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

Bibliography

• Rowland M, Tozer TM. Clinical pharmacokinetics: concepts and applications. Williams &Wilkins, Philadelphia; 1995
   Google Scholar
• Mehavar R. Role of protein binding in pharmacokinetics. Am J Pharm Educ 2005;69(8):1-8
   Google Scholar
• Howard ML, Hill JJ, Galluppi GR, McLean MA. Plasma protein binding in drug discovery and development. Comb Chem High Troughput Screen 2010;13:170-87
   PubMed Web of Science ®Google Scholar
• Weiss HM, Fresneau M, Moenius T, Binding of pimecrolimus and tacrolimus to skin and plasma proteins : implication for systemic exposure after topical application. Drug Metab Dispos 2008;36(9):1812-18
   PubMed Web of Science ®Google Scholar
• Wasan KM, Cassidy SM. Role of plasma lipoproteins in modifying the biological activity of hydrophobic drugs. J Pharm Sci 1998;87(4):411-24
   PubMed Web of Science ®Google Scholar
• Dawidowicz AL, Kobielski M, Pieniadz J. Anomalous relationship between free drug fraction and its total concentration in drug-protein systems II. Binding of different ligands to plasma proteins. Eur J Pharm Sci 2008;35:136-41
   PubMed Web of Science ®Google Scholar
• Berezhkovskiy LM. On the possibility of self-induction of drug protein binding. J Pharm Sci 2010;99:4400-5
   PubMed Web of Science ®Google Scholar
• Herve F, Urien S, Albengres E, Drug binding in plasma: a summary of recent trends in the study of drug and hormone binding. Clin Pharmacokinet 1994;26(1):44-58
   PubMed Web of Science ®Google Scholar
• Tillement JP, Duche JC, Barre J. Drug binding to blood proteins: characteristics, roles and pathophysiological changes. Bull Acad Natle Med 2006;190(4-5):935-47
   PubMed Web of Science ®Google Scholar
• Trainor GL. The importance of plasma protein binding in drug discovery. Expert Opin Drug Discov 2007;2(1):51-64
   PubMed Web of Science ®Google Scholar
• Tillement JP, Urien S, Chaumet-Riffaud P, Blood binding and tissue uptake of drugs. Recent advances and perspectives. Fundam Clin Pharmacol 1988;2:223-38
   PubMed Web of Science ®Google Scholar
• Gerskowitch VP, Hodge J, Hull RAD, Unexpected relationship between plasma protein binding and the pharmacodynamics of 2-NAP, a CCK1- receptor antagonist. Br J Clin Pharmacol 2007;63(5):618-22
   PubMed Web of Science ®Google Scholar
• Boffito M, Back DJ, Blaschke TF, Protein binding in antiretroviral therapies. AIDS Res Hum Retroviruses 2003;19(9):825-35
   PubMed Web of Science ®Google Scholar
• Spooner N, Lad R, Barfield M. Dried Blood Spots as a sample collection technique for the determination of pharmacokinetics in clinical studies: considerations for the validation of a quantitative bioanalytical method. Anal Chem 2009;81:1557-63
   PubMed Web of Science ®Google Scholar
• Patel P, Mulla H, Tanna S. Facilitating pharmacokinetic studies in children: a new use of dried blood spots. Arch Dis Child 2010;95:484-7
   PubMed Web of Science ®Google Scholar
• Banker MJ, Clark TH. Plasma/serum protein binding determinations. Curr Drug Metab 2008;9:854-9
   PubMed Web of Science ®Google Scholar
• Vuignier K, Schappler J, Veuthey JL, Drug protein binding: a critical review of analytical tools. Anal Bioanal Chem 2010;398:53-66
   PubMed Web of Science ®Google Scholar
• Chuang VTG, Maruyama T, Otagiri M. Updates on contemporary protein binding techniques. Drug Metab Pharmacokinet 2009;24(4):358-64
   PubMed Web of Science ®Google Scholar
• Note for guidance on the investigation of drug interactions CPMP/EWP/560/95 (1997). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.tga.gov.au/docs/pdf/euguide/ewp/056095en.pdf
   Google Scholar
• Guidance on the investigation of drug interactions CPMP/EWP/560/95 Draft (2010). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/05/WC500090112.pdf
   Google Scholar
• Pharmacokinetics in patients with impaired renal function-Study design, data analysis and impact on dosing and labelling Draft (2010). FDA/Center for drug evaluation and research. Available from: www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM204959.pdf
   Google Scholar
• Pharmacokinetics in patients with impaired hepatic function -Study design, data analysis and impact on dosing and labelling (2003). FDA/Center for drug evaluation and research. Available from: www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm072123.pdf
   Google Scholar
• Goodman and Gilman's the pharmacological basis of therapeutics. 10th edition. McGraw-Hill, New York; 2001
   Google Scholar
• Liu X, Chen C, Hop CECA. Do we need to optimize plasma protein and tissue binding in drug discovery? Curr Top Med Chem 2011;11:450-66
   PubMed Web of Science ®Google Scholar
• Trainor GL. Plasma protein binding and the free drug principle: recent developments and applications. Annu Rep Med Chem 2007;42:489-502
   Web of Science ®Google Scholar
• Berezhkovskij LM. On the influence of protein binding on pharmacological activity of drugs. J Pharm Sci 2010;99(4):2153-65
   PubMed Web of Science ®Google Scholar
• Braggio S, Montanari D, Rossi T, Ratti E. Drug efficiency: a new concept to guide lead optimization programs towards the selection of better clinical candidates. Expert Opin Drug Discov 2010;5(7):1-9
   PubMedGoogle Scholar
• Summerfield SG, Lucas AJ, Porter RA, Toward an improved prediction of human in vivo brain penetration. Xenobiotica 2008;38(12):1518-35
   PubMed Web of Science ®Google Scholar
• Read KD, Braggio S. Assessing brain free fraction in early drug discovery. Expert Opin Drug Metab Toxicol 2010;6(3):337-44
   PubMed Web of Science ®Google Scholar
• Benko R, Matuz M, Doro P, Pharmacokinetics and pharmacodynamics of levofloxacin in critically ill patients with ventilator-associated pneumonia. Int J Antimicro Ag 2007;30:162-8
   PubMed Web of Science ®Google Scholar
• Smith DA, Di L, Kerns EH. The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery. Nat Rev Drug Discov 2010;9(12):929-39
   PubMed Web of Science ®Google Scholar
• Guidance on Nonclinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization for Pharmaceuticals CPMP/ICH/286/95 (2009). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002720.pdf
   Google Scholar
• Pharmacokinetics and metabolic studies in the safety evaluation of new medical products in animals 3BS11A (1994). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002886.pdf
   Google Scholar
• Pharmacokinetic studies in man 3CC3a (1988). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.tga.gov.au/DOCS/pdf/euguide/vol3c/3cc3aen.pdf
   Google Scholar
• Note for guidance on Toxicokinetics: a guidance for assessing systemic exposure in toxicology studies CPMP/ICH/384/95 (2009). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002770.pdf
   Google Scholar
• Note for guidance on dose selection for carcinogenicity studies of pharmaceuticals EMEA/CHMP/ICH/383/1995 (2008). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002768.pdf
   Google Scholar
• Lumpkin MH, Bruckner JV, Campbell JL, Plasma binding of thrichloroacetic acid in mice, rats and humans under cancer bioassay and environmental exposure conditions. Drug Metab Dispos 2003;31:1203-7
   PubMed Web of Science ®Google Scholar
• Kajbaf M, Barnaby RJ, Bottacini M, Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica 2003;33:415-28
   PubMed Web of Science ®Google Scholar
• Hoke JF, Dyker AG, Barnaby RJ, Lees KR. Pharmacokinetics of a glycine site antagonist (gavestinel) following multiple dosing in patients with acute stroke. Eur J Clin Pharmacol 2000;55:867-72
   PubMed Web of Science ®Google Scholar
• Iavarone L, Hoke JF, Bottacini M, First time in human for GV196771: interspecies scaling applied on dose selection. J Clin Pharmacol 1999;39:560-6
   PubMed Web of Science ®Google Scholar
• Dyker AG, Lees KR. Safety and tolerability of GV150526 (a glycine site antagonist at the N-methyl- D-aspartate receptor) in patients with acute stroke. Stroke 1999;30(5):986-92
   PubMed Web of Science ®Google Scholar
• Webster R, Leishman D, Walker D. Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Curr Opin Drug Discov Devel 2002;5(1):116-26
   PubMed Web of Science ®Google Scholar
• Barre J, Riant P, Tillement JP. Measurement of free drug in phase 1: is it useful? Fundam Clin Pharmacol 1990;4(S2):141s-50s
   PubMedGoogle Scholar
• Note for guidance on the evaluation of the pharmacokinetics of medicinal products in patients with impaired renal function CHMP/EWP/225/02 (2004). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500003123.pdf
   Google Scholar
• Guideline on the evaluation of the pharmacokinetics of medicinal products in patients with impaired hepatic function CPMP/EWP/2339/02 (2005). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.tga.gov.au/docs/pdf/euguide/ewp/233902en.pdf
   Google Scholar
• Palatini P, Orlando R, De Martin S. The effect of liver disease on inhibitory and plasma protein-binding displacement interactions: an update. Expert Opin Drug Metab Toxicol 2010;6(10):1215-30
   PubMed Web of Science ®Google Scholar
• Leopold D, Webb D, Buss DC, The ex vivo plasma protein binding of theophylline in renal disease. Br J Clin Pharmacol 1985;19(6):823-5
   PubMed Web of Science ®Google Scholar
• Verbeeck RK, Cardinal JA, Wallace SM. Effect of age and sex on the plasma binding of acidic and basic drugs. Eur J Clin Pharmacol 1984;27(1):91-7
   PubMed Web of Science ®Google Scholar
• Guideline on the investigation of medicinal products in the term and preterm neonate. Doc Ref. EMEA/536810/2008 (2009). The European Agency for the Evaluation of Medicinal Products. Human medicines evaluation unit. Available from: www.emea.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500003750.pdf
   Google Scholar
• Viani A, Rizzo G, Carrai M, Pacifici GM. The effect of aging on plasma albumin and plasma protein binding of diazepam, salicylic acid and digitoxin in healthy subjects and patients with renal impairment. Br J Clin Pharmacol 1992;33(3):299-304
   PubMed Web of Science ®Google Scholar
• Clinical lactation studies – study design; data analysis, and recommendations for labelling. Draft (2005). FDA/Center for drug evaluation and research. Available from: www.fda.gov/downloads/RegulatoryInformation/Guidances/ucm127505.pdf
   Google Scholar
• Pharmacokinetics in pregnancy – study design, data analysis and impact on dosing and labelling. Draft (2004). FDA/Center for drug evaluation and research. Available from: www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm072133.pdf
   Google Scholar
• Rolan PE. Plasma protein binding displacement interactions. Why are they still regarded as clinically important? Br J Clin Pharmacol 1994;37(2):125-8
   PubMed Web of Science ®Google Scholar
• Benet LZ, Hoener BA. Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 2002;71(3):115-21
   PubMed Web of Science ®Google Scholar
• Sandson NB, Marcucci C, Bourke DL, Smith-Lamacchia R. An interaction between aspirin and valproate: the relevance of plasma protein displacement drug-drug interactions. Am J Psychiatry 2006;163(11):1891-6
   PubMed Web of Science ®Google Scholar
• Christensen H, Baker M, Tucker GT, Rostami-Hodjegan A. Prediction of plasma protein binding displacement and its implications for quantitative assessment of metabolic drug-drug interactions from in vitro data. J Pharm Sci 2006;95:2778-87
   PubMed Web of Science ®Google Scholar
• Israili ZH, Dayton PG. Human alpha-1-glycoprotein and its interactions with drugs. Drug Metab Rev 2001;33(2):161-235
   PubMed Web of Science ®Google Scholar
• Fuse E, Tanii H, Kurata N, Unexpected clinical pharmacology of UCN-01 caused by specific binding to human alpha1-AGP. Cancer Res 1998;58(15):3248-53
   PubMed Web of Science ®Google Scholar
• Mealy NE, Bayes M. Radafaxine hydrochloride. Drugs Future 2004;29(9):967
   Google Scholar
• Volcow ND, Wang GJ, Fowler JS, The slow and long-lasting blockade of dopamine transporters in human brain induced by the new antidepressant drug radafaxine predicts poor reinforcing effects. Biol Psychiatry 2005;57(6):640-6
   PubMed Web of Science ®Google Scholar
• Rossato P. Can plasma protein binding represent a safety issue for drug development? The radafaxine case. Drug Metab Rev 2008;40(s3):15
   Google Scholar
• Sadler BM, Gillotin C, Lou Y, Stein DS. In vivo effect of alpha1-acid glycoprotein on pharmacokinetics of amprenavir, a human immunodeficiency virus protease inhibitor. Antimicrob Agents Chemother 2001;45(3):852-6
   PubMed Web of Science ®Google Scholar
• Baille TA, Cayen MN, Fouda H, Drug metabolites in safety testing. Toxicol Appl Pharmacol 2002;182:188-96
   PubMed Web of Science ®Google Scholar
• Atrakchi AH. Interpretation and considerations on the safety evaluation of human drug metabolites. Chem Res Toxicol 2009;22:1217-20
   PubMed Web of Science ®Google Scholar
• Hinderling PH. Red blood cells: a neglected compartment in pharmacokinetics and pharmacodynamics. Pharmacol Rev 1997;49(3):279-94
   PubMed Web of Science ®Google Scholar
• Snoeck E, Piotrovskij V, Jacqmin P, Population analysis of the non linear red blood cell partitioning and the concentration- effect relationship of draflazine following various infusion rates. Br J Clin Pharm 1997;43(6):603-12
   PubMed Web of Science ®Google Scholar
• Tanaka C, Kawai R, Rowland M. Dose-dependent pharmacokinetics of cyclosporine A in rats: events in tissues. Drug Metab Dispos 2000;28:582-9
   PubMed Web of Science ®Google Scholar
• Mohammed SS, Christopher MM, Metha P, Increased erythrocyte and protein binding of codeine in patients with sickle cell disease. J Pharm Sci 1993;82(11):1112-17
   PubMed Web of Science ®Google Scholar
• Highley MS, De Bruijn EA. Erythrocytes and the transport of drugs and endogenous compounds. Pharm Res 1996;13(2):186-95
   PubMed Web of Science ®Google Scholar
• Gneushev ET, Gneusheva IA. The binding of drugs to erythrocytes. Eksp Klin Farmakol 1996;59(5):75
   Google Scholar
• Maling TJB, Siebers RW, Burgess CD, Individual variability of amiodarone distribution in plasma and erythrocytes: implications for therapeutic monitoring. Ther Drug Monit 1989;11:121-6
   PubMed Web of Science ®Google Scholar
• Urien S, Bastian G, Lucas C, Binding of a new vinca alkaloid derivative, S12363, to human plasma proteins and platelets. Usefulness of an erythrocyte partitioning technique. Invest New Drugs 1992;10:263-8
   PubMed Web of Science ®Google Scholar
• Loos WJ, Gelberbloom H, Verweij J, Red blood cells: a neglected compartment in topotecan pharmacokinetic analysis. Anticancer Drugs 2003;14(3):227-32
   PubMed Web of Science ®Google Scholar
• Farowski F, Cornely OA, Vehreschild JJ, Intracellular concentrations of posaconazole in different compartments of peripheral blood. Antimicrob Agents Chemother 2010;54(7):2928-31
   PubMed Web of Science ®Google Scholar
• Berquivist Y, Domeij-Nimberg B. Distribution of chloroquine and its metabolite desethyl-chloroquine in human blood cells and its implication for the quantitative determination of these compounds in serum and plasma. J Chromatogr 1983;272(1):137-48
   PubMed Web of Science ®Google Scholar
• Water NJ, Jones R, Williams G, Sohal B. Validation of a Rapid Equilibrium Dialysis approach for the measurement of plasma protein binding. J Pharm Sci 2008;97(10):4586-95
   PubMed Web of Science ®Google Scholar
• Fura A, Harper TW, Zhang H, Shift in pH of biological fluids during storage and processing: effect on bionalysis. J Pharm Sci 2003;32:513-22
   Google Scholar
• Kochansky CJ, McMasters D, Lu P, Impact of pH on plasma protein binding in equilibrium dialysis. Mol Pharm 2008;5(3):438-48
   PubMed Web of Science ®Google Scholar