4.6 Article

Drug-gut microbiota metabolic interactions: the case of UniPR1331, selective antagonist of the Eph-ephrin system, in mice

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DOI: 10.1016/j.jpba.2019.113067

Keywords

Eph-ephrin system; UniPR1331; High performance liquid chromatography (HPLC); High-resolution mass spectrometry (HR-MS); Drug-gut microbiota interactions; Faecal fermentation assay

Funding

  1. Centro Interdipartimentale Misure (CIM) G. Casnati of the University of Parma

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The interest on the role of gut microbiota in the biotransformation of drugs and xenobiotics has grown over the last decades and a deeper understanding of the mutual interactions is expected to help future improvements in the fields of drug development, toxicological risk assessment and precision medicine. In this paper, a microbiome drug metabolism case is presented, involving a lipophilic small molecule,N-(3 beta-hydroxy-Delta(5)-cholen-24-oyl)-L-tryptophan, UniPR1331, active as antagonist of the Eph ephrin system and effective in vivo in a murine orthotopic model of glioblastoma multiforme (GBM). Following the administration of a single 30 mg/l

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