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Randomized Controlled Trial
. 2011 Jun;55(6):2636-40.
doi: 10.1128/AAC.01744-10. Epub 2011 Mar 28.

Pharmacokinetics and safety of MP-376 (levofloxacin inhalation solution) in cystic fibrosis subjects

David E Geller  1 , Patrick A Flume, David C Griffith, Elizabeth Morgan, Dan White, Jeffery S Loutit, Michael N Dudley
Affiliations
Randomized Controlled Trial

Pharmacokinetics and safety of MP-376 (levofloxacin inhalation solution) in cystic fibrosis subjects

David E Geller et al. Antimicrob Agents Chemother. 2011 Jun.

Abstract

The pharmacokinetics and tolerability of nebulized MP-376 (levofloxacin inhalation solution [Aeroquin]) were determined in cystic fibrosis (CF) subjects. Ten CF subjects received single 180-mg doses of two formulations of MP-376, followed by a multiple-dose phase of 240 mg once daily for 7 days. Serum and expectorated-sputum samples were assayed for levofloxacin content. Safety was evaluated following the single- and multiple-dose study phases. Nebulized MP-376 produced high concentrations of levofloxacin in sputum. The mean maximum plasma concentration (C(max)) ranged between 2,563 and 2,932 mg/liter for 180-mg doses of the 50- and 100-mg/ml formulations, respectively. After 7 days of dosing, the mean C(max) for the 240-mg dose was 4,691 mg/liter. The mean serum levofloxacin C(max) ranged between 0.95 and 1.28 for the 180-mg doses and was 1.71 for the 240-mg dose. MP-376 was well tolerated. Nebulized MP-376 produces high sputum and low serum levofloxacin concentrations. The pharmacokinetics, safety, and tolerability were similar for the two formulations. MP-376 240 mg (100 mg/ml) is being advanced into late-stage clinical development.

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Figures

Fig. 1.
Fig. 1.
Serum levofloxacin levels after aerosol dosing of 180 or 240 mg MP-376.
Fig. 2.
Fig. 2.
Levofloxacin serum and sputum AUCs after aerosol dosing of MP-376, and comparative data for a 750-mg oral levofloxacin dose (750 PO [per os]) in CF subjects (3).
See this image and copyright information in PMC

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