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Pharmacokinetic Studies around the Mono- and Difunctionalization of a Bioavailable Cyclic Decapeptide Scaffold

Fouche, Marianne and Schaefer, Michael and Berghausen, Joerg and Desrayaud, Sandrine and Roth, Hans-Joerg (2016) Pharmacokinetic Studies around the Mono- and Difunctionalization of a Bioavailable Cyclic Decapeptide Scaffold. ChemMedChem.

Abstract

We have previously reported the design of several cyclic decapeptides including 1, based on a generic scaffold, that achieved favourable oral bioavailability and exposure. With the goal to further investigate the potential of this approach, we describe herein the effect of functionalization of this scaffold. A series of cyclic decapeptides was therefore subjected to a range of in vitro assays and PK studies in order to investigate whether the introduction of polar or charged groups could be tolerated by the “engineered” scaffold while maintaining good PK profiles. We have identified several cyclic decapeptides exhibiting excellent PK profiles while also showing an improved solubility compared to 1.

Item Type: Article
Date Deposited: 19 May 2016 23:45
Last Modified: 29 Jun 2016 23:45
URI: https://oak.novartis.com/id/eprint/28437

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