title: Human pharmacokinetics and safety profile of finafloxacin, a new fluoroquinolone antibiotic, in healthy volunteers.
abstract: Finafloxacin is a new fluoroquinolone antibiotic with the unique property of increasing antibacterial activity at pH values lower than neutral. Whereas its antibacterial activity at neutral pH matches that of other quinolones in clinical use, it is expected to surpass this activity in tissues and body fluids acidified by the infection or inflammation processes. Pharmacokinetic parameters of oral single and multiple doses of up to 800 mg of finafloxacin and safety/tolerability observations were assessed in a phase I study including 95 healthy volunteers. Finafloxacin is well absorbed after oral administration, generating maximum concentrations (C(max)s) in plasma at least comparable to those of other fluoroquinolones, with a half-life of around 10 h. About one-third of the dose is excreted unchanged in the urine. Renal elimination appears to be a saturable process leading to slight increases of the area under the concentration-time curve extrapolated to infinity and dose normalized (AUC(∞,norm)) at dosages of 400 mg and above. Safety and tolerability data characterize finafloxacin as a drug with a favorable safety profile. In particular, adverse reactions regarded as class-typical of fluoroquinolones, such as, e.g., electrocardiogram (ECG) changes, neurotoxic effects, or hypoglycemia, were not observed in the study population.
authors.affiliation: MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany.
authors.forename: Heena
authors.initials: H
authors.lastname: Patel
authors.forename: Arne
authors.initials: A
authors.lastname: Andresen
authors.forename: Andreas
authors.initials: A
authors.lastname: Vente
authors.forename: Hans-Dietrich
authors.initials: HD
authors.lastname: Heilmann
authors.forename: Will
authors.initials: W
authors.lastname: Stubbings
authors.forename: Michael
authors.initials: M
authors.lastname: Seiberling
authors.forename: Luis
authors.initials: L
authors.lastname: Lopez-Lazaro
authors.forename: Rolf
authors.initials: R
authors.lastname: Pokorny
authors.forename: Harald
authors.initials: H
authors.lastname: Labischinski
mesh_terms: D000284:Administration, Oral; D000328:Adult; D004311:Double-Blind Method; D005260:Female; D024841:Fluoroquinolones / Q000009:adverse effects* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D006801:Humans; D008297:Male; D008875:Middle Aged
chemical_list: D024841:Fluoroquinolones; C560572:finafloxacin