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19F-NMR based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers

Pearson, David and Garnier, Maxime and Luneau, Alexandre and James, Alexander David and Walles, Markus (2018) 19F-NMR based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers. Xenobiotica. pp. 1-24. ISSN 0049-82541366-5928

Abstract

1. Leniolisib is a novel oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor,
currently in clinical development for the treatment of inflammatory and
autoimmune diseases. 2. We investigated the absorption, metabolism, and
excretion of leniolisib in healthy subjects after a single oral 400 mg dose as part
of a first-in-human clinical study. The parent drug and metabolites were
quantified by 19F-NMR in plasma, urine and faeces after liquid chromatography
separation, and structures were determined by liquid chromatography coupled to
tandem mass spectrometry. 3. Drug related material was mainly excreted as
oxidative metabolites in urine and faeces, providing evidence that elimination
occurs mainly by metabolism. No metabolites were abundant in plasma relative
to the parent drug. An average mass balance of 66% was obtained, demonstrating
that relatively extensive elimination/excretion data can be obtained by 19F-NMR
in a first in human clinical study without use of a radiolabeled drug

Item Type: Article
Date Deposited: 29 Sep 2018 00:45
Last Modified: 29 Sep 2018 00:45
URI: https://oak.novartis.com/id/eprint/37026

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