Critical Care Research and Practice

Review Article

Meeting the Unmet Need in the Management of MDR Gram-Positive Infections with Oral Bactericidal Agent Levonadifloxacin

Table 2

Features of levonadifloxacin.
Antibiotic classBenzoquinolizine fluoroquinolone
Administration routeIntravenous and oral
Intravenous dose regimen800 mg BID
Oral dose regimen1000 mg BID
IndicationsABSSSI with concurrent bacteremia and DFI
Activity spectrumMRSA, QRSA, VRSA, VISA, Quinolone-S Gram-negatives, RTI pathogens
MRSA coverage>99 percent
Gram-negative coveragePartial
Intracellular activityYes (including MRSA + QRSA)
Biofilm eradicationStrong action for MRSA/QRSA biofilms
Activity in acidic conditionsEnhanced
T max2.68 ± 1.27 h for oral 1000 mg
C max21.48 ± 8.82 μg/mL for oral 1000 mg
Plasma AUCHighest plasma exposures among quinolones
Intravenous 800 mg: 377.8 ± 35.33 mg·h/L
Oral 1000 mg: 318.4 ± 33.2
Epithelial lining fluid AUCHighest lung penetration among quinolones 1000 mg oral OD: 345.2 μg·h/mL
Mean elimination half-life of 800 mg BID infused over 90 minutes6.8 hours
Metabolism72% of intravenous levonadifloxacin excreted as levonadifloxacin sulfate metabolite (approximately 50.3% in urine and 21.6% in faeces)
Dose adjustment in renal impaired patientsNot required
Dose adjustment in hepatic impairmentNot required
Liver safetyVery good
Cardiovascular system safetyExcellent
Gastrointestinal tolerabilityExcellent
<5% of dose is excreted as unchanged levonadifloxacin suggesting minimal role of renal system in elimination of levonadifloxacin. ABSSSI: acute bacterial skin and skin structure infections; AUC: area under curve; BID: bis in die/twice a day; CAP: community-acquired pneumonia; cIAI: complicated intra-abdominal infections; Cmax: maximum mean plasma concentration; DFI: diabetic foot infections; MDR: multidrug-resistant; MRSA: methicillin-resistant Staphylococcus aureus; MSSA: methicillin-susceptible Staphylococcus aureus; QRSA: quinolone-resistant Staphylococcus aureus; RTI: respiratory tract infections; Tmax: time to reach maximum concentration; VISA: vancomycin-intermediate Staphylococcus aureus; VRSA: vancomycin-resistant Staphylococcus aureus.