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Journal of Antimicrobial Chemotherapy 2005 55(Supplement 2):ii31-ii35; doi:10.1093/jac/dki006
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JAC © The British Society for Antimicrobial Chemotherapy 2005; all rights reserved

Supplement

Pharmacokinetics and excretion of dalbavancin in the rat

Marco Cavaleri1,*, Simona Riva1, Anna Valagussa1, Marco Guanci2, Luigi Colombo1, James Dowell3 and Martin Stogniew3

1 Vicuron Pharmaceuticals Italy, Via R. Lepetit 34-21040, Gerenzano, Varese, Italy; 2 IPAS SA via Mastri 36, 6853 Ligornetto, Switzerland; 3 Vicuron Pharmaceuticals, King of Prussia, PA, USA

* Corresponding author. Tel: +39-029-647-4242; Fax: +39-029-647-4238; Email: mcavaleri{at}vicuron.it

Objectives: The pharmacokinetics, tissue distribution and excretion routes of dalbavancin, a semi-synthetic glycopeptide, were investigated in rats.

Methods: A 20 mg/kg intravenous dose of dalbavancin or [3H]dalbavancin was administered to rats in three studies. Concentrations of dalbavancin or drug-derived radioactivity were assessed in blood, plasma, tissues, bile, urine and faeces by HPLC-MS/MS, scintillation counting or microbiological methods.

Results: Dalbavancin decayed tri-exponentially in plasma with an apparent terminal t1/2 of 187 h (approximately 8 days). Dalbavancin has dual routes of elimination, with around two-thirds of the excreted drug-derived radioactivity being found in the urine and around one-third in the faeces. After 70 days, 44.2% and 22.3% of the drug-derived radioactivity had been recovered in the urine and faeces, respectively. Biliary excretion of drug-derived radioactivity accounted for over half of the radioactivity excreted faecally. At 70 days post-dose, <5% of the dose remained in the carcass, showing that drug elimination was complete.

Conclusions: Dalbavancin has a long t1/2 (approximately 8 days) in the rat and distributes widely throughout the body. It is not selectively retained in any single organ, tissue or blood component and is completely eliminated by both renal and non-renal routes in rats. These data were useful in designing and interpreting animal infection model studies used to select the dose for human studies.

Keywords: glycopeptides , tissue distribution , mass balance


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