286
Views
8
CrossRef citations to date
0
Altmetric
Reviews

Translational pharmacokinetics: challenges of an emerging approach to drug development in stroke

, BSc, , PhD, , FRS FIBIOL FMedSci (Professor of Physiology) & , MD MRCS PhD (Neurosurgery Registrar & Researcher)
Pages 681-695 | Published online: 27 Apr 2011

Bibliography

  • Meairs S, Wahlgren N, Dirnagl U, Stroke Research Priorities for the Next Decade - A Representative View of the European Scientific Community. Cerebrovasc Dis 2006;22:75-82
  • Huang P, Chen C, Yang Y, Eligibility for Recombinant Tissue Plasminogen Activator in Acute Ischemic Stroke. Cerebrovasc Dis 2006;22:423-8
  • Dorhout Mees SM, Rinkel GJE, Feigin VL, Calcium antagonists for aneurysmal subarachnoid haemorrhage. Cochrane Database Syst Rev 2007, doi:10.1002/14651858.CD000277.pub3
  • O'Collins VE, Macleod MR, Donnan GA, 1,026 Experimental treatments in acute stroke. Ann Neurol 2006;59:467-77
  • Savitz SI. A critical appraisal of the NXY-059 neuroprotection studies for acute stroke: a need for more rigorous testing of neuroprotective agents in animal models of stroke. Exp Neurol 2007;205:20-5
  • Sena E, van der Worp HB, Howells D, How can we improve the pre-clinical development of drugs for stroke? Trends Neurosci 2007;30:433-9
  • Gladstone DJ, Black SE, Hakim AM. Toward wisdom from failure: lessons from neuroprotective stroke trials and new therapeutic directions. Stroke 2002;33:2123-36
  • Fisher M. STAIR: enhancing the development and approval of acute stroke therapies: stroke therapy academic industry roundtable. Stroke 2005;36:1808-13
  • Ritter JM. Pharmacokinetic(s) matters: stroke treatment et cetera. Br J Clin Pharmacol 2008;65:299-300
  • Savitz SI, Fisher M. Future of neuroprotection for acute stroke: in the aftermath of the SAINT trials. Ann Neurol 2007;61:396-402
  • Allan SM, Tyrrell PJ, Rothwell NJ. Interleukin-1 and neuronal injury. Nat Rev Immunol 2005;5:629-40
  • Mulcahy NJ, Ross J, Rothwell NJ, Delayed administration of interleukin-1 receptor antagonist protects against transient cerebral ischaemia in the rat. Br J Pharmacol 2003;140:471-6
  • Emsley HC, Smith CJ, Gavin CM, An early and sustained peripheral inflammatory response in acute ischaemic stroke: relationships with infection and atherosclerosis. J Neuroimmunol 2003;139:93-101
  • Emsley HC, Smith CJ, Georgiou RF, A randomised phase II study of interleukin-1 receptor antagonist in acute stroke patients. J Neurol Neurosurg Psychiatry 2005;76:1366-72
  • Tadros A, Crocco T, Davis SM, Emergency medical services-based community stroke education: pilot results from a novel approach. Stroke 2009;40:2134-42
  • de la Ossa NP, Sanchez-Ojanguren J, Palomeras E, Influence of the stroke code activation source on the outcome of acute ischemic stroke patients. Neurology 2008;70:1238-43
  • Gargano JW, Wehner S, Reeves MJ. Do Presenting Symptoms Explain Sex Differences in Emergency Department Delays Among Patients With Acute Stroke? Stroke 2009, doi:10.1161/STROKEAHA.108.543116
  • Berthet C, Lei H, Thevenet J, Neuroprotective role of lactate after cerebral ischemia. J Cereb Blood Flow Metab 2009;29:1780-9
  • Sacco RL, DeRosa JT, Haley EC, Glycine antagonist in neuroprotection for patients with acute stroke: GAIN Americas: a randomized controlled trial. JAMA 2001;285:1719-28
  • Kaya D, Gursoy-Ozdemir Y, Yemisci M, VEGF protects brain against focal ischemia without increasing blood-brain permeability when administered intracerebroventricularly. J Cereb Blood Flow Metab 2005;25:1111-18
  • Fagan SC, Edwards DJ, Borlongan CV, Optimal delivery of minocycline to the brain: implication for human studies of acute neuroprotection. Exp Neurol 2004;186:248-51
  • Barone FC, Irving EA, Ray AM, SB 239063, a Second-Generation p38 Mitogen-Activated Protein Kinase Inhibitor, Reduces Brain Injury and Neurological Deficits in Cerebral Focal Ischemia. J Pharmacol Exp Ther 2001;296:312-21
  • Galea J, Ogungbenro K, Hulme S, Intravenous anakinra can achieve experimentally effective concentrations in the central nervous system within a therapeutic time window: results of a dose-ranging study. J Cereb Blood Flow Metab 2011;31:439-47
  • McColl B, Allan S, Rothwell N. Systemic infection, inflammation and acute ischemic stroke. Neuroscience 2009;158:1049-61
  • Hurst S, Loi C, Brodfuehrer J, Impact of physiological, physicochemical and biopharmaceutical factors in absorption and metabolism mechanisms on the drug oral bioavailability of rats and humans. Expert Opin Drug Metab Toxicol 2007;3:469-89
  • Smith WS, Sung G, Saver J, Mechanical Thrombectomy for Acute Ischemic Stroke: final results of the multi MERCI trial. Stroke 2008;39:1205-12
  • del Zoppo GJ, Higashida RT, Furlan AJ, PROACT: a phase II randomized trial of recombinant pro-urokinase by direct arterial delivery in acute middle cerebral artery stroke. Stroke 1998;29:4-11
  • Munoz R, Morell V, Cruz E, Critical Care of Children with Heart Disease [Internet]. Springer London; 2010
  • Yang BB, Baughman S, Sullivan JT. Pharmacokinetics of anakinra in subjects with different levels of renal function. Clin Pharmacol Ther 2003;74:85-94
  • Clark SR, McMahon CJ, Gueorguieva I, Interleukin-1 receptor antagonist penetrates human brain at experimentally therapeutic concentrations. J Cereb Blood Flow Metab 2008;28:387-94
  • Greenhalgh AD, Galea J, Denes A, Rapid brain penetration of interleukin-1 receptor antagonist in rat cerebral ischaemia: pharmacokinetics, distribution, protection. Br J Pharmacol 2010;160:153-9
  • Galliford JW, Malasana R, Farrington K. Switching from subcutaneous to intravenous erythropoietin alpha in haemodialysis patients requires a major dose increase. Nephrol Dial Transplant 2005;20:1956-62
  • Emsley HC, Hopkins SJ. Acute ischaemic stroke and infection: recent and emerging concepts. Lancet Neurol 2008;7:341-53
  • Langdon PC, Lee AH, Binns CW. Dysphagia in acute ischaemic stroke: severity, recovery and relationship to stroke subtype. J Clin Neurosci 2007;14:630-4
  • Crome P, Rizeq M, George S, Drug absorption may be delayed after stroke: results of the paracetamol absorption test. Age Ageing 2001;30:391-3
  • DeSesso JM, Jacobson CF. Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol 2001;39:209-28
  • Dhuria SV, Hanson LR, Frey WH. Intranasal delivery to the central nervous system: mechanisms and experimental considerations. J Pharm Sci 2010;99:1654-73
  • De Rosa R, Garcia AA, Braschi C, Intranasal administration of nerve growth factor (NGF) rescues recognition memory deficits in AD11 anti-NGF transgenic mice. Proc Natl Acad Sci USA 2005;102:3811-16
  • Fletcher L, Kohli S, Sprague SM, Intranasal delivery of erythropoietin plus insulin-like growth factor–I for acute neuroprotection in stroke. J Neurosurg 2009;111:164-70
  • Hanson LR, Roeytenberg A, Martinez PM, Intranasal deferoxamine provides increased brain exposure and significant protection in rat ischemic stroke. J Pharmacol Exp Ther 2009;330:679-86
  • Harkema JR. Comparative pathology of the nasal mucosa in laboratory animals exposed to inhaled irritants. Environ Health Perspect 1990;85:231-8
  • Cecchelli R, Berezowski V, Lundquist S, Modelling of the blood-brain barrier in drug discovery and development. Nat Rev Drug Discov 2007;6:650-61
  • Kola I, Landis J. Can the pharmaceutical industry reduce attrition rates? Nat Rev Drug Discov 2004;3:711-16
  • Abbott NJ, Ronnback L, Hansson E. Astrocyte-endothelial interactions at the blood-brain barrier. Nat Rev Neurosci 2006;7:41-53
  • Abbott NJ, Patabendige AA, Dolman DE, Structure and function of the blood-brain barrier. Neurobiol Dis 2010;37:13-25
  • Engelhardt B, Sorokin L. The blood–brain and the blood–cerebrospinal fluid barriers: function and dysfunction. Semin Immunopathol 2009;31:497-511
  • de Lange ECM, Danhof M. Considerations in the use of cerebrospinal fluid pharmacokinetics to predict brain target concentrations in the clinical setting: implications of the barriers between blood and brain. Clin Pharmacokinet 2002;41:691-703
  • van de Waterbeemd H, Smith DA, Beaumont K, Property-based design:? optimization of drug absorption and pharmacokinetics. J Med Chem 2001;44:1313-33
  • Clark DE. In silico prediction of blood-brain barrier permeation. Drug Discov Today 2003;8:927-33
  • Hagenbuch B, Meier PJ. Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties. Pflugers Arch 2004;447:653-65
  • Loscher W, Potschka H. Drug resistance in brain diseases and the role of drug efflux transporters. Nat Rev Neurosci 2005;6:591-602
  • Abbott NJ, Khan EU, Rollinson CMS, Drug resistance in epilepsy: the role of the blood-brain barrier. Novartis Found. Symp 2002;243:38-47; discussion 47-53, 180-5
  • Hermann DM, Bassetti CL. Implications of ATP-binding cassette transporters for brain pharmacotherapies. Trends Pharmacol Sci 2007;28:128-34
  • Spudich A, Kilic E, Xing H, Inhibition of multidrug resistance transporter-1 facilitates neuroprotective therapies after focal cerebral ischemia. Nat Neurosci 2006;9:487-8
  • Kilic E, Spudich A, Kilic U, ABCC1: a gateway for pharmacological compounds to the ischaemic brain. Brain 2008;131:2679-89
  • White BC, Sullivan JM, DeGracia DJ, Brain ischemia and reperfusion: molecular mechanisms of neuronal injury. J Neurol Sci 2000;179:1-33
  • Castellanos M, Serena J. Applicability of biomarkers in ischemic stroke. Cerebrovasc Dis 2007;24:7-15
  • Warach S, Latour LL. Evidence of reperfusion injury, exacerbated by thrombolytic therapy, in human focal brain ischemia using a novel imaging marker of early blood-brain barrier disruption. Stroke 2004;35:2659-61
  • The National Institute of Neurological Disorders and Stroke rt-PA Stroke Study Group. Tissue plasminogen activator for acute ischemic stroke. The National Institute of Neurological Disorders and Stroke rt-PA Stroke Study Group. N Engl J Med 1995;333:1581-7
  • Rha J, Saver JL. The impact of recanalization on ischemic stroke outcome. A meta-analysis. Stroke 2007, doi:10.1161/01.STR.0000258112.14918.24
  • Latour LL, Kang D, Ezzeddine MA, Early blood-brain barrier disruption in human focal brain ischemia. Ann Neurol 2004;56:468-77
  • Simard JM, Kent TA, Chen M, Brain oedema in focal ischaemia: molecular pathophysiology and theoretical implications. Lancet Neurol 2007;6:258-68
  • Batra A, Latour LL, Ruetzler CA, Increased plasma and tissue MMP levels are associated with BCSFB and BBB disruption evident on post-contrast FLAIR after experimental stroke. J Cereb Blood Flow Metab 2010;30:1188-99
  • Chen B, Friedman B, Cheng Q, Severe blood-brain barrier disruption and surrounding tissue injury. Stroke 2009;40:e666-74
  • Jin R, Yang G, Li G. Molecular insights and therapeutic targets for blood-brain barrier disruption in ischemic stroke: critical role of matrix metalloproteinases and tissue-type plasminogen activator. Neurobiol Dis 2010;38:376-85
  • Huang P, Chen C, Yang Y, Eligibility for Recombinant tissue plasminogen activator in acute ischemic stroke. Cerebrovasc Dis 2006;22:423-8
  • Pillai DR, Dittmar MS, Baldaranov D, Cerebral ischemia-reperfusion injury in rats[mdash]A 3 T MRI study on biphasic blood-brain barrier opening and the dynamics of edema formation. J Cereb Blood Flow Metab 2009;29:1846-55
  • Durukan A, Marinkovic I, Strbian D, Post-ischemic blood-brain barrier leakage in rats: one-week follow-up by MRI. Brain Res 2009;1280:158-65
  • Strbian D, Durukan A, Pitkonen M, The blood-brain barrier is continuously open for several weeks following transient focal cerebral ischemia. Neuroscience 2008;153:175-81
  • McColl BW, Rothwell NJ, Allan SM. Systemic Inflammation alters the kinetics of cerebrovascular tight junction disruption after experimental stroke in mice. J Neurosci 2008;28:9451-62
  • Vo KD, Santiago F, Lin W, MR Imaging enhancement patterns as predictors of hemorrhagic transformation in acute ischemic stroke. AJNR Am J Neuroradiol 2003;24:674-9
  • Vries HED, Kuiper J, Boer AGD, The blood-brain barrier in neuroinflammatory diseases. Pharmacol Rev 1997;49:143-56
  • Kidwell CS, Latour L, Saver JL, Thrombolytic toxicity: blood brain barrier disruption in human ischemic stroke. Cerebrovasc Dis 2008;25:338-43
  • Farrall AJ, Wardlaw JM. Blood-brain barrier: Ageing and microvascular disease - systematic review and meta-analysis. Neurobiol Aging 2009;30:337-52
  • Ohtsuki S, Terasaki T. Contribution of carrier-mediated transport systems to the blood–brain barrier as a supporting and protecting interface for the brain; importance for CNS drug discovery and development. Pharm Res 2007;24:1745-58
  • Katoh M, Suzuyama N, Takeuchi T, Kinetic analyses for species differences in P-glycoprotein-mediated drug transport. J Pharm Sci 2006;95:2673-83
  • Savitz SI. A critical appraisal of the NXY-059 neuroprotection studies for acute stroke: a need for more rigorous testing of neuroprotective agents in animal models of stroke. Exp Neurol 2007;205:20-5
  • Shen DD, Artru AA, Adkison KK. Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacodynamics. Adv Drug Deliv Rev 2004;56:1825-57
  • Ungerstedt U, Pycock C. Functional correlates of dopamine neurotransmission. Bull Schweiz Akad Med Wiss 1974;30:44-55
  • Elmquist WF, Sawchuk RJ. Application of microdialysis in pharmacokinetic studies. Pharm Res 1997;14:267-88
  • Dahlin AP, Wetterhall M, Caldwell KD, Methodological aspects on microdialysis protein sampling and quantification in biological fluids: an in vitro study on human ventricular CSF. Anal Chem 2010;82:4376-85
  • Helmy A, Carpenter KLH, Skepper JN, Microdialysis of cytokines: methodological considerations, scanning electron microscopy, and determination of relative recovery [Internet]. 2009, [no volume]
  • Liu X, Van Natta K, Yeo H, Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid. Drug Metab Dispos 2009;37:787-93
  • Rosso L, Brock CS, Gallo JM, A new model for prediction of drug distribution in tumor and normal tissues: pharmacokinetics of temozolomide in glioma patients. Cancer Res 2009;69:120-7
  • Keller M, Montgomery S, Ball W, Lack of efficacy of the substance P (Neurokinin1 Receptor) antagonist aprepitant in the treatment of major depressive disorder. Biol Psychiatry 2006;59:216-23
  • Cawthorne C, Prenant C, Smigova A, Biodistribution, pharmacokinetics and metabolism of interleukin-1 receptor antagonist (IL-1RA) using [(18)F]-IL1RA and PET imaging in rats [Internet]. Br J Pharmacol 2010, doi:10.1111/j.1476-5381.2010.01068.x
  • Aboagye EO, Price PM, Jones T. In vivo pharmacokinetics and pharmacodynamics in drug development using positron-emission tomography. Drug Discov Today 2001;6:293-302
  • Christensen JD, Yurgelun-Todd DA, Babb SM, Measurement of human brain dexfenfluramine concentration by 19F magnetic resonance spectroscopy. Brain Res 1999;834:1-5
  • Schenck JF. Physical interactions of static magnetic fields with living tissues. Prog Biophys Mol Biol 2004;87:185-204
  • Bolo NR, Hode Y, Nedelec J, brain pharmacokinetics and tissue distribution in vivo of fluvoxamine and fluoxetine by fluorine magnetic resonance spectroscopy. Neuropsychopharmacology 2000;23:428-38
  • Lyoo IK, Renshaw PF. Magnetic resonance spectroscopy: current and future applications in psychiatric research. Biol Psychiatry 2002;51:195-207
  • Mire-Sluis A, Gaines Das R, Padilla A. WHO cytokine standardization: facilitating the development of cytokines in research, diagnosis and as therapeutic agents. J Immunol Methods 1998;216:103-16
  • Chirmule N, Oyaizu N, Kalyanaraman VS, Misinterpretation of results of cytokine bioassays. J Immunol Methods 1991;137:141-4
  • De Jongh R, Vranken J, Vundelinckx G, The effects of anticoagulation and processing on assays of il-6, sil-6r, sil-2r and soluble transferrin receptor. Cytokine 1997;9:696-701
  • Hoffmann JN, Hartl WH, Faist E, Tumor necrosis factor measurement and use of different anticoagulants: Possible interference in plasma samples and supernatants from endotoxin-stimulated monocytes. Inflamm Res 1997;46:342-7
  • Morgan EH, Peters T. The biosynthesis of rat serum albumin. J Biol Chem 1971;246:3500-7
  • Wilkes MM, Navickis RJ. Patient survival after human albumin administration. Ann Intern Med 2001;135:149-64
  • SAFE Study investigators: effect of baseline serum albumin concentration on outcome of resuscitation with albumin or saline in patients in intensive care units: analysis of data from the saline versus albumin fluid evaluation (SAFE) study. BMJ 2006;333:1044
  • Fleischmann RM, Tesser J, Schiff MH, Safety of extended treatment with anakinra in patients with rheumatoid arthritis. Ann Rheum Dis 2006;65:1006-12
  • Kricka LJ. Human anti-animal antibody interferences in immunological assays. Clin Chem 1999;45:942-56
  • Aarons L. Physiologically based pharmacokinetic modelling: a sound mechanistic basis is needed. Br J Clin Pharmacol 2005;60:581-3
  • Balant LP, Gex-Fabry M. Modelling during drug development. Eur J Pharm Biopharm 2000;50:13-26
  • Nestorov I. Whole body pharmacokinetic models. Clin Pharmacokinet 2003;42:883-908
  • Aarons L. Population pharmacokinetics: theory and practice. Br J Clin Pharmacol 1991;32:669-70
  • Vozeh S, Steimer JL, Rowland M, The use of population pharmacokinetics in drug development. Clin Pharmacokinet 1996;30:81-93
  • Bellissant E, Sebille V, Paintaud G. Methodological issues in pharmacokinetic-pharmacodynamic modelling. Clin Pharmacokinet 1998;35:151-66
  • Holford N, Ma SC, Ploeger BA. Clinical trial simulation: a review. Clin Pharmacol Ther 2010;88:166-82
  • FDA: Innovation or stagnation: challenge and opportunity on the critical path to new medical products. 2004, [no volume]
  • Barrett JS, Fossler MJ, Cadieu KD, Pharmacometrics: a multidisciplinary field to facilitate critical thinking in drug development and translational research settings. J Clin Pharmacol 2008;48:632-49
  • Gueorguieva I, Clark SR, McMahon CJ, Pharmacokinetic modelling of interleukin-1 receptor antagonist in plasma and cerebrospinal fluid of patients following subarachnoid haemorrhage. Br J Clin Pharmacol 2008;65:317-25
  • Gueorguieva I, Ogungbenro K, Graham G, A program for individual and population optimal design for univariate and multivariate response pharmacokinetic-pharmacodynamic models. Comput Methods Programs Biomed 2007;86:51-61
  • Denes A, Thornton P, Rothwell N, Inflammation and brain injury: acute cerebral ischaemia, peripheral and central inflammation. Brain Behav Immun 2010;24:708-23

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.