Genomes and Genes
Summary: Dynamic and kinetic mechanisms of exogenous chemical and drug ABSORPTION; BIOLOGICAL TRANSPORT; TISSUE DISTRIBUTION; BIOTRANSFORMATION; elimination; and TOXICOLOGY as a function of dosage, and rate of METABOLISM. It includes toxicokinetics, the pharmacokinetic mechanism of the toxic effects of a substance. ADME and ADMET are short-hand abbreviations for absorption, distribution, metabolism, elimination and toxicology.
Publications242 found, 100 shown here
- Opsonization, biodistribution, and pharmacokinetics of polymeric nanoparticlesDonald E Owens
Department of Chemical Engineering, University of Texas at Austin, 1 University Station, C0400, Austin, TX 78712, USA
Int J Pharm 307:93-102. 2006..This method creates a hydrophilic protective layer around the nanoparticles that is able to repel the absorption of opsonin proteins via steric repulsion forces, thereby blocking and delaying the first step in the opsonization process...
- Stealth liposomes and long circulating nanoparticles: critical issues in pharmacokinetics, opsonization and protein-binding propertiesS M Moghimi
Molecular Targeting and Polymer Toxicology Group, School of Pharmacy and Biomolecular Sciences, University of Brighton, BN2 4GJ, Brighton, UK
Prog Lipid Res 42:463-78. 2003..For example, stimulated or newly recruited macrophages can recognize and rapidly internalize sterically protected nanoparticles by opsonic-independent mechanisms. These concepts are also examined...
- Pharmacokinetics and biodistribution of nanoparticlesShyh Dar Li
School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA
Mol Pharm 5:496-504. 2008..The pharmacokinetics (PK) and tissue distribution of the nanoparticles largely define their therapeutic effect and toxicity...
- Pharmacokinetics of subcutaneous immunoglobulin and their use in dosing of replacement therapy in patients with primary immunodeficienciesMelvin Berger
Immunology Research and Development, CSL Behring, King of Prussia, PA 19406 0901, USA
Clin Immunol 139:133-41. 2011Bioavailability and pharmacokinetics of subcutaneous IgG (SCIG) and intravenous IgG (IVIG) differ. It is not clear if and/or how the dose should be adjusted when switching from IVIG to SCIG...
- Pregnancy-induced changes in pharmacokinetics: a mechanistic-based approachGail D Anderson
Department of Pharmacy, University of Washington, Seattle, Washington 98195, USA
Clin Pharmacokinet 44:989-1008. 2005..This same method can also be used to improve our understanding regarding the effect of pregnancy on pharmacokinetics of drugs. Limited studies suggest bioavailability of drugs is not altered during pregnancy...
- An integrated metabolomics and pharmacokinetics strategy for multi-component drugs evaluationKe Lan
Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Sichuan 610041, PR China
Curr Drug Metab 11:105-14. 2010..The pharmacokinetics (PK) of multi-component therapeutics is a great technical challenge, which has led to significant limitations ..
- Age-related changes in pharmacokinetics and pharmacodynamics: basic principles and practical applicationsA A Mangoni
Department of Health Care of the Elderly, Guy s, King s, and St Thomas School of Medicine, King s College London, London
Br J Clin Pharmacol 57:6-14. 2004..This review focuses on the main age-related physiological changes affecting different organ systems and their implications for pharmacokinetics and pharmacodynamics of drugs.
- Development of a physiology-based whole-body population model for assessing the influence of individual variability on the pharmacokinetics of drugsStefan Willmann
Bayer Technology Services GmbH, Process Technology Systems Biology, Building E41, D 51368 Leverkusen, Germany
J Pharmacokinet Pharmacodyn 34:401-31. 2007..the new population model is well suited to assess the influence of individual physiological variability on the pharmacokinetics of drugs. It is expected that this new tool can be beneficially applied in the planning of clinical studies.
- Sex differences in pharmacokinetics and pharmacodynamicsMonica Gandhi
Division of Infectious Diseases, Department of Medicine, University of California San Francisco, San Francisco, California 94143 1352, USA
Annu Rev Pharmacol Toxicol 44:499-523. 2004..This review examines the biologic basis of differences in pharmacokinetics and pharmacodynamics between the sexes and summarizes studies that have addressed these differences...
- Update on the pharmacokinetics and redox properties of protein-bound uremic toxinsHiroshi Watanabe
Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto 862 0973, Japan
J Pharm Sci 100:3682-95. 2011..In this review, we summarized the recent works providing the new insight on the pharmacokinetics and redox properties of these uremic toxins...
- INDI: a computational framework for inferring drug interactions and their associated recommendationsAssaf Gottlieb
The Blavatnik School of Computer Science, Tel Aviv University, Tel Aviv, Israel
Mol Syst Biol 8:592. 2012..Most computational inference methods focus on modeling drug pharmacokinetics, aiming at interactions that result from a common metabolizing enzyme (CYP)...
- CSF as a surrogate for assessing CNS exposure: an industrial perspectiveJiunn H Lin
Department of Preclinical Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania, USA
Curr Drug Metab 9:46-59. 2008..Depending on the physicochemical properties of drugs and the site/timing of CSF sampling, the unbound drug concentration at the biophase within the brain could differ significantly from the corresponding CSF drug concentration...
- Sulfur mustard toxicity: history, chemistry, pharmacokinetics, and pharmacodynamicsKamyar Ghabili
Tuberculosis and Lung Disease Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
Crit Rev Toxicol 41:384-403. 2011..in 1917, SM and other mustard agents have been the subjects of intensive research, and their chemistry, pharmacokinetics and mechanisms of toxic action are now fairly well understood...
- Preclinical prediction of human brain target site concentrations: considerations in extrapolating to the clinical settingJoost Westerhout
Department of Pharmacology, Leiden Amsterdam Center for Drug Research, Leiden University, 2300 RA Leiden, The Netherlands
J Pharm Sci 100:3577-93. 2011..g., inhibition of an efflux transporter or induction of pathological state). With the use of advanced mathematical modeling procedures, we may dissect contributions of individual mechanisms in animals as links to the human situation...
- Population pharmacokinetics III: design, analysis, and application of population pharmacokinetic StudiesEne I Ette
Vertex Pharmaceuticals, Inc, 130 Waverly St, Cambridge, MA 02139 4242, USA
Ann Pharmacother 38:2136-44. 2004..To present a framework within which population pharmacokinetic (PPK) studies should be designed and analyzed and discuss the application of developed PPK models...
- PK/PD modelling and beyond: impact on drug developmentDouwe D Breimer
Leiden Amsterdam Center for Drug Research, Leiden University, Leiden, The Netherlands
Pharm Res 25:2720-2. 2008..This will give rise to new opportunities of drug combinations, which can only be developed rationally through the appropriate application of dynamical systems-based PK/PD models...
- Predicting drug-drug interactions: an FDA perspectiveLei Zhang
Office of Clinical Pharmacology, Office of Translational Sciences, Center for Drug Evaluation and Research, Food and Drug Administration, Rm 3188, Bldg 51, 10903 New Hampshire Avenue, Silver Spring, Maryland 20993, USA
AAPS J 11:300-6. 2009..This report summarizes critical elements in the in vitro evaluation of drug interaction potential during drug development and uses a case study to highlight the impact of in vitro information on drug labeling...
- The dynamics of drug action on the within-host population growth of infectious agents: melding pharmacokinetics with pathogen population dynamicsD J Austin
Wellcome Trust Centre for the Epidemiology of Infectious Diseases, University of Oxford, South Parks Road, Oxford, OX1 3PS, U K
J Theor Biol 194:313-39. 1998..Under chemotherapeutic regimens, expressions for R0 are derived allowing estimates to be made of the ideal treatment regime required to eliminate the pathogen, both for HIV and P. falciparum malaria...
- Imaging the function of P-glycoprotein with radiotracers: pharmacokinetics and in vivo applicationsP Kannan
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
Clin Pharmacol Ther 86:368-77. 2009P-glycoprotein (P-gp), an efflux transporter, controls the pharmacokinetics of various compounds under physiological conditions...
- Population pharmacokinetics II: estimation methodsEne I Ette
Vertex Pharmaceuticals, Inc, Cambridge, MA, USA
Ann Pharmacother 38:1907-15. 2004....
- Impact of OATP transporters on pharmacokineticsA Kalliokoski
Department of Clinical Pharmacology, University of Helsinki, Helsinki, Finland
Br J Pharmacol 158:693-705. 2009..polypeptides (OATP) form a family of influx transporters expressed in various tissues important for pharmacokinetics. Of the 11 human OATP transporters, OATP1B1, OATP1B3 and OATP2B1 are expressed on the sinusoidal membrane of ..
- Role of P-glycoprotein in pharmacokinetics: clinical implicationsJiunn H Lin
Department of Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
Clin Pharmacokinet 42:59-98. 2003..Because of its importance in pharmacokinetics, P-glycoprotein transport screening has been incorporated into the drug discovery process, aided by the ..
- Pharmacokinetics and tolerability of a new intravenous immunoglobulin preparation, IGIV-C, 10% (Gamunex, 10%)M Ballow
Division of Allergy Immunology and Pediatric Rheumatologym Kaleida Hralth at The Children s Hospital of Buffalo SUNY Buffalo, Department of Pediatrics, Buffalo, New York 14222, USA
Vox Sang 84:202-10. 2003..Two clinical studies were conducted to compare the pharmacokinetics of the new product, IGIV-C, 10% (Gamunex, 10%), formulated with glycine, with the licensed solvent-detergent (..
- Role of red blood cells in pharmacokinetics of chemotherapeutic agentsDirk Schrijvers
Department of Medical Oncology, AZ Middelheim, Antwerp, Belgium
Clin Pharmacokinet 42:779-91. 2003..The erythrocyte concentration of mercaptopurine has a prognostic value in the treatment of childhood acute lymphoblastic leukemia. In this review, the role of red blood cells for various anticancer drugs is further discussed...
- Clinical relevance of pharmacokinetics and pharmacodynamics in cardiac critical care patientsFederico Pea
Institute of Clinical Pharmacology and Toxicology, Department of Experimental and Clinical Pathology and Medicine, Medical School, University of Udine, Udine, Italy
Clin Pharmacokinet 47:449-62. 2008b>Pharmacokinetics is a discipline aimed at predicting the best dosage and dosing regimen for each single drug in order to ensure and maintain therapeutically effective concentrations at the action sites...
- Pharmacokinetics and its role in small molecule drug discovery researchG R Jang
Department of Pharmacokinetics and Drug Metabolism, Amgen Inc, Thousand Oaks, California 91320-1799, USA
Med Res Rev 21:382-96. 2001b>Pharmacokinetics (PK), which describes the disposition of a drug in the body, should be a primary consideration in the selection of a drug candidate, ultimately contributing to its eventual clinical success or failure...
- Conditional weighted residuals (CWRES): a model diagnostic for the FOCE methodAndrew C Hooker
Division of Pharmacokinetics and Drug Therapy, Dept of Pharmaceutical Biosciences, Faculty of Pharmacy, Uppsala University, Box 591, 751 24, Uppsala, Sweden
Pharm Res 24:2187-97. 2007..Utilizing WRES with the FOCE method may lead to misguided model development/evaluation. We present a new diagnostic tool, the conditional weighted residuals (CWRES), which are calculated based on the FOCE approximation...
- Assessment of actual significance levels for covariate effects in NONMEMU Wählby
Division of Pharmacokinetics and Drug Therapy, Department of Pharmaceutical Biosciences, Uppsala University, Box 591, 751 24 Uppsala, Sweden
J Pharmacokinet Pharmacodyn 28:231-52. 2001..Estimation with FOCE-INTER and the covariate randomization procedure provide means to achieve agreement between nominal and actual significance levels...
- Assessing antibody pharmacokinetics in mice with in vivo imagingJack Hoppin
inviCRO, LLC, 2 Oliver St Suite 611, Boston, MA 02109, USA
J Pharmacol Exp Ther 337:350-8. 2011..Images and analysis results from a case study are presented with a discussion of output data content and relevant informatics gained with this approach to studying antibody pharmacokinetics.
- Physiologically-based pharmacokinetics in drug development and regulatory scienceMalcolm Rowland
Centre for Pharmacokinetic Research, University of Manchester, United Kingdom
Annu Rev Pharmacol Toxicol 51:45-73. 2011..Finally, some attention is given to the positioning of PBPK within the drug development and approval paradigm and its future application in truly personalized medicine...
- ADMET in silico modelling: towards prediction paradise?Han van de Waterbeemd
Pfizer Global Research and Development, PDM, Sandwich, Kent CT13 9NJ, UK
Nat Rev Drug Discov 2:192-204. 2003Following studies in the late 1990s that indicated that poor pharmacokinetics and toxicity were important causes of costly late-stage failures in drug development, it has become widely appreciated that these areas should be considered as ..
- Physiologically based pharmacokinetic modelling 2: predicting the tissue distribution of acids, very weak bases, neutrals and zwitterionsTrudy Rodgers
Centre for Applied Pharmacokinetic Research, School of Pharmacy and Pharmaceutical Sciences, The University of Manchester, England
J Pharm Sci 95:1238-57. 2006..Such advancements in parameter prediction will assist WBPBPK modelling, where time, cost and labour requirements greatly deter its application...
- Physiologically based pharmacokinetics joined with in vitro-in vivo extrapolation of ADME: a marriage under the arch of systems pharmacologyA Rostami-Hodjegan
Centre for Applied Pharmacokinetics Research, School of Pharmacy and Pharmaceutical Sciences, Faculty of Medical and Human Sciences, University of Manchester, Manchester, UK
Clin Pharmacol Ther 92:50-61. 2012Classic pharmacokinetics (PK) rarely takes into account the full knowledge of physiology and biology of the human body. However, physiologically based PK (PBPK) is built mainly from drug-independent "system" information...
- The Simcyp population-based ADME simulatorMasoud Jamei
Modelling and Simulation Group, Simcyp Limited, Blades Enterprise Centre, Sheffield, UK
Expert Opin Drug Metab Toxicol 5:211-23. 2009..This review describes the framework and organisation of the simulator and how it combines the different categories of information...
- Gliadin nanoparticles as carriers for the oral administration of lipophilic drugs. Relationships between bioadhesion and pharmacokineticsM A Arangoa
, , Universidad de Navarra, Pamplona, Spain
Pharm Res 18:1521-7. 2001..These pharmacokinetic modifications were directly related to the bioadhesive capacity of these carriers with the stomach mucosa...
- Steady-State pharmacokinetics and tolerability of trans-resveratrol 2000 mg twice daily with food, quercetin and alcohol (ethanol) in healthy human subjectsCharles la Porte
Ottawa Hospital Research Institute, Ottawa, Ontario K1H 8L6, Canada
Clin Pharmacokinet 49:449-54. 2010..The pharmacokinetics of trans-resveratrol have been investigated in single-dose studies and in studies with relatively low dosages...
- Application of in silico approaches to predicting drug--drug interactionsS Ekins
Lilly Research Laboratories, Lilly Corporate Center, Drop Code 1730, Indianapolis, IN 46285, USA
J Pharmacol Toxicol Methods 45:65-9. 2001..poor absorption, distribution, metabolism, and excretion (ADME), and the related properties of toxicity and pharmacokinetics are responsible for a large proportion of failures...
- Application of allometric principles for the prediction of pharmacokinetics in human and veterinary drug developmentIftekhar Mahmood
Office of Blood Review and Research, Center for Biologic Evaluation and Research, Food and Drug Administration, 1451 Rockville Pike, MD, USA
Adv Drug Deliv Rev 59:1177-92. 2007..Interspecies scaling is also a very useful tool in veterinary medicine. The knowledge of pharmacokinetics in veterinary medicine is important for dosage selection, particularly in the treatment of large animals such ..
- Pharmacokinetic predictions in children by using the physiologically based pharmacokinetic modellingF Bouzom
Technologie Servier, 27 rue Eugene Vignat, BP 11749, 45007 Orléans Cedex 1, France
Fundam Clin Pharmacol 22:579-87. 2008..Physiologically based pharmacokinetics is one way to integrate the physiological changes occurring in the childhood and to anticipate their impact ..
- Tailor-made drug treatment for children: creation of an infrastructure for data-sharing and population PK-PD modelingIbrahim Ince
Department of Pediatric Surgery, Erasmus MC Sophia Children s Hospital, Rotterdam, The Netherlands
Drug Discov Today 14:316-20. 2009..In addition to modeling of drug disposition (PK) pathways, we emphasize the need for modeling of effect (PD) pathways and the use of a multidisciplinary infrastructure for data-sharing...
- When drug therapy gets old: pharmacokinetics and pharmacodynamics in the elderlyKlaus Turnheim
Institut fur Pharmakologie, Universitat Wien, Währinger Str 13a, Vienna A 1090, Austria
Exp Gerontol 38:843-53. 2003..Hence drugs should be used very restrictively in geriatric patients. If drug therapy is absolutely necessary, the dosage should be titrated to a clearly defined clinical or biochemical therapeutic goal starting from a low initial dose...
- Sex differences in pharmacokinetics and pharmacodynamicsOffie P Soldin
Departments of Medicine, Oncology and Physiology, Center for the Study of Sex Differences, Georgetown University Medical Center, Washington, DC, USA
Clin Pharmacokinet 48:143-57. 2009..This review summarizes the sex-based differences that impact on pharmacokinetics, and includes a general comparison of clinical pharmacology as it applies to men, women and pregnant women...
- Prediction of drug clearance in children: impact of allometric exponents, body weight, and ageIftekhar Mahmood
From the Office of Clinical Pharmacology, Center for Drug Evaluation and Research, Food and Drug Administration, Bethesda, Maryland, USA
Ther Drug Monit 29:271-8. 2007..75 should be replaced by the exponent of the allometric equation developed for that drug...
- Physiologically based pharmacokinetics (PBPK)Pascal Espie
UCB Pharma SA, Belgium
Drug Metab Rev 41:391-407. 2009..In addition, by providing a link between tissue concentrations and toxicological or pharmacological effects, PBPK modeling represents a framework for mechanistic pharmacokinetic-pharmacodynamic models...
- Modelling approaches to dose estimation in childrenTrevor N Johnson
Simcyp Ltd, Blades Enterprise Centre, John Street, Sheffield S2 4SU, UK
Br J Clin Pharmacol 59:663-9. 2005..However, following such an exercise, well-conducted PK-PD or PK studies will still be needed to determine the most appropriate doses for neonates, infants, children and adolescents...
- Mechanism-based concepts of size and maturity in pharmacokineticsB J Anderson
Department of Anaesthesiology, University of Auckland School of Medicine, Auckland, New Zealand
Annu Rev Pharmacol Toxicol 48:303-32. 2008..A sigmoid E(max) model (Hill equation) describes gradual maturation of clearance in early life leading to a mature adult clearance achieved at a later age...
- Outcome of an outbreak of acute hepatitis C among healthy volunteers participating in pharmacokinetics studiesAlberto Larghi
Division of Internal Medicine, Department of Medicine, Surgery and Dentistry, Ospedale San Paolo, Italy
Hepatology 36:993-1000. 2002..15 patients with acute hepatitis C (AHC) among 29 healthy volunteers participating in 2 consecutive pharmacokinetics studies...
- Using the time of maximum effect site concentration to combine pharmacokinetics and pharmacodynamicsCharles F Minto
Department of Anaesthesia and Pain Management, Royal North Shore Hospital, Sydney, Australia
Anesthesiology 99:324-33. 2003..The authors propose an alternative methodology to rationally combine the results of separate pharmacokinetic and pharmacodynamic studies, based on t(peak), the time of peak effect after bolus injection...
- Predicting drug disposition, absorption/elimination/transporter interplay and the role of food on drug absorptionJoseph M Custodio
Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, California 94143 0446, USA
Adv Drug Deliv Rev 60:717-33. 2008..That is, high fat meals and lipidic excipients would be expected to have little effect on F for Class 1 drugs; they would increase F of Class 2 drugs, while decreasing F for Class 3 drugs...
- Pharmacokinetics and in vivo drug release rates in liposomal nanocarrier developmentDaryl C Drummond
Hermes Biosciences, Inc, South San Francisco, California 94080, USA
J Pharm Sci 97:4696-740. 2008..is a function not only of the properties of the encapsulated drug, but to a significant extent of the pharmacokinetics, biodistribution, and drug release rates of the individual carrier...
- The influence of sex on pharmacokineticsJanice B Schwartz
Institute on Aging and Jewish Home of San Francisco, and University of California, San Francisco, California 94112, USA
Clin Pharmacokinet 42:107-21. 2003..The relative role of sex on pharmacokinetics as compared to genetics, age, disease, social habits and their potential interactions in the clinical setting ..
- Mechanism-based pharmacokinetic-pharmacodynamic modeling: biophase distribution, receptor theory, and dynamical systems analysisMeindert Danhof
Leiden Amsterdam Center for Drug Research, Division of Pharmacology, Leiden University, 2300 RA Leiden, The Netherlands
Annu Rev Pharmacol Toxicol 47:357-400. 2007..This has yielded models with much-improved properties for extrapolation and prediction. These models constitute a theoretical basis for rational drug discovery and development...
- Challenges and obstacles of ocular pharmacokinetics and drug deliveryArto Urtti
Drug Discovery and Development Technology Center, University of Helsinki, Viikinkaari 5 E, 00014 University of Helsinki, Finland
Adv Drug Deliv Rev 58:1131-5. 2006..Ocular drug delivery is hampered by the barriers protecting the eye. This review presents an overview of the essential factors in ocular pharmacokinetics and selected pharmacological future challenges in ophthalmology.
- Modelling and PBPK simulation in drug discoveryHannah M Jones
Pfizer Global R and D, Department of Pharmacokinetics, Dynamics and Metabolism, IPC 654, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK
AAPS J 11:155-66. 2009..Specific reference is made to its utility (1) at the lead development stage for the prioritization of compounds for animal PK studies and (2) at the clinical candidate selection and "first in human" stages for the prediction of human PK...
- An evaluation of the utility of physiologically based models of pharmacokinetics in early drug discoveryNeil Parrott
F Hoffmann La Roche AG, Pharmaceuticals Division, CH 4070 Bl, Switzerland
J Pharm Sci 94:2327-43. 2005Generic physiologically-based models of pharmacokinetics were evaluated for early drug discovery. Plasma profiles after intravenous and oral dosing were simulated in rat for 68 compounds from six chemical classes...
- Clinical pharmacokinetics and pharmacodynamics of allopurinol and oxypurinolRichard O Day
School of Medical Sciences, Faculty of Medicine, University of New South Wales and Department of Clinical Pharmacology and Toxicology, St Vincent s Hospital, Sydney, New South Wales, Australia
Clin Pharmacokinet 46:623-44. 2007..The net effect is an increased degree of hypouricaemia, but the interaction is probably limited to patients with normal renal function or only moderate impairment...
- Effects of food on clinical pharmacokineticsB N Singh
Department of Pharmacy and Administrative Sciences, College of Pharmacy and Allied Health Professions, St John s University, Jamaica, New York, USA
Clin Pharmacokinet 37:213-55. 1999..A mechanistic understanding of the effects of food may serve as a key to the pharmacokinetic optimisation of patient therapy, both in outpatients and hospitalised patients of various age groups...
- The virtual laboratory approach to pharmacokinetics: design principles and conceptsWilhelm Huisinga
DFG Research Center MATHEON and Freie Universität Berlin, Fachbereich Mathematik und Informatik, Arnimallee 2 6, D 14195 Berlin, Germany
Drug Discov Today 11:800-5. 2006Modeling and simulation in pharmacokinetics has turned into the focus of pharmaceutical companies, driven by the emerging consensus that in silico predictions, combined with in vitro data, have the potential to significantly increase ..
- Drugs in pregnancy. Pharmacokinetics in pregnancyM Dawes
Department of Clinical Pharmacology, St Thomas' Hospital, Lambeth Palace Road, London, SE1 7EH, UK
Best Pract Res Clin Obstet Gynaecol 15:819-26. 2001b>Pharmacokinetics describes the handling of a drug by the body - how the drug is absorbed, distributed and eliminated and how these processes determine plasma concentrations of the drug...
- Role of pharmacogenetics of ATP-binding cassette transporters in the pharmacokinetics of drugsIngolf Cascorbi
Institute of Pharmacology, University Hospital Schleswig Holstein, Hospitalstrasse 4, D 24105 Kiel, Germany
Pharmacol Ther 112:457-73. 2006..variances in the genes of membrane transporters could explain at least in part interindividual differences of pharmacokinetics and clinical outcome of a variety of drugs...
- Can the pharmaceutical industry reduce attrition rates?Ismail Kola
Basic Research at Merck Research Labs, 126 East Lincoln Avenue, Rahway, New Jersey 07075, USA
Nat Rev Drug Discov 3:711-5. 2004
- Development and evaluation of a generic physiologically based pharmacokinetic model for childrenAndrea N Edginton
Competence Center Systems Biology, Bayer Technology Services GmbH, Leverkusen, Germany
Clin Pharmacokinet 45:1013-34. 2006....
- The role of transporters in the pharmacokinetics of orally administered drugsSarah Shugarts
Department of Biopharmaceutical Sciences, University of California, San Francisco, CA 94143 0912, USA
Pharm Res 26:2039-54. 2009....
- Pharmacokinetics of mycophenolic acid in severe lupus nephritisPaungpaga Lertdumrongluk
Renal Division, Lupus Research Unit, Faculty of Medicine, Department of Medicine, Chulalongkorn University, Bangkok, Thailand
Kidney Int 78:389-95. 2010..The dosage of the drug was not related to MPA pharmacokinetics. In the mycophenolate mofetil group, however, MPA-area under the curve was positively, and significantly, ..
- The lasso--a novel method for predictive covariate model building in nonlinear mixed effects modelsJakob Ribbing
Department of Pharmaceutical Biosciences, Division of Pharmacokinetics and Drug Therapy, Uppsala University, Box 591, 75124 Uppsala, Sweden
J Pharmacokinet Pharmacodyn 34:485-517. 2007Covariate models for population pharmacokinetics and pharmacodynamics are often built with a stepwise covariate modelling procedure (SCM)...
- So many studies, too few subjects: establishing functional relevance of genetic polymorphisms on pharmacokineticsJ Andrew Williams
Pfizer Global Research and Development, Department of Pharmacokinetics, Dynamics and Metabolism, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
J Clin Pharmacol 46:258-64. 2006Based on current literature, greater clarity in defining the magnitude of polymorphism effects on pharmacokinetics can be achieved by addressing key components of study design, including adequate subject numbers per study group...
- Integrating in vitro ADMET data through generic physiologically based pharmacokinetic modelsDavid E Leahy
Cyprotex Discovery Limited, Macclesfield, Cheshire, UK
Expert Opin Drug Metab Toxicol 2:619-28. 2006..model, Cloe PK) (Cyprotex), which is parameterised for human and rat physiology, to the estimation of plasma pharmacokinetics, are summarised in this paper...
- Evaluation of bioequivalence of highly variable drugs using clinical trial simulations. II: Comparison of single and multiple-dose trials using AUC and CmaxA A el-Tahtawy
Food and Drug Administration, Center for Drug Evaluation and Research, Rockville, Maryland 20857, USA
Pharm Res 15:98-104. 1998..The main methodology was Monte Carlo simulation, and we also used deterministic simulation, and examination of clinical trials. The results are compared with those previously observed for Cmax (maximum concentration.)..
- Gamma generalized linear models for pharmacokinetic dataRuth Salway
Department of Mathematical Sciences, University of Bath, Bath BA2 7AY, UK
Biometrics 64:620-6. 2008..The methods are applied to data from 12 individuals following administration of the antiasthmatic agent theophylline...
- Uncertainty factors for chemical risk assessment: interspecies differences in the in vivo pharmacokinetics and metabolism of human CYP1A2 substratesK Walton
Clinical Pharmacology Group, Biomedical Sciences Building, University of Southampton, Bassett Crescent East, SO16 7PX, Southampton, UK
Food Chem Toxicol 39:667-80. 2001..This work supports the need to replace the generic default factors by a compound-related value derived from specific, relevant, quantitative data; this would result in more relevant and reliable non-cancer risk assessments...
- Clinical trial simulation: a reviewN Holford
Department of Pharmacology and Clinical Pharmacology, University of Auckland, Auckland, New Zealand
Clin Pharmacol Ther 88:166-82. 2010..This will take advantage of optimizing the experimental design and leave the task of evaluating the probable real-world performance of a limited number of candidate trial designs and analysis procedures...
- Pharmacokinetics of the oral direct renin inhibitor aliskiren alone and in combination with irbesartan in renal impairmentSujata Vaidyanathan
Novartis Pharmaceuticals Corporation, East Hanover, New Jersey, USA
Clin Pharmacokinet 46:661-75. 2007..This study assessed the effects of renal impairment on the pharmacokinetics and safety of aliskiren alone and in combination with the angiotensin receptor antagonist irbesartan.
- Effect of cationic carriers on the pharmacokinetics and tumor localization of nucleic acids after intravenous administrationHolger K de Wolf
Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, PO Box 80082, 3508 TB Utrecht, The Netherlands
Int J Pharm 331:167-75. 2007..Rather, the benefits are arising from carrier-induced changes in the intratumoral fate of the nucleic acids...
- New mathematical methods in pharmacokinetic modelingMaria Durisova
Institute of Experimental Pharmacology, Slovak Academy of Sciences, 841 04 Bratislava 4, Slovak Republic
Basic Clin Pharmacol Toxicol 96:335-42. 2005In recent years, several new methods for the mathematical modeling have gradually emerged in pharmacokinetics, and the development of pharmacokinetic models based on these methods has become one of the most rapidly growing and exciting ..
- Bridging the gap: ageing, pharmacokinetics and pharmacodynamicsDominick G A Burton
School of Pharmacy and Biomolecular Science, University of Brighton, Cockcroft Building, Brighton, BN2 4GJ, UK
J Pharm Pharmacol 57:671-9. 2005Changes in pharmacokinetics and pharmacodynamics in elderly patients generally result in an increase in the incidence of drug toxicity and adverse drug reactions...
- Population pharmacokinetics of oral risperidone in children, adolescents and adults with psychiatric disordersAn Thyssen
Johnson and Johnson Pharmaceutical Research and Development, a division of Janssen Pharmaceutica NV, B 2340 Beerse, Belgium
Clin Pharmacokinet 49:465-78. 2010..The pharmacokinetic profile of risperidone is well documented in adults. In this study, the pharmacokinetics of oral risperidone in children and adolescents were investigated along with population pharmacokinetics in ..
- Impact of genetic polymorphisms in CYP2C9 and CYP2C19 on the pharmacokinetics of clinically used drugsTakeshi Hirota
Department of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
Drug Metab Pharmacokinet 28:28-37. 2013..This review summarizes the currently available important information on this topic...
- Theoretical versus empirical allometry: Facts behind theories and application to pharmacokineticsIftekhar Mahmood
Division of Hematology, Office of Blood Review and Research OBRR, Center for Biologic Evaluation and Research, Food and Drug Administration, Rockville, Maryland, USA
J Pharm Sci 99:2927-33. 2010..enough evidence from experimental data that negate the notion of fixed exponents in biology, physiology, and pharmacokinetics. In short, the notion of a fixed exponent is theoretical and there is no evidence that the exponent of a ..
- Role of population pharmacokinetics in drug development. A pharmaceutical industry perspectiveE Samara
Department of Pharmacokinetics and Biopharmaceutics, Abbott Laboratories, Abbott Park, Illinois, USA
Clin Pharmacokinet 32:294-312. 1997..However, several important issues remain to be resolved (such as the optimal study design, quality of the data and user-friendly software) which could determine the future role of the population approach in drug development...
- Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in ratsWei He
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, People s Republic of China
Int J Nanomedicine 6:521-33. 2011..It is concluded that an oil/water nanoemulsion system with good biocompatibility can be prepared by using food proteins as emulsifiers, allowing better and more rapid absorption of lipophilic drugs...
- Software for population pharmacokinetics and pharmacodynamicsL Aarons
School of Pharmacy and Pharmaceutical Sciences, University of Manchester, England
Clin Pharmacokinet 36:255-64. 1999..Although robustness and reliability are important concerns, they were not addressed in the present review. Most of the programs surveyed are in continual development...
- Applications of population pharmacokinetics in current drug labellingJ Z Duan
Office of Clinical Pharmacology, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, MD, USA
J Clin Pharm Ther 32:57-79. 2007The application of population pharmacokinetics (PopPK) appears increasingly in drug labelling. The current study was to examine the use of PopPK in dose recommendation in drug-product labels.
- Pharmacokinetics and metabolism in early drug discoveryD A Smith
Pfizer Central Research, Department of Drug Metabolism, Sandwich, Kent, CT13 9NJ, UK
Curr Opin Chem Biol 3:373-8. 1999..Through linking of in silico and in vitro methods, considerable progress has recently been made towards this future perspective. Despite this progress, these approaches do not yet replace in vivo methods...
- Chirality and pharmacokinetics: an area of neglected dimensionality?Andrew J Hutt
Department of Pharmacy, King s College London, UK
Drug Metabol Drug Interact 22:79-112. 2007....
- Prescribing medications in pediatrics: concerns regarding FDA approval and pharmacokineticsEmily Novak
Yale University School of Nursing, New Haven, CT, USA
Pediatr Nurs 33:64-70. 2007..a common guideline for prescribing "off-label" in pediatrics, but must be used in combination with multiple respected pediatric resources and with full knowledge of pharmacokinetics in children, particularly in young children.
- Parametric and nonparametric population methods: their comparative performance in analysing a clinical dataset and two Monte Carlo simulation studiesAida Bustad
Laboratory of Applied Pharmacokinetics, USC Keck School of Medicine, Los Angeles, California, USA
Clin Pharmacokinet 45:365-83. 2006....
- Improving predictive modeling in pediatric drug development: pharmacokinetics, pharmacodynamics, and mechanistic modelingWilliam Slikker
Office of Research, National Center for Toxicological Research FDA, 3900 NCTR Road, Jefferson, Arkansas 72079 9502, USA
Ann N Y Acad Sci 1053:505-18. 2005..Disease state, as exemplified by obesity, was addressed as a modifier of drug pharmacokinetics and pharmacodynamics during development...
- Guidelines on paediatric dosing on the basis of developmental physiology and pharmacokinetic considerationsImke H Bartelink
Department of Pharmacy, University Medical Center, Utrecht, The Netherlands
Clin Pharmacokinet 45:1077-97. 2006..The integration of these guidelines, and combining them with pharmacodynamic effects, should be considered and could form a basis for further study...
- ABC multidrug transporters: target for modulation of drug pharmacokinetics and drug-drug interactionsBéatrice Marquez
Pharmacologie Cellulaire et Moléculaire, Louvain Drug Research Institute, Universite Catholique de Louvain, B 1200 Brussels, Belgium
Curr Drug Targets 12:600-20. 2011..All together, these data justify why studying drug active transport should be part of the evaluation of new drugs, as recently recommended by the FDA...
- Pharmacokinetics and physiologically-based pharmacokinetic modeling of nanoparticlesRaymond S H Yang
Quantitative and Computational Toxicology Group, Department of Environmental and Radiological Health Sciences, Colorado State University, Fort Collins, CO 80523, USA
J Nanosci Nanotechnol 10:8482-90. 2010..As toxicology is a continuum of pharmacokinetics and pharmacodynamics, this is a review of recent advances on pharmacokinetics and physiologically-based ..
- Lumping in pharmacokineticsCeline Brochot
INERIS, Institut National de l Environnement Industriel et des Risques, Experimental Toxicology Unit, Parc Alata BP2, 60550 Verneuil en Halatte, France
J Pharmacokinet Pharmacodyn 32:719-36. 2005..presenting the theory, we study, here, through practical examples, the potential of such methods in toxico/pharmacokinetics. As a tutorial, we first simplify a 2-compartment pharmacokinetic model by symbolic lumping...
- Resurgence in the use of physiologically based pharmacokinetic models in pediatric clinical pharmacology: parallel shift in incorporating the knowledge of biological elements and increased applicability to drug development and clinical practiceTrevor N Johnson
Simcyp Limited, Sheffield, UK
Paediatr Anaesth 21:291-301. 2011....
- Information tools for exploratory data analysis in population pharmacokineticsO Petricoul
UPRES EA-3286, Faculty of Pharmacy, Marseille, France
J Pharmacokinet Pharmacodyn 28:577-99. 2001..The rationale for using these indexes is shown using simulated and real data...
- Numerical simulation of local pharmacokinetics of a drug after intravascular delivery with an eluting stentDmitri V Sakharov
Gaubius Laboratory, TNO Prevention and Health, PO Box 2215, 2301 CE Leiden, The Netherlands
J Drug Target 10:507-13. 2002We use mathematical modelling to delineate the influence of two important factors on local pharmacokinetics of a drug delivered via an eluting stent, namely: (1) diffusional resistance of a stent coating, and (2) reversible binding of a ..
- Pharmacokinetics/genotype associations for major cytochrome P450 enzymes in native and first- and third-generation Japanese populations: comparison with Korean, Chinese, and Caucasian populationsS P Myrand
Drug Safety Research and Development, Pfizer Global Research and Development PGRD, Ann Arbor, Michigan, USA
Clin Pharmacol Ther 84:347-61. 2008..We conclude that equivalent plasma drug concentrations and metabolic profiles can be expected for native Japanese, first- and third-generation Japanese, Koreans, and Chinese for compounds handled through these six CYP enzymes...
- Facilitation of drug evaluation in children by population methods and modellingMichel Tod
Department of Pharmacy toxicology, Hopital Cochin Saint Vincent de Paul, Paris, FranceEA 3738, Universite Lyon 1, Universite de Lyon, Lyon, France
Clin Pharmacokinet 47:231-43. 2008The pharmacokinetics and pharmacodynamics of drugs are different in adult and paediatric populations, the latter being particularly heterogeneous...
- Essentials for starting a pediatric clinical study (1): Pharmacokinetics in childrenTsuyoshi Yokoi
Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Kanazawa University, Japan
J Toxicol Sci 34:SP307-12. 2009..function changes drastically by age, drug therapy should be arranged according to the age-related changes in pharmacokinetics of its age...
- Applications of physiologically based absorption models in drug discovery and developmentNeil Parrott
F Hoffmann La Roche Ltd Pharmaceuticals Division, Pharma Research Non Clinical Development, Non Clinical Drug Safety, Basel, Switzerland
Mol Pharm 5:760-75. 2008....
- Pharmacokinetics of high-dose chemotherapyY Nieto
BMT Programs at the University of Colorado, USA
Bone Marrow Transplant 33:259-69. 2004..This variation has been recognized to be due, in part, to the wide variation in the pharmacokinetics (PK) of high-dose chemotherapy (HDC)...
- A framework for assessing inter-individual variability in pharmacokinetics using virtual human populations and integrating general knowledge of physical chemistry, biology, anatomy, physiology and genetics: A tale of 'bottom-up' vs 'top-down' recognition Masoud Jamei
Simcyp Limited, Sheffield, UK
Drug Metab Pharmacokinet 24:53-75. 2009..of the drive to decrease this failure rate in drug development involves attempts to use physiologically-based pharmacokinetics 'bottom-up' modeling and simulation to optimize molecular features with respect to the absorption, ..
- Pharmacokinetics and pharmacodynamics of plerixafor in patients with non-Hodgkin lymphoma and multiple myelomaDouglas A Stewart
Department of Oncology and Medicine, Tom Baker Cancer Centre, Calgary, Alberta, Canada
Biol Blood Marrow Transplant 15:39-46. 2009..Plerixafor was safe and effective in mobilizing CD34(+) cells for transplantation...
- PHARMACODYNAMICS OF AGENTS FOR BLADDER CANCER THERAPYJESSIE AU; Fiscal Year: 2003This competitive renewal application is to define the pharmacokinetics and pharmacodynamics of the drugs commonly used in intravesical therapy, in order to optimize the treatment regimen...
- Molecular mechanism of antiangiogenic properties of gold nanoparticlePriyabrata Mukherjee; Fiscal Year: 2010..Also to determine the toxicity, pharmacokinetics, metabolism of AuNP and finally test its efficacy as anti-angiogenic agent to inhibit tumor growth and ..
- Localized modulation of RPE P-gp/MRP activity for back-of-the-eye drug deliverySoumyajit Majumdar; Fiscal Year: 2007..efflux proteins, P- gp and/or MRP, expressed on the retinal pigmented epithelium (RPE), and thus alter ocular pharmacokinetics of systemically/intravitreally co-administered substrates...
- Azithromycin to prevent BPD in Ureaplasma-infected Preterms: Single Dose PK studyRose Viscardi; Fiscal Year: 2007..Currently, the pharmacokinetics, safety, and biologic effects of azithromycin in the preterm population are unknown...
- Drug Interactions and Bioavailability of CranberryJennifer Donovan; Fiscal Year: 2005..aims of this research are 1) to evaluate the potential for CB-drug interactions and 2) to determine the pharmacokinetics and renal clearance of four major CB flavonoids...
- Multivalent Vaccine for Opiate AddictionPaul R Pentel; Fiscal Year: 2010..Vaccines which alter drug pharmacokinetics have shown substantial preclinical and preliminary clinical evidence of efficacy for nicotine and cocaine ..
- Movement-Responsive Cage for Simultaneous Pharmacology Studies in MiniPigsDouglas Mann; Fiscal Year: 2007..cytochrome P450 enzymes are so homologous that pigs should be the preferred model for drug metabolism and pharmacokinetics studies. Yet, pigs are under-utilized...
- K777 for treatment of Chagas Disease: IND-enabling Studies and IND SubmissionSHING CHANG; Fiscal Year: 2010..IND) application, the First in Man Phase I dose escalation clinical trial to assess safety, tolerability and pharmacokinetics after a single oral dose will be conducted in the United States in healthy volunteers...
- Investigating the Role of Adipocytes on Leukemia RelapseSTEVEN DAVID MITTELMAN; Fiscal Year: 2010..Alternatively, it may be an effect of obesity to confound the leukemia treatment, possibly due to altered pharmacokinetics of chemotherapeutic agents...
- Pilot Trial of Bumetanide for Neonatal SeizuresJANET SUSAN SOUL; Fiscal Year: 2010..2) Evaluate the pharmacokinetics and safety of bumetanide (BTN) in newborns with refractory seizures caused by HIE in a Phase I Trial...