Nemonoxacin is a novel C-8-methoxy nonfluorinated
quinolone with remarkably enhanced in vitro activity against a wide variety of clinically relevant pathogens, especially gram-positive bacteria, including multidrug-resistant Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus. It has a low propensity for selecting resistant pathogens than
fluoroquinolones, since bacteria become resistant to
nemonoxacin only when three different mutations occur in their
quinolone resistance-determining regions.
Nemonoxacin shows greater efficacy than most of the widely used
fluoroquinolones in the murine model of systemic, pulmonary, or ascending
urinary tract infection.
Nemonoxacin has a sound PK profile in healthy volunteers. It rapidly reaches maximum concentration Cmax 1-2 hours after
oral administration in the fasting state and has a relatively long elimination half-life of more than 10 hours, which is similar to
fluoroquinolones. Approximately 60%-75% of the administered dose is excreted in unchanged form via kidneys over 24-72 hours. Phase II and III studies of oral
nemonoxacin and Phase II studies of intravenous
nemonoxacin have been completed in patients with community-acquired
pneumonia (CAP), before which the Phase I studies of oral and intravenous
nemonoxacin indicated sound tolerance and safety with healthy volunteers. The published results demonstrate that an oral dose of either 500 mg or 750 mg
nemonoxacin once daily for 7 days is as effective and safe as
levofloxacin 500 mg once daily for 7 days.
Nemonoxacin is well-tolerated in patients with CAP. The most common adverse events of
oral administration are observed in the gastrointestinal and nervous system, the incidence of which is similar to
levofloxacin treatment. The Phase III studies of intravenous
nemonoxacin for treating CAP and oral
nemonoxacin for
diabetic foot infection has been registered with promising outcomes to be expected.