Prediction of Transporter-Mediated Rosuvastatin Hepatic Uptake Clearance and Drug Interaction in Humans Using Proteomics-Informed REF Approach

Suspended, plated, or sandwich-cultured human hepatocytes are routinely used for in vitro to in vivo extrapolation (IVIVE) of transporter-mediated hepatic clearance (CL) of drugs. However, these hepatocyte models have been reported to underpredict transporter-mediated in vivo hepatic uptake CL (CLup...

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Veröffentlicht in:	Drug metabolism and disposition 2021-02, Vol.49 (2), p.159-168
Hauptverfasser:	Kumar, Vineet, Yin, Mengyue, Ishida, Kazuya, Salphati, Laurent, Hop, Cornelis E.C.A., Rowbottom, Christopher, Xiao, Guangqing, Lai, Yurong, Mathias, Anita, Chu, Xiaoyan, Humphreys, W. Griffith, Liao, Mingxiang, Nerada, Zsuzsanna, Szilvásy, Nóra, Heyward, Scott, Unadkat, Jashvant D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line Chromatography, Liquid - methods Drug Interactions Hepatocytes - metabolism Humans Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics Organic Anion Transporters - metabolism Proteomics - methods Rosuvastatin Calcium - pharmacokinetics Tandem Mass Spectrometry - methods
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