Optimising in vivo pharmacology studies—Practical PKPD considerations

Abe, 2009, A novel type of implantable and programmable infusion pump for small laboratory animals, Journal of Pharmacological and Toxicological Methods, 59, 7, 10.1016/j.vascn.2008.09.002 Agoram, 2007, The role of mechanism-based pharmacokinetic-pharmacodynamic (PK–PD) modelling in translational research of biologics, Drug Discovery Today, 12, 1018, 10.1016/j.drudis.2007.10.002 Ariens, 1954, Affinity and intrinsic activity in the theory of competitive inhibition, Archives Internationale de Pharmacodynamie et de Therapie, 99, 32 Benet, 2002, Changes in plasma protein binding have little clinical relevance, Clinical Pharmacology & Therapeutics, 71, 115, 10.1067/mcp.2002.121829 Benson, N., Snelder, N. Ploeger, B., Napier, C., Sale, H., Birdsall, N.J.M., Butt, R.P., & Van der Graaf, P.H. (in press). Estimation of binding rate constants using a simultaneous mixed-effects method; application to SS, RR and racemic reboxetine. British Journal of Pharmacology. Berezhkovskiy, 2010, On the influence of protein binding on pharmacological activity of drugs, Journal of Pharmaceutical Sciences, 99, 2153, 10.1002/jps.21958 Bueters, 2009, Correct assessment of new compounds using in vivo screening models can reduce false positives, Drug Discovery Today, 14, 89, 10.1016/j.drudis.2008.09.003 Bundgaard, 2006, Mechanistic model of acute autoinhibitory feedback action after administration of SSRIs in rats: Application to escitalopram-induced effects on brain serotonin levels, European Journal of Pharmaceutical Sciences, 29, 394, 10.1016/j.ejps.2006.08.004 Calabrese, 2003, Special Issue: HORMESIS: Environmental and biomedical perspectives, Critical Reviews in Toxicology, 33, 213, 10.1080/713611039 Chakraborty, 1999, Mathematical modeling of circadian cortisol concentrations in indirect response models, Journal of Pharmacokinetics and Biopharmaceutics, 27, 23, 10.1023/A:1020678628317 Cohen, 2008, Pharmacokinetic and pharmacodynamic data to de derived from early-phase drug development—Designing informative human pharmacology studies, Clinical Pharmacokinetics, 47, 373, 10.2165/00003088-200847060-00002 Danhof, 2005, Mechanism-based pharmacokinetic–pharmacodynamic modeling—A new classification of biomarkers, Pharmacetical Research, 22, 1432, 10.1007/s11095-005-5882-3 Danhof, 2007, Mechanism-based pharmacokinetic–pharmacodynamic modeling for the prediction of in vivo drug concentration–effect relationships—Application in drug candidate selection and lead optimization, 885 Dayneka, 1993, Comparison of four basic models of indirect pharmacodynamic responses, Journal of Pharmacokinetics and Biopharmaceutics, 21, 457, 10.1007/BF01061691 Gabrielsson, 2006 Gabrielsson, 2009, Quantitative pharmacology or pharmacokinetic pharmacodynamic integration should be a vital component in integrative pharmacology, Journal of Pharmacology and Experimental Therapeutics, 331, 1, 10.1124/jpet.109.157172 Gabrielsson, 2009, Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds: Strategic considerations, Drug Discovery Today, 14, 358, 10.1016/j.drudis.2008.12.011 Gabrielsson, 1985, Constant rate of infusion—Improvement of tests for teratogenicity and embryotoxicity, Life Sciences, 37, 2275, 10.1016/0024-3205(85)90018-9 Grahame-Smith, 1997, ‘Keep on taking the tablets’: Pharmacological adaptation during long-term drug therapy, British Journal of Clinical Pharmacology, 44, 227, 10.1046/j.1365-2125.1997.00578.x Green, 2006, Neuropharmacology of 5-hydroxytryptamine, British Journal of Pharmacology, 147, S145, 10.1038/sj.bjp.0706427 Isaksson, 2009, Turnover modeling of non-esterified fatty acids in rats after multiple intravenous infusions of nicotinic acid, Dose–Response, 7, 247, 10.2203/dose-response.08-028.Isaksson Iwaki, 1996, Acute dose-dependent disposition studies of nicotinic acid in rats, Drug Metabolism and Disposition, 24, 773 Jusko, 1996, Historical perspectives on mechanistic pharmacokinetic/pharmacodynamic modelling, European Journal of Pharmaceutical Sciences, 4, S 17, 10.1016/S0928-0987(96)00026-7 Kenakin, 1997 Kenakin, 2008 Kleinbloesem, 1987, Rate of increase in the plasma concentration of nifedipine as a major determinant of its hemodynamic effects in humans, Clinical Pharmacoly & Therapeutics, 41, 26, 10.1038/clpt.1987.5 Kreilgaard, 2008, Prediction of clinical response based on pharmacokinetic/pharmacodynamic models of 5-hydroxytryptamine reuptake inhibitors in mice, British Journal of Pharmacology, 155, 276, 10.1038/bjp.2008.243 Levy, 1993, The case for preclinical pharmacodynamics, 7 Levy, 1994, Mechanism-based pharmacodynamic modeling, Clinical Pharmacology and Therapeutics, 56, 356, 10.1038/clpt.1994.149 Nagashima, 1969, Kinetics of pharmacologic effects in man: The anticoagulant action of warfarin, Clinical Pharmacology & Therapeutics, 10, 22, 10.1002/cpt196910122 Nau, 1981, A new model for embryotoxicity testing: Teratogenicity and pharmacokinetics of valproic acid following constant-rate administration in the mouse using human therapeutic drug and metabolite concentrations, Life Sciences, 29, 2803, 10.1016/0024-3205(81)90541-5 Oakes, 2005, Tesaglitazar, a dual PPARα/γ agonist, ameliorates glucose and lipid intolerance in obese Zucker rats, American Journal of Physiology, 289, R938 Ollerstam, 2006, Pharmacokinetic–pharmacodynamic modeling of drug-induced effect on the QT interval in conscious telemetered dogs, Journal of Pharmacological and Toxicological Methods, 53, 174, 10.1016/j.vascn.2005.07.002 Ollerstam, 2007, Comparison of the QT interval response during sinus and paced rhythm in conscious and anesthetized beagle dogs, Journal of Pharmacological and Toxicological Methods, 56, 131, 10.1016/j.vascn.2007.05.002 Olsen, 2008, Using pharmacokinetic–pharmacodynamic modelling as a tool for prediction of therapeutic effective plasma levels of antipsychotics, Euopean Journal of Pharmacology, 584, 318, 10.1016/j.ejphar.2008.02.005 Peletier, 2005, A dynamical systems analysis of the indirect response model with special emphasis on time to peak response, Journal of Pharmacokinetics and Pharmacodynamics, 32, 607, 10.1007/s10928-005-0047-x Ramazan, 1985, Kinetics of drug action in disease states. XIV. Effect of infusion rate on pentylenetetrazol concentrations in serum, brain and cerebrospinal fluid of rats at onset of convulsions, Journal of Pharmacology & Experimental Therapeutics, 234, 624 Rowland, 1995 Sällström, 2005, A pharmacodynamic turnover model capturing asymmetric circadian baselines of body temperature, heart rate and blood pressure in rats: Challenges in terms of tolerance and animal-handling effects, Journal of Pharmacokinetics and Pharmacodynamics, 3, 835, 10.1007/s10928-005-0087-2 Schmidt, 2010, Significance of protein binding in pharmacokinetics and pharmacodynamics, Journal of Pharmaceutical Sciences, 99, 1107, 10.1002/jps.21916 Sheiner, 1991, The intellectual health of clinical drug evaluation, Clinical Pharmacology & Therapeutics, 50, 4, 10.1038/clpt.1991.97 Stevens, 2009, A new minimal-stress freely-moving rat model for preclinical studies on intranasal administration of CNS drugs, Pharmeutical Research, 26, 1911, 10.1007/s11095-009-9907-1 Tabo, 2007, Monophasic action potential in anaesthetized guinea pigs as a biomarker for prediction of liability for drug-induced delayed ventricular repolarization, Journal of Pharmacological and Toxicological Methods, 55, 271, 10.1016/j.vascn.2006.11.002 Van der Graaf, 2008, Application of translational pharmacokinetic–pharmacodynamic (PKPD) modelling and simulation to preclinical safety testing, Preclinical World, 2008, 10 Van der Graaf, 2009, Pharmacokinetic–pharmacodynamic reasoning in drug discovery and early development, Future Medicinal Chemistry, 1, 1371, 10.4155/fmc.09.124 Yuan, 1993, Modeling blood/plasma concentrations in dosed feed and dosed drinking water toxicology studies, Toxicology and Applied Pharmacology, 119, 131, 10.1006/taap.1993.1052 Zuideveld, 2002, Pharmacokinetic–pharmacodynamic modelling of the hypothermic and corticosterone effects of the 5-HT1A receptor agonist flesinoxan, European Journal of Pharmacology, 445, 43, 10.1016/S0014-2999(02)01665-5