What Is Old Is New Again: Delafloxacin, a Modern Fluoroquinolone

Abstract

Delafloxacin is a new fluoroquinolone antimicrobial approved for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) in adults using dosage regimens of 300 mg intravenously every 12 hours, 450 mg orally every 12 hours, or switching from intravenous to oral regimens for a 5-to 14-day treatment duration. Dosage adjustments in patients with severe renal dysfunction (estimated glomerular filtration rate [eGFR] = 15-29 ml/min/1.73 m 2 ) are not required for oral doses but should be decreased to 200 mg intravenously every 12 hours in patients requiring parenteral therapy. Due to insufficient data, use of delafloxacin is not recommended for patients on hemodialysis or with endstage renal disease (eGFR < 15 ml/min/1.73 m 2 ). Delafloxacin works through inhibition of DNA gyrase (topoisomerase II) and topoisomerase IV, which are essential enzymes for bacterial DNA transcription, replication, repair, and recombination and exhibits bactericidal activity against gram-positive and gram-negative organisms through a concentration-dependent matter. Delafloxacin has a very broad spectrum of activity against atypical, anaerobic, and resistant gram-negative and gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa. During phase 3 trials, the most common side effects associated with delafloxacin were gastrointestinal (nausea, diarrhea). Unlike other fluoroquinolones, there does not seem to be a risk of QTc prolongation or phototoxicity with delafloxacin. The availability of both parenteral and oral formulations for delafloxacin distinguishes it from many of the currently available agents approved for ABSSSIs. Phase 3 studies for the treatment of respiratory infections are currently under way, and future results of these studies will further help delineate the role of delafloxacin. KEY WORDS delafloxacin, fluoroquinolone, methicillin-resistant Staphylococcus aureus, skin infection.

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

“…The recommended oral dose of DFL is 450 mg, which is administered every 12 h daily. Frequent administration of conventional DFL formulation might be needed due to its low bioavailability and rapid metabolism with a mean half-life of ≤2.5 h after administration [13][14][15]. However, frequent administration of antibiotics is usually discouraging for patient compliance reasons, and it may lead to resistance, especially for CA-RTIs treatment [16].…”

Community-Acquired Bacterial Pneumonia—Changing Epidemiology, Resistance Patterns, and Newer Antibiotics: Spotlight on Delafloxacin

“…Overall, delafloxacin demonstrated non-inferiority with moxifloxacin, and was effective and well tolerated; in addition, it provides coverage for Gram-positive, Gram-negative, and atypical pathogens. Delafloxacin is available in both parenteral and oral formulations, which distinguishes it from other available agents [109]. Delafloxacin is only approved in the USA for CABP [4].…”

Simple and Accurate HPTLC-Densitometric Method for Quantification of Delafloxacin (A Novel Fluoroquinolone Antibiotic) in Plasma Samples: Application to Pharmacokinetic Study in Rats

“…Acute bacterial skin and skin structure infections (ABSSSIs) and community-acquired respiratory tract infections (CARTIs) are the most common infections which require hospitalization of patients for the treatment [1,2]. Delafloxacin (DLX), which is a new fluoroquinolone antibiotic, recently approved for the treatment of both ABSSSIs and CARTIs by USFDA and for ABSSSIs only by EMA [3][4][5]. It has been found active against major pathogens responsible for ABSSSIs and CARTIs [6,7].…”