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The importance of plasma protein binding in drug discovery

Pages 51-64 | Published online: 16 Jan 2007

Keep up to date with the latest research on this topic with citation updates for this article.

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Birk Poller, Sophie Werner, Norbert Domange, Lina Mettler, Richard R. Stein, Jacqueline Loretan, Markus Wartmann, Bernard Faller & Felix Huth. (2022) Time matters – in vitro cellular disposition kinetics help rationalizing cellular potency disconnects. Xenobiotica 52:8, pages 878-889.
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Yue Hu, Haijun Li, Min Wu, Hong Zhang, Yanhua Ding, Yun Peng, Xiaojiao Li & Zhenxiang Yu. (2021) Single and multiple dose pharmacokinetics and safety of ZSP1273, an RNA polymerase PB2 protein inhibitor of the influenza A virus: a phase 1 double-blind study in healthy subjects. Expert Opinion on Investigational Drugs 30:11, pages 1159-1167.
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Maki Miyamoto, Yohei Kosugi, Shinji Iwasaki, Ikumi Chisaki, Sayaka Nakagawa, Nobuyuki Amano & Hideki Hirabayashi. (2021) Characterization of plasma protein binding in two mouse models of humanized liver, PXB mouse and humanized TK-NOG mouse. Xenobiotica 51:1, pages 51-60.
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Mengchun Chen, Xufei Zhang, Yijie Chen, Wei Sun, Zhe Wang, Chengke Huang, Guoxin Hu & Ruijie Chen. (2020) Comparison of the inhibitory effect of ketoconazole, voriconazole, fluconazole, and itraconazole on the pharmacokinetics of bosentan and its corresponding active metabolite hydroxy bosentan in rats. Xenobiotica 50:3, pages 280-287.
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Takuya Ebihara, Hisao Shimizu, Masami Yamamoto, Tomoaki Higuchi, Fumihiro Jinno & Yoshihiko Tagawa. (2019) The effect of elevated α1-acid glycoprotein on the pharmacokinetics of TAK-272 (SCO-272), an orally active renin inhibitor, in rats. Xenobiotica 49:5, pages 584-590.
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Fotios Tsopelas, Constantinos Giaginis & Anna Tsantili-Kakoulidou. (2017) Lipophilicity and biomimetic properties to support drug discovery. Expert Opinion on Drug Discovery 12:9, pages 885-896.
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Yan Li, Chun Chen, Chunping Zhang, Jingyu Duan, Huankai Yao & Qunli Wei. (2017) Probing the binding interaction of AKR with human serum albumin by multiple fluorescence spectroscopy and molecular modeling. Journal of Biomolecular Structure and Dynamics 35:6, pages 1189-1199.
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Mario Pellegatti, Sabrina Pagliarusco, Lara Solazzo & Dimitri Colato. (2011) Plasma protein binding and blood-free concentrations: which studies are needed to develop a drug?. Expert Opinion on Drug Metabolism & Toxicology 7:8, pages 1009-1020.
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John Reilly, Donnya Etheridge, Brian Everatt, Zhengjin Jiang, Clive Aldcroft, Penny Wright, Ian Clemens, Brian Cox, NeilJ. Press, Simon Watson, David Porter, Clayton Springer & RobinA. Fairhurst. (2011) STUDIES IN DRUG ALBUMIN BINDING USING HSA AND RSA AFFINITY METHODS. Journal of Liquid Chromatography & Related Technologies 34:4, pages 317-327.
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Rumin Zhang & Frederick Monsma. (2010) Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs. Expert Opinion on Drug Discovery 5:11, pages 1023-1029.
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