In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey.

[1]  S. Bhadresa,et al.  Pharmacokinetics of IDX184, a liver-targeted oral prodrug of 2′-methylguanosine-5′-monophosphate, in the monkey and formulation optimization for human exposure , 2016, European Journal of Drug Metabolism and Pharmacokinetics.

[2]  S. Mandlekar,et al.  Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models , 2015, Biopharmaceutics & drug disposition.

[3]  Kayoko Ohura,et al.  Design of Fexofenadine Prodrugs Based on Tissue-Specific Esterase Activity and Their Dissimilar Recognition by P-Glycoprotein. , 2015, Journal of pharmaceutical sciences.

[4]  S. Yamashita,et al.  Quantitative Assessment of Intestinal First-pass Metabolism of Oral Drugs Using Portal-vein Cannulated Rats , 2015, Pharmaceutical Research.

[5]  Aleksandra Galetin,et al.  Hepatic, Intestinal, Renal, and Plasma Hydrolysis of Prodrugs in Human, Cynomolgus Monkey, Dog, and Rat: Implications for In Vitro–In Vivo Extrapolation of Clearance of Prodrugs , 2014, Drug Metabolism and Disposition.

[6]  Hugues Dolgos,et al.  Utility of In Vitro Systems and Preclinical Data for the Prediction of Human Intestinal First-Pass Metabolism during Drug Discovery and Preclinical Development , 2013, Drug Metabolism and Disposition.

[7]  S. Yamashita,et al.  In Vivo Assessment of the Impact of Efflux Transporter on Oral Drug Absorption Using Portal Vein–Cannulated Rats , 2013, Drug Metabolism and Disposition.

[8]  X. Chu,et al.  Species differences in drug transporters and implications for translating preclinical findings to humans , 2013, Expert opinion on drug metabolism & toxicology.

[9]  William A. Lee,et al.  Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. , 2013, Molecular pharmaceutics.

[10]  V. Herring,et al.  The Role of Human Carboxylesterases in Drug Metabolism: Have We Overlooked Their Importance? , 2013, Pharmacotherapy.

[11]  S. Yamashita,et al.  Assessment of Intestinal Availability of Various Drugs in the Oral Absorption Process Using Portal Vein-Cannulated Rats , 2012, Drug Metabolism and Disposition.

[12]  Yuichiro Sato,et al.  Simultaneous Absolute Protein Quantification of Carboxylesterases 1 and 2 in Human Liver Tissue Fractions using Liquid Chromatography-Tandem Mass Spectrometry , 2012, Drug Metabolism and Disposition.

[13]  Kevin C. Johnson.  Comparison of methods for predicting dissolution and the theoretical implications of particle-size-dependent solubility. , 2012, Journal of pharmaceutical sciences.

[14]  E. T. Williams,et al.  Characterization of the Expression and Activity of Carboxylesterases 1 and 2 from the Beagle Dog, Cynomolgus Monkey, and Human , 2011, Drug Metabolism and Disposition.

[15]  Li Di,et al.  Development of a new permeability assay using low-efflux MDCKII cells. , 2011, Journal of pharmaceutical sciences.

[16]  Michael Gertz,et al.  Physiologically Based Pharmacokinetic Modeling of Intestinal First-Pass Metabolism of CYP3A Substrates with High Intestinal Extraction , 2011, Drug Metabolism and Disposition.

[17]  Micaela B. Reddy,et al.  Physiological modeling and assessments of regional drug bioavailability of danoprevir to determine whether a controlled release formulation is feasible , 2011, Biopharmaceutics & drug disposition.

[18]  M. Miura,et al.  Involvement of Carboxylesterase 1 and 2 in the Hydrolysis of Mycophenolate Mofetil , 2010, Drug Metabolism and Disposition.

[19]  Y. Mizuki,et al.  Prediction of the Intestinal First-Pass Metabolism of CYP3A Substrates in Humans Using Cynomolgus Monkeys , 2010, Drug Metabolism and Disposition.

[20]  Kayoko Ohura,et al.  The role of intestinal carboxylesterase in the oral absorption of prodrugs. , 2010, Current drug metabolism.

[21]  Michael Gertz,et al.  Prediction of Human Intestinal First-Pass Metabolism of 25 CYP3A Substrates from In Vitro Clearance and Permeability Data , 2010, Drug Metabolism and Disposition.

[22]  John D. Davis,et al.  Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: utility and limitations. , 2008, Current drug metabolism.

[23]  A. Galetin,et al.  Potential role of intestinal first-pass metabolism in the prediction of drug–drug interactions , 2008, Expert opinion on drug metabolism & toxicology.

[24]  Masakiyo Hosokawa,et al.  Structure and Catalytic Properties of Carboxylesterase Isozymes Involved in Metabolic Activation of Prodrugs , 2008, Molecules.

[25]  T. Kamataki,et al.  Characterization of cynomolgus monkey cytochrome P450 (CYP) cDNAs: is CYP2C76 the only monkey-specific CYP gene responsible for species differences in drug metabolism? , 2007, Archives of biochemistry and biophysics.

[26]  Masoud Jamei,et al.  Prediction of intestinal first-pass drug metabolism. , 2007, Current drug metabolism.

[27]  Teruko Imai,et al.  Carboxylesterase in the liver and small intestine of experimental animals and human. , 2007, Life sciences.

[28]  A. Dokoumetzidis,et al.  Predictive models for oral drug absorption: from in silico methods to integrated dynamical models , 2007, Expert opinion on drug metabolism & toxicology.

[29]  Teruko Imai,et al.  Substrate Specificity of Carboxylesterase Isozymes and Their Contribution to Hydrolase Activity in Human Liver and Small Intestine , 2006, Drug Metabolism and Disposition.

[30]  T. Imai,et al.  IDENTIFICATION OF ESTERASES EXPRESSED IN CACO-2 CELLS AND EFFECTS OF THEIR HYDROLYZING ACTIVITY IN PREDICTING HUMAN INTESTINAL ABSORPTION , 2005, Drug Metabolism and Disposition.

[31]  B. Vig,et al.  Targeted delivery to PEPT1-overexpressing cells: Acidic, basic, and secondary floxuridine amino acid ester prodrugs , 2005, Molecular Cancer Therapeutics.

[32]  A. Avdeef,et al.  PAMPA--a drug absorption in vitro model 13. Chemical selectivity due to membrane hydrogen bonding: in combo comparisons of HDM-, DOPC-, and DS-PAMPA models. , 2004, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[33]  K. Beaumont,et al.  Design of ester prodrugs to enhance oral absorption of poorly permeable compounds: challenges to the discovery scientist. , 2003, Current drug metabolism.

[34]  Y. Rojanasakul,et al.  Characterization of Mefenamic Acid-Guaiacol Ester: Stability and Transport Across Caco-2 Cell Monolayers , 2002, Pharmaceutical Research.

[35]  Younggil Kwon,et al.  Handbook of Essential Pharmacokinetics, Pharmacodynamics and Drug Metabolism for Industrial Scientists , 2001, Springer US.

[36]  B Agoram,et al.  Predicting the impact of physiological and biochemical processes on oral drug bioavailability. , 2001, Advanced drug delivery reviews.

[37]  J. DeSesso,et al.  Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. , 2001, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[38]  Y Zhang,et al.  Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. , 1999, Journal of controlled release : official journal of the Controlled Release Society.

[39]  Lawrence X. Yu,et al.  Compartmental transit and dispersion model analysis of small intestinal transit flow in humans , 1996 .

[40]  Hans Lennernäs,et al.  EXPERIMENTAL ESTIMATION OF THE EFFECTIVE UNSTIRRED WATER LAYER THICKNESS IN THE HUMAN JEJUNUM, AND ITS IMPORTANCE IN ORAL-DRUG ABSORPTION , 1995 .

[41]  T. Kamataki,et al.  Molecular cloning of monkey liver cytochrome P-450 cDNAs: similarity of the primary sequences to human cytochromes P-450. , 1992, Biochimica et biophysica acta.

[42]  P. Artursson,et al.  A method for the determination of cellular permeability coefficients and aqueous boundary layer thickness in monolayers of intestinal epithelial caco 2 cells grown in permeable filter chambers , 1991 .

[43]  C. Wilke,et al.  Correlation of diffusion coefficients in dilute solutions , 1955 .

[44]  K. Tetsuka,et al.  Quantitative prediction of intestinal glucuronidation of drugs in rats using in vitro metabolic clearance data. , 2012, Drug metabolism and pharmacokinetics.

[45]  S. Komuro,et al.  Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data. , 2011, Drug metabolism and pharmacokinetics.

[46]  Z. Yao,et al.  A portal vein cannulation technique for drug discovery in mice , 2008, Lab Animal.

[47]  R. Buschmann.  Morphometry of the small intestinal enterocytes of the fasted rat and the effects of colchicine , 2004, Cell and Tissue Research.

[48]  H. Yamazaki,et al.  Cytochrome P450-dependent drug oxidation activities in liver microsomes of various animal species including rats, guinea pigs, dogs, monkeys, and humans , 1997, Archives of Toxicology.