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Modulation of oral bioavailability and metabolism for closely related cyclic hexapeptides

Vorherr, Thomas and Lewis, Ian and Berghausen, Joerg and Desrayaud, Sandrine and Schaefer, Michael (2017) Modulation of oral bioavailability and metabolism for closely related cyclic hexapeptides. International journal of peptide research and therapeutics..

Abstract

Recently, a variety of studies concerned with the permeability and oral bioavailability of cyclic peptides have been reported. In particular, strategies aiming at modifying peptides to maintain or to enhance solubility while enabling permeability constitute a significant challenge, but are of high interest to ensure a smooth drug discovery process. Current methodologies include N-methylation, matching of hydrogen bonding acceptors and donors across the macrocycle, and additional masking of polarity. In this study, we investigate further the pivotal effects of shielding on permeability and studied the metabolism of the corresponding peptides in more detail by comparing peptide concentrations in the portal versus the jugular vein in rats. Interestingly, minor changes in one particular side chain impact permeability and also liver metabolism.

Item Type: Article
Date Deposited: 31 Mar 2017 00:45
Last Modified: 31 Mar 2017 00:45
URI: https://oak.novartis.com/id/eprint/31715

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