List of works - Aleksandra Galetin

A Novel Physiologically Based Model of Creatinine Renal Disposition to Integrate Current Knowledge of Systems Parameters and Clinical Observations

scientific article published on 22 May 2020

A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance

scientific article published on 26 March 2012

Assessment of algorithms for predicting drug-drug interactions via inhibition mechanisms: comparison of dynamic and static models.

scientific article

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 ⬇️

scientific article published on January 24, 2012

Comparative analysis of CYP3A heteroactivation by steroid hormones and flavonoids in different in vitro systems and potential in vivo implications

scientific article published on 17 April 2008

Comparison of in-vivo and in-silico methods used for prediction of tissue: plasma partition coefficients in rat ⬇️

scientific article published on December 21, 2011

Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions

scientific article published on January 2010

Critique of the two-fold measure of prediction success for ratios: application for the assessment of drug-drug interactions

scientific article published on 29 October 2010

Cyclosporine inhibition of hepatic and intestinal CYP3A4, uptake and efflux transporters: application of PBPK modeling in the assessment of drug-drug interaction potential

scientific article

Development and Application of a Mechanistic Pharmacokinetic Model for Simvastatin and its Active Metabolite Simvastatin Acid Using an Integrated Population PBPK Approach.

scientific article published on 2 December 2014

Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations

scientific article published on 20 December 2007

Drug-drug interaction potential of marketed oncology drugs: in vitro assessment of time-dependent cytochrome P450 inhibition, reactive metabolite formation and drug-drug interaction prediction.

scientific article

Editorial [Hot Topic: Intestinal First-Pass Metabolism - Bridging the Gap Between In Vitro and In Vivo (Prediction of Intestinal First-Pass Metabolism (Guest Editor: Aleksandra Galetin))]

scientific article published in October 2007

Evaluation of various static in vitro-in vivo extrapolation models for risk assessment of the CYP3A inhibition potential of an investigational drug

scientific article published on 18 September 2013

Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: utility and limitations.

scientific article published on October 2008

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

scientific article published on 3 July 2014

Hepatocellular binding of drugs: correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data

scientific article

Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid

scientific article published in April 2004

IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4.

scientific article published in May 2010

ITC commentary on the prediction of digoxin clinical drug-drug interactions from in vitro transporter assays

scientific article published in September 2014

ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans

scientific article

Identification of the effect of multiple polymorphisms on the pharmacokinetics of simvastatin and simvastatin acid using a population-modeling approach

scientific article published on 5 March 2014

In Vitro and in Silico Tools To Assess Extent of Cellular Uptake and Lysosomal Sequestration of Respiratory Drugs in Human Alveolar Macrophages

scientific article published on 2 March 2017

In Vitro-In Vivo Extrapolation of OATP1B-Mediated Drug-Drug Interactions in Cynomolgus Monkey

scientific article published on 11 April 2018

Intestinal and Hepatic Metabolic Activity of Five Cytochrome P450 Enzymes: Impact on Prediction of First-Pass Metabolism

scientific article published on 23 May 2006

Isoform selectivity and kinetics of morphine 3- and 6-glucuronidation by human udp-glucuronosyltransferases: evidence for atypical glucuronidation kinetics by UGT2B7.

scientific article published in September 2003

Kinetic characterization of rat hepatic uptake of 16 actively transported drugs

scientific article published on 5 July 2011

Maximal inhibition of intestinal first-pass metabolism as a pragmatic indicator of intestinal contribution to the drug-drug interactions for CYP3A4 cleared drugs.

scientific article published on October 2007

Mechanistic Models as Framework for Understanding Biomarker Disposition: Prediction of Creatinine-Drug Interactions

scientific article published on 14 May 2020

Mechanistic pharmacokinetic modeling for the prediction of transporter-mediated disposition in humans from sandwich culture human hepatocyte data

scientific article

Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption

scientific article published in June 2009

Methods for predicting in vivo pharmacokinetics using data from in vitro assays

scientific article

Microsomal prediction ofin vivoclearance and associated interindividual variability of six benzodiazepines in humans

scientific article published in June 2005

Modelling atypical CYP3A4 kinetics: principles and pragmatism

scientific article

Multiple inhibition mechanisms and prediction of drug-drug interactions: status of metabolism and transporter models as exemplified by gemfibrozil-drug interactions.

scientific article

Multisite kinetic analysis of interactions between prototypical CYP3A4 subgroup substrates: midazolam, testosterone, and nifedipine

scientific article published in September 2003

PBPK models for the prediction of in vivo performance of oral dosage forms

scientific article published in European Journal of Pharmaceutical Sciences in June 2014

Physiologically based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction.

scientific article published in June 2011

Potential role of intestinal first-pass metabolism in the prediction of drug–drug interactions

scientific article published in July 2008

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

scientific article

Prediction of human drug clearance by multiple metabolic pathways: integration of hepatic and intestinal microsomal and cytosolic data

scientific article

Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data.

scientific article

Prediction of in vivo drug-drug interactions from in vitro data : factors affecting prototypic drug-drug interactions involving CYP2C9, CYP2D6 and CYP3A4.

scientific article

Prediction of in vivo drug-drug interactions from in vitro data: impact of incorporating parallel pathways of drug elimination and inhibitor absorption rate constant

scientific article

Prediction of metabolic clearance using fresh human hepatocytes: Comparison with cryopreserved hepatocytes and hepatic microsomes for five benzodiazepines

scientific article published in April 2008

Prediction of time-dependent CYP3A4 drug-drug interactions: impact of enzyme degradation, parallel elimination pathways, and intestinal inhibition

scientific article

Predictive utility of in vitro rifampin induction data generated in fresh and cryopreserved human hepatocytes, Fa2N-4, and HepaRG cells.

scientific article

Progress curve mechanistic modeling approach for assessing time-dependent inhibition of CYP3A4.

scientific article published on 23 May 2012

Progress towards prediction of human pharmacokinetic parameters from in vitro technologies.

scientific article published on November 2003

Quantitative ADME proteomics - CYP and UGT enzymes in the Beagle dog liver and intestine

scientific article published on 18 July 2014

Quantitative Translation of Microfluidic Transporter in Vitro Data to in Vivo Reveals Impaired Albumin-Facilitated Indoxyl Sulfate Secretion in Chronic Kidney Disease

scientific article published on 27 September 2019

Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach

scientific article published in December 2002

Reduced physiologically-based pharmacokinetic model of repaglinide: impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk.

scientific article

Relative importance of intestinal and hepatic glucuronidation-impact on the prediction of drug clearance

scientific article published on 31 January 2009

Simultaneous assessment of uptake and metabolism in rat hepatocytes: a comprehensive mechanistic model

scientific article

The use of ROC analysis for the qualitative prediction of human oral bioavailability from animal data.

scientific article

Towards Further Verification of Physiologically-Based Kidney Models: Predictability of the Effects of Urine-Flow and Urine-pH on Renal Clearance

scientific article published on 09 November 2018

Understanding the transport properties of metabolites: case studies and considerations for drug development.

scientific article published on 17 December 2013

Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes

scientific article published on 4 June 2012

Utility of recombinant enzyme kinetics in prediction of human clearance: impact of variability, CYP3A5, and CYP2C19 on CYP3A4 probe substrates.

scientific article published in September 2004

List of works by Aleksandra Galetin

A Novel Physiologically Based Model of Creatinine Renal Disposition to Integrate Current Knowledge of Systems Parameters and Clinical Observations

A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance

Assessment of algorithms for predicting drug-drug interactions via inhibition mechanisms: comparison of dynamic and static models.

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 ⬇️

Comparative analysis of CYP3A heteroactivation by steroid hormones and flavonoids in different in vitro systems and potential in vivo implications

Comparison of in-vivo and in-silico methods used for prediction of tissue: plasma partition coefficients in rat ⬇️

Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions

Critique of the two-fold measure of prediction success for ratios: application for the assessment of drug-drug interactions

Cyclosporine inhibition of hepatic and intestinal CYP3A4, uptake and efflux transporters: application of PBPK modeling in the assessment of drug-drug interaction potential

Development and Application of a Mechanistic Pharmacokinetic Model for Simvastatin and its Active Metabolite Simvastatin Acid Using an Integrated Population PBPK Approach.

Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations

Drug-drug interaction potential of marketed oncology drugs: in vitro assessment of time-dependent cytochrome P450 inhibition, reactive metabolite formation and drug-drug interaction prediction.

Editorial [Hot Topic: Intestinal First-Pass Metabolism - Bridging the Gap Between In Vitro and In Vivo (Prediction of Intestinal First-Pass Metabolism (Guest Editor: Aleksandra Galetin))]

Evaluation of various static in vitro-in vivo extrapolation models for risk assessment of the CYP3A inhibition potential of an investigational drug

Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: utility and limitations.

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

Hepatocellular binding of drugs: correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data

Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid

IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4.

ITC commentary on the prediction of digoxin clinical drug-drug interactions from in vitro transporter assays

ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans

Identification of the effect of multiple polymorphisms on the pharmacokinetics of simvastatin and simvastatin acid using a population-modeling approach

In Vitro and in Silico Tools To Assess Extent of Cellular Uptake and Lysosomal Sequestration of Respiratory Drugs in Human Alveolar Macrophages

In Vitro-In Vivo Extrapolation of OATP1B-Mediated Drug-Drug Interactions in Cynomolgus Monkey

Intestinal and Hepatic Metabolic Activity of Five Cytochrome P450 Enzymes: Impact on Prediction of First-Pass Metabolism

Isoform selectivity and kinetics of morphine 3- and 6-glucuronidation by human udp-glucuronosyltransferases: evidence for atypical glucuronidation kinetics by UGT2B7.

Kinetic characterization of rat hepatic uptake of 16 actively transported drugs

Maximal inhibition of intestinal first-pass metabolism as a pragmatic indicator of intestinal contribution to the drug-drug interactions for CYP3A4 cleared drugs.

Mechanistic Models as Framework for Understanding Biomarker Disposition: Prediction of Creatinine-Drug Interactions

Mechanistic pharmacokinetic modeling for the prediction of transporter-mediated disposition in humans from sandwich culture human hepatocyte data

Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption

Methods for predicting in vivo pharmacokinetics using data from in vitro assays

Microsomal prediction ofin vivoclearance and associated interindividual variability of six benzodiazepines in humans

Modelling atypical CYP3A4 kinetics: principles and pragmatism

Multiple inhibition mechanisms and prediction of drug-drug interactions: status of metabolism and transporter models as exemplified by gemfibrozil-drug interactions.

Multisite kinetic analysis of interactions between prototypical CYP3A4 subgroup substrates: midazolam, testosterone, and nifedipine

PBPK models for the prediction of in vivo performance of oral dosage forms

Physiologically based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction.

Potential role of intestinal first-pass metabolism in the prediction of drug–drug interactions

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

Prediction of human drug clearance by multiple metabolic pathways: integration of hepatic and intestinal microsomal and cytosolic data

Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data.

Prediction of in vivo drug-drug interactions from in vitro data : factors affecting prototypic drug-drug interactions involving CYP2C9, CYP2D6 and CYP3A4.

Prediction of in vivo drug-drug interactions from in vitro data: impact of incorporating parallel pathways of drug elimination and inhibitor absorption rate constant

Prediction of metabolic clearance using fresh human hepatocytes: Comparison with cryopreserved hepatocytes and hepatic microsomes for five benzodiazepines

Prediction of time-dependent CYP3A4 drug-drug interactions: impact of enzyme degradation, parallel elimination pathways, and intestinal inhibition

Predictive utility of in vitro rifampin induction data generated in fresh and cryopreserved human hepatocytes, Fa2N-4, and HepaRG cells.

Progress curve mechanistic modeling approach for assessing time-dependent inhibition of CYP3A4.

Progress towards prediction of human pharmacokinetic parameters from in vitro technologies.

Quantitative ADME proteomics - CYP and UGT enzymes in the Beagle dog liver and intestine

Quantitative Translation of Microfluidic Transporter in Vitro Data to in Vivo Reveals Impaired Albumin-Facilitated Indoxyl Sulfate Secretion in Chronic Kidney Disease

Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach

Reduced physiologically-based pharmacokinetic model of repaglinide: impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk.

Relative importance of intestinal and hepatic glucuronidation-impact on the prediction of drug clearance

Simultaneous assessment of uptake and metabolism in rat hepatocytes: a comprehensive mechanistic model

The use of ROC analysis for the qualitative prediction of human oral bioavailability from animal data.

Towards Further Verification of Physiologically-Based Kidney Models: Predictability of the Effects of Urine-Flow and Urine-pH on Renal Clearance

Understanding the transport properties of metabolites: case studies and considerations for drug development.

Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes

Utility of recombinant enzyme kinetics in prediction of human clearance: impact of variability, CYP3A5, and CYP2C19 on CYP3A4 probe substrates.