Lewis, Ian, Schaefer, Michael, Wagner, Beatrix, Oberer, Lukas, Sager, Emine, 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