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Meeting the Challenge of Predicting Hepatic Clearance of Compounds Slowly Metabolized by Cytochrome P450 Using a Novel Hepatocyte Model, HepatoPac
Tom S. Chan et al.
DRUG METABOLISM AND DISPOSITION (2013)
Toxicity ranking of heavy metals with screening method using adult Caenorhabditis elegans and propidium iodide replicates toxicity ranking in rat
Piper Reid Hunt et al.
FOOD AND CHEMICAL TOXICOLOGY (2012)
Comparative assessment of In Vitro-In Vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs
Patrick Poulin et al.
JOURNAL OF PHARMACEUTICAL SCIENCES (2012)
Evaluation of hepatic clearance prediction using in vitro data: Emphasis on fraction unbound in plasma and drug ionisation using a database of 107 drugs
David Hallifax et al.
JOURNAL OF PHARMACEUTICAL SCIENCES (2012)
In vitro-in vivo extrapolation of clearance: Modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing calculation methods
Patrick Poulin et al.
JOURNAL OF PHARMACEUTICAL SCIENCES (2012)
Translatability scoring in drug development: eight case studies
Alexandra Wendler et al.
JOURNAL OF TRANSLATIONAL MEDICINE (2012)
Characterization of Organic Anion Transporting Polypeptide (OATP) Expression and Its Functional Contribution to the Uptake of Substrates in Human Hepatocytes
Emi Kimoto et al.
MOLECULAR PHARMACEUTICS (2012)
Novel In Vitro-In Vivo Extrapolation (IVIVE) Method to Predict Hepatic Organ Clearance in Rat
Ken-ichi Umehara et al.
PHARMACEUTICAL RESEARCH (2012)
Effects of N1-methylnicotinamide on oxidative and glycooxidative stress markers in rats with streptozotocin-induced diabetes mellitus
Zuzana Orszaghova et al.
REDOX REPORT (2012)
Zebrafish embryos as an alternative to animal experiments-A commentary on the definition of the onset of protected life stages in animal welfare regulations
Uwe Straehle et al.
REPRODUCTIVE TOXICOLOGY (2012)
A Novel Relay Method for Determining Low-Clearance Values
Li Di et al.
DRUG METABOLISM AND DISPOSITION (2012)
Use of Mechanistic Modeling to Assess Interindividual Variability and Interspecies Differences in Active Uptake in Human and Rat Hepatocytes
Karelle Menochet et al.
DRUG METABOLISM AND DISPOSITION (2012)
An Investigation of the Bioactivation Potential and Metabolism Profile of Zebrafish versus Human
Hui Ting Chng et al.
JOURNAL OF BIOMOLECULAR SCREENING (2012)
Mechanistic Pharmacokinetic Modeling for the Prediction of Transporter-Mediated Disposition in Humans from Sandwich Culture Human Hepatocyte Data
Hannah M. Jones et al.
DRUG METABOLISM AND DISPOSITION (2012)
Simultaneous Assessment of Uptake and Metabolism in Rat Hepatocytes: A Comprehensive Mechanistic Model
Karelle Menochet et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2012)
Characterization of In Vitro Glucuronidation Clearance of a Range of Drugs in Human Kidney Microsomes: Comparison with Liver and Intestinal Glucuronidation and Impact of Albumin
Katherine L. Gill et al.
DRUG METABOLISM AND DISPOSITION (2012)
The reconstituted 'humanized liver' in TK-NOG mice is mature and functional
Masami Hasegawa et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2011)
Kinetic Characterization of Rat Hepatic Uptake of 16 Actively Transported Drugs
Yoshiyuki Yabe et al.
DRUG METABOLISM AND DISPOSITION (2011)
Substitute of animals in drug research: An approach towards fulfillment of 4R′s
KK Sharma et al.
INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES (2011)
The Corrected Traditional Equations for Calculation of Hepatic Clearance that Account for the Difference in Drug Ionization in Extracellular and Intracellular Tissue Water and the Corresponding Corrected PBPK Equation
Leonid M. Berezhkovskiy
JOURNAL OF PHARMACEUTICAL SCIENCES (2011)
Study on possible mechanism of orotic acid-induced fatty liver in rats
Yu-Ming Wang et al.
NUTRITION (2011)
Human Disease Models in Drosophila melanogaster and the Role of the Fly in Therapeutic Drug Discovery
Udai Bhan Pandey et al.
PHARMACOLOGICAL REVIEWS (2011)
Identification and developmental expression of the full complement of Cytochrome P450 genes in Zebrafish
Jared V. Goldstone et al.
BMC GENOMICS (2010)
Application of In Vivo Animal Models to Characterize the Pharmacokinetic and Pharmacodynamic Properties of Drug Candidates in Discovery Settings
Benny M. Amore et al.
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING (2010)
Investigation of the Rate-Determining Process in the Hepatic Elimination of HMG-CoA Reductase Inhibitors in Rats and Humans
Takao Watanabe et al.
DRUG METABOLISM AND DISPOSITION (2010)
Assessment of a Micropatterned Hepatocyte Coculture System to Generate Major Human Excretory and Circulating Drug Metabolites
Wendy WeiWei Wang et al.
DRUG METABOLISM AND DISPOSITION (2010)
Network Analysis of Primary Hepatocyte Dedifferentiation Using a Shotgun Proteomics Approach
Cliff Rowe et al.
JOURNAL OF PROTEOME RESEARCH (2010)
Males still dominate animal studies
Irving Zucker et al.
NATURE (2010)
Prediction of Human Metabolic Clearance from In Vitro Systems: Retrospective Analysis and Prospective View
David Hallifax et al.
PHARMACEUTICAL RESEARCH (2010)
A high-throughput method for assessing chemical toxicity using a Caenorhabditis elegans reproduction assay
Windy A. Boyd et al.
TOXICOLOGY AND APPLIED PHARMACOLOGY (2010)
Optimising in vivo pharmacology studies-Practical PKPD considerations
Johan Gabrielsson et al.
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS (2010)
Can Animal Models of Disease Reliably Inform Human Studies?
H. Bart van der Worp et al.
PLOS MEDICINE (2010)
Prediction of Hepatic Clearance in Human From In Vitro Data for Successful Drug Development
Masato Chiba et al.
AAPS JOURNAL (2009)
Predicting Circulating Human Metabolites: How Good Are We?
Shelby Anderson et al.
CHEMICAL RESEARCH IN TOXICOLOGY (2009)
Assessment of Three Human in Vitro Systems in the Generation of Major Human Excretory and Circulating Metabolites
Deepak Dalvie et al.
CHEMICAL RESEARCH IN TOXICOLOGY (2009)
Methodological Uncertainty in Quantitative Prediction of Human Hepatic Clearance from In Vitro Experimental Systems
D. Hallifax et al.
CURRENT DRUG METABOLISM (2009)
Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds: strategic considerations
Johan Gabrielsson et al.
DRUG DISCOVERY TODAY (2009)
Prediction of Drug Clearance by Glucuronidation from in Vitro Data: Use of Combined Cytochrome P450 and UDP-Glucuronosyltransferase Cofactors in Alamethicin-Activated Human Liver Microsomes
Peter J. Kilford et al.
DRUG METABOLISM AND DISPOSITION (2009)
Liver tissue engineering in the evaluation of drug safety
Ajit Dash et al.
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2009)
Physiologically Based Pharmacokinetic Modeling to Predict Transporter-Mediated Clearance and Distribution of Pravastatin in Humans
Takao Watanabe et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2009)
Quantitative Pharmacology or Pharmacokinetic Pharmacodynamic Integration Should Be a Vital Component in Integrative Pharmacology
J. Gabrielsson et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2009)
Survey of the Quality of Experimental Design, Statistical Analysis and Reporting of Research Using Animals
Carol Kilkenny et al.
PLOS ONE (2009)
Characterization of Drosophila melanogaster cytochrome P450 genes
Henry Chung et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2009)
Comparison of intrinsic metabolic clearance in fresh and cryopreserved human hepatocytes
E. Floby et al.
XENOBIOTICA (2009)
Pharmacokinetic and pharmacodynamic data to be derived from early-phase drug development - Designing informative human pharmacology studies
Adam Cohen
CLINICAL PHARMACOKINETICS (2008)
Zebrafish: a predictive model for assessing drug-induced toxicity
Patricia McGrath et al.
DRUG DISCOVERY TODAY (2008)
The Albumin Effect and drug glucuronidation: Bovine serum albumin and fatty acid-free human serum albumin enhance the glucuronidation of UDP-glucuronosyltransferase (UGT) 1A9 substrates but not UGT1A1 and UGT1A6 activities
Andrew Rowland et al.
DRUG METABOLISM AND DISPOSITION (2008)
Reliability of human cryopreserved hepatocytes and liver microsomes as in vitro systems to predict metabolic clearance
R. Stringer et al.
XENOBIOTICA (2008)
Zebrafish based assays for the assessment of cardiac, visual and gut function — potential safety screens for early drug discovery
Stéphane Berghmans et al.
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS (2008)
Microscale culture of human liver cells for drug development
Salman R. Khetani et al.
NATURE BIOTECHNOLOGY (2008)
Rodent models of partial hepatectomies
Paulo N. A. Martins et al.
LIVER INTERNATIONAL (2008)
In vitro-in vivo extrapolation of hepatic clearance:: Biological tools, scaling factors, model assumptions and correct concentrations
O. Pelkonen et al.
XENOBIOTICA (2007)
Use of hepatocytes to assess the contribution of hepatic uptake to clearance in vivo
Matthew G. Soars et al.
DRUG METABOLISM AND DISPOSITION (2007)
Binding of inhibitory fatty acids is responsible for the enhancement of UDP-glucuronosyltransferase 2B7 activity by albumin: Implications for in vitro-in vivo extrapolation
Andrew Rowland et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2007)
Evaluation of cryopreserved human hepatocytes as an alternative in vitro system to microsomes for the prediction of metabolic clearance
Hayley S. Brown et al.
DRUG METABOLISM AND DISPOSITION (2007)
Comparison of treatment effects between animal experiments and clinical trials: systematic review
Pablo Perel et al.
BMJ-BRITISH MEDICAL JOURNAL (2007)
Specialized hepatocyte-like cells regulate Drosophila lipid metabolism
Eugenio Gutierrez et al.
NATURE (2007)
Scaling factors for the extrapolation of in vivo metabolic drug clearance from in vitro data:: Reaching a consensus on values of human microsomal protein and hepatocellularity per gram of liver
Zoe E. Barter et al.
CURRENT DRUG METABOLISM (2007)
Predictive value of animal models for human cytochrome P450 (CYP)-mediated metabolism: A comparative study in vitro
M. Turpeinen et al.
XENOBIOTICA (2007)
Determination of the hepatocellularity number for human, dog, rabbit, rat and mouse livers from protein concentration measurements
Anna-Karin Sohlenius-Sternbeck
TOXICOLOGY IN VITRO (2006)
Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction
Marcella Martignoni et al.
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY (2006)
Prediction of hepatic clearance using cryopreserved human hepatocytes:: a comparison of serum and serum-free incubations
Nadege Blanchard et al.
JOURNAL OF PHARMACY AND PHARMACOLOGY (2006)
Binding of drugs to hepatic microsomes: Comment and assessment of current prediction methodology with recommendation for improvement
D Hallifax et al.
DRUG METABOLISM AND DISPOSITION (2006)
Determination of a human hepatic microsomal scaling factor for predicting in vivo drug clearance
N Hakooz et al.
PHARMACEUTICAL RESEARCH (2006)
Impact of extracellular protein binding on passive and active drug transport across Caco-2 cells
S Neuhoff et al.
PHARMACEUTICAL RESEARCH (2006)
A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes
RJ Riley et al.
DRUG METABOLISM AND DISPOSITION (2005)
The binding of drugs to hepatocytes and its relationship to physicochemical properties
RP Austin et al.
DRUG METABOLISM AND DISPOSITION (2005)
Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches
K Ito et al.
PHARMACEUTICAL RESEARCH (2005)
Prediction of in vitro intrinsic clearance from hepatocytes: Comparison of suspensions and monolayer cultures
SJ Griffin et al.
DRUG METABOLISM AND DISPOSITION (2005)
Comparison of the use of liver models for predicting drug clearance using in vitro kinetic data from hepatic microsomes and isolated hepatocytes
K Ito et al.
PHARMACEUTICAL RESEARCH (2004)
Where is the evidence that animal research benefits humans?
P Pound et al.
BMJ-BRITISH MEDICAL JOURNAL (2004)
Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance
DF McGinnity et al.
DRUG METABOLISM AND DISPOSITION (2004)
Impact of serum on clearance predictions obtained from suspensions and primary cultures of rat hepatocytes
N Blanchard et al.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2004)
Inter-individual variability in levels of human microsomal protein and hepatocellularity per gram of liver
ZE Wilson et al.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY (2003)
Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism
A Westlind-Johnsson et al.
DRUG METABOLISM AND DISPOSITION (2003)
Functional and phylogenetic analyses of a putative Drosophila melanogaster UDP-glycosyltransferase gene
T Luque et al.
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY (2002)
Prediction of hepatic clearance and availability by cryopreserved human hepatocytes: An application of serum incubation method
Y Shibata et al.
DRUG METABOLISM AND DISPOSITION (2002)
A systematic gene expression screen of Caenorhabditis elegans cytochrome P450 genes reveals CYP35 as strongly xenobiotic inducible
R Menzel et al.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS (2001)
Determining the best animal model for human cytochrome P450 activities: a comparison of mouse, rat, rabbit, dog, micropig, monkey and man
JJP Bogaards et al.
XENOBIOTICA (2000)