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Plasma protein binding and blood-free concentrations: which studies are needed to develop a drug?

(DMPK Director (now retired)) , (DMPK principal scientist) , (DMPK scientist) & (DMPK scientist)
Pages 1009-1020 | Published online: 02 Jun 2011

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Anis Ahmad, Aiman Ahmad, Raja Sudhakar, Himani Varshney, Naidu Subbarao, Saba Ansari, Abdul Rauf & Asad U. Khan. (2017) Designing, synthesis, and antimicrobial action of oxazoline and thiazoline derivatives of fatty acid esters. Journal of Biomolecular Structure and Dynamics 35:15, pages 3412-3431.
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Articles from other publishers (21)

Changkyu Lee. (2024) Albumin hydrogels for repeated capture of drugs from the bloodstream and release into the tumor. Journal of Controlled Release 365, pages 384-397.
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Zon-Min Lee, Ling-Sai Chang, Kuang-Che Kuo, Meng-Chiao Lin & Hong-Ren Yu. (2023) Impact of Protein Binding Capacity and Daily Dosage of a Drug on Total Serum Bilirubin Levels in Susceptible Infants. Children 10:6, pages 926.
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Joaquim Trigo Marquês, Catarina Frazão De Faria, Marina Reis, Diana Machado, Susana Santos, Maria da Soledade Santos, Miguel Viveiros, Filomena Martins & Rodrigo F. M. De Almeida. (2022) In vitro Evaluation of Isoniazid Derivatives as Potential Agents Against Drug-Resistant Tuberculosis. Frontiers in Pharmacology 13.
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Hiran A. Prag, Laura Pala, Duvaraka Kula-Alwar, John F. Mulvey, Du Luping, Timothy E. Beach, Lee M. Booty, Andrew R. Hall, Angela Logan, Volha Sauchanka, Stuart T. Caldwell, Ellen L. Robb, Andrew M. James, Zhelong Xu, Kourosh Saeb-Parsy, Richard C. Hartley, Michael P. Murphy & Thomas Krieg. (2020) Ester Prodrugs of Malonate with Enhanced Intracellular Delivery Protect Against Cardiac Ischemia-Reperfusion Injury In Vivo. Cardiovascular Drugs and Therapy 36:1, pages 1-13.
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Yejin Esther Yun & Andrea N. Edginton. (2021) Prediction of fraction unbound in plasma in children in data-limited scenarios for human health risk assessment. Computational Toxicology 18, pages 100168.
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Yanwen Chen, Weiwei Tang, Andrew Gordon & Bin Li. (2020) Development of an Integrated Tissue Pretreatment Protocol for Enhanced MALDI MS Imaging of Drug Distribution in the Brain. Journal of the American Society for Mass Spectrometry 31:5, pages 1066-1073.
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Karolina Wanat. (2020) Biological barriers, and the influence of protein binding on the passage of drugs across them. Molecular Biology Reports 47:4, pages 3221-3231.
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Samar Y. Mahmoud, Fredrik Svensson, Azedine Zoufir, Dezső Módos, Avid M. Afzal & Andreas Bender. (2019) Understanding Conditional Associations between ToxCast in Vitro Readouts and the Hepatotoxicity of Compounds Using Rule-Based Methods . Chemical Research in Toxicology 33:1, pages 137-153.
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Wei-Ching Chen, Pei-Wei Huang, Wan-Ling Yang, Yen-Lun Chen, Ying-Ning Shih & Hong-Jaan Wang. (2019) Fundamentals of Pharmacokinetics to Assess the Correlation Between Plasma Drug Concentrations and Different Blood Sampling Methods. Pharmaceutical Research 36:2.
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Hua-xin Zhang, Dan Zhou & Qing-hua Xia. (2018) Study on the molecular recognition action of lamivudine by human serum albumin. Journal of Molecular Recognition 31:7, pages e2705.
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Pran Kishore Deb, Omar Al-Attraqchi, Mailavaram Raghu Prasad & Rakesh K. Tekade. 2018. Dosage Form Design Considerations. Dosage Form Design Considerations 371 399 .
P. Nugent, J.N. Duncan & D.B. Colagiovanni. 2017. A Comprehensive Guide to Toxicology in Nonclinical Drug Development. A Comprehensive Guide to Toxicology in Nonclinical Drug Development 189 213 .
Ting-Ting Liu, Li-Li Xiang, Jian-Ling Wang & Dong-Ying Chen. (2015) Application of capillary electrophoresis-frontal analysis for comparative evaluation of the binding interaction of captopril with human serum albumin in the absence and presence of hydrochlorothiazide. Journal of Pharmaceutical and Biomedical Analysis 115, pages 31-35.
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George Lambrinidis, Theodosia Vallianatou & Anna Tsantili-Kakoulidou. (2015) In vitro, in silico and integrated strategies for the estimation of plasma protein binding. A review. Advanced Drug Delivery Reviews 86, pages 27-45.
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Paolo Ascenzi, Gabriella Fanali, Mauro Fasano, Valentina Pallottini & Viviana Trezza. (2014) Clinical relevance of drug binding to plasma proteins. Journal of Molecular Structure 1077, pages 4-13.
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Karine Vuignier, Jean-Luc Veuthey, Pierre-Alain Carrupt & Julie Schappler. (2013) Global analytical strategy to measure drug–plasma protein interactions: from high-throughput to in-depth analysis. Drug Discovery Today 18:21-22, pages 1030-1034.
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Xiang-Wei Zhu, Alexander Sedykh, Hao Zhu, Shu-Shen Liu & Alexander Tropsha. (2013) The Use of Pseudo-Equilibrium Constant Affords Improved QSAR Models of Human Plasma Protein Binding. Pharmaceutical Research 30:7, pages 1790-1798.
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Paul Nugent, J. Neil Duncan & Dorothy B. Colagiovanni. 2013. A Comprehensive Guide to Toxicology in Preclinical Drug Development. A Comprehensive Guide to Toxicology in Preclinical Drug Development 309 334 .
Emily A. Peterson, Alessandro A. Boezio, Paul S. Andrews, Christiane M. Boezio, Tammy L. Bush, Alan C. Cheng, Deborah Choquette, James R. Coats, Adria E. Colletti, Katrina W. Copeland, Michelle DuPont, Russell Graceffa, Barbara Grubinska, Joseph L. Kim, Richard T. Lewis, Jingzhou Liu, Erin L. Mullady, Michele H. Potashman, Karina Romero, Paul L. Shaffer, Mary K. Stanton, John C. Stellwagen, Yohannes Teffera, Shuyan Yi, Ti Cai & Daniel S. La. (2012) Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors. Bioorganic & Medicinal Chemistry Letters 22:15, pages 4967-4974.
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Gabriella Fanali, Alessandra di Masi, Viviana Trezza, Maria Marino, Mauro Fasano & Paolo Ascenzi. (2012) Human serum albumin: From bench to bedside. Molecular Aspects of Medicine 33:3, pages 209-290.
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Francisco Max Damico, Mariana Ramos Scolari, Gabriela Lourençon Ioshimoto, Beatriz Sayuri Takahashi, Armando da Silva CunhaJr.Jr., Sílvia Ligório Fialho, Daniela Maria Bonci, Fabio Gasparin & Dora Fix Ventura. (2012) Vitreous pharmacokinetics and electroretinographic findings after intravitreal injection of acyclovir in rabbits. Clinics 67:8, pages 931-937.
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