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A Detailed Investigation on Conformation, Permeability and PK Properties of Two Related Cyclohexapeptides

Lewis, Ian and Schaefer, Michael and Wagner, Beatrix and Oberer, Lukas and Sager, Emine and Wipfli, Peter and Vorherr, Thomas (2014) A Detailed Investigation on Conformation, Permeability and PK Properties of Two Related Cyclohexapeptides. International Journal of Peptide Research and Therapeutics. ISSN 1573-3904

Abstract

Abstract: This contribution provides detailed insights regarding permeability properties of published cyclohexapeptides related to their conformation. The study includes data on oral bioavailability and PK parameters including application of a known enhancer. Interestingly, the latter did not show an effect, neither on the cyclic peptide exhibiting low oral uptake nor on the similar molecule showing a 30 % oral bioavailability in mice. These results are discussed in the context of exposed polar surface area for the preferred conformation and structural data obtained by NMR and X-ray crystallography.

Graphical Abstract: [Figure not available: see fulltext.]

Item Type: Article
Keywords: Conformation Cyclohexapeptides Permeability Pharmacokinetics
Date Deposited: 18 Oct 2017 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/23595

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