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Pharmacokinetics and unexpected safety issues of LBM415, a novel oral peptide deformylase inhibitor.

Rolan, Paul and MacLeod, Catherine and Bracken, Kathryn and Sun, Haiying and Evans, Thomas George (2011) Pharmacokinetics and unexpected safety issues of LBM415, a novel oral peptide deformylase inhibitor. Clinical Pharmacology and Therapeutics, 90 (2). pp. 256-262. ISSN 0009-9236

Abstract

Peptide deformylase (PDF) inhibitors represent a potential new class of antibiotics targeting a large number of bacterial species. We studied the pharmacokinetics and safety of LBM415, a novel PDF inhibitor, administered as a single oral dose at 100-3000 mg in the fasted state and at 1000 mg in the fed state in healthy volunteers. LBM415 was then administered from 100 mg qd to 1000 mg t.i.d for 11 days. Dose proportional pharmacokinetics was observed with a Cmax at 1000 mg b.i.d (the projected therapeutic dose) of 17.85±5.96 µg/mL and the AUC0-24h was 36.83±10.36 µg/ml*hr. The half-life determined after a 1000 mg single dose was 2.18±0.61 hours. The compound was well tolerated at low doses, but at the highest dose of 1000 mg t.i.d, reversible cyanosis and low oxygen saturation, attributable to methemoglobinemia, was detected on Day 10. Oxygen saturation was as low as 88% in one subject on Day 11.

Item Type: Article
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Additional Information: none
Keywords: LBM415, Pedptide deformylase, antibiotics, Phase 1, methemoglobinemia
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/3484

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