sitafloxacin monotherapy for quinolone-resistant rectal and urogenital Mycoplasma genitalium infections: a prospective cohort study

“… 14 , 15 , 18 In terms of safety, sitafloxacin 200 mg daily is generally well tolerated, with the most common side effects being gastrointestinal problems and liver function disorders. 19 , 20 A randomized trial comparing sitafloxacin with moxifloxacin found that the two drugs had a similar incidence of adverse effects. 19 Additionally, sitafloxacin and moxifloxacin are less associated with tendon rupture, which is an adverse effect of the second-generation quinolones 21 ; however, data on the safety of sitafloxacin are limited owing to its low availability.…”

Sitafloxacin Expresses Potent Anti-Mycobacterium abscessus Activity

“…The antibacterial activity of quinolones (e.g., moxifloxacin and levofloxacin) commonly used to treat M. abscessus infections is unsatisfactory ( Choi et al, 2012a ). Sitafloxacin, a new fluoroquinolone that is effective against a broad range of bacteria, has the advantages of oral administration and superior safety ( Wu et al, 2014 ; Amano et al, 2016 ; Nakajima et al, 2016 ; Miyazaki et al, 2019 ; Mori et al, 2020 ; Li et al, 2021a , b ). Importantly, sitafloxacin exhibits antibacterial activity against M. tuberculosis and M. avium both in vitro and in vivo ( Tomioka et al, 1999 ; Sato et al, 2003 ; Asakura et al, 2019 ).…”

“…A phase I clinical trial investigating the pharmacokinetics and tolerance to sitafloxacin found that a serum concentration of 1 mg/L was safely attained and well tolerated by healthy male volunteers administered a single 100 mg dose orally ( Li et al, 2021b ). This serum concentration is similar to the MIC 50 of sitafloxacin for M. abscessus found in the current study, thus a safe and effective dose can be achieved for treating M. abscessus clinically.…”

Sitafloxacin- Versus Moxifloxacin-Based Sequential Treatment for Mycoplasma Genitalium Infections: Protocol for a Multicenter, Open-Label Randomized Controlled Trial

“…For those harboring parC G248T (S83I) and gyrA mutations, the effectiveness was further reduced to 18.8% [ 19 ]. Both sitafloxacin and moxifloxacin are newer-generation quinolones that exhibit a comparable incidence of gastrointestinal side effects [ 22 , 23 ]. These agents are less frequently associated with tendon rupture than levofloxacin, a prevalent fluoroquinolone drug [ 24 ].…”