In Vitro-In Vivo Extrapolation and Scaling Factors for Clearance of Human and Preclinical Species with Liver Microsomes and Hepatocytes

Application of empirical scalars to enable early prediction of human hepatic clearance using IVIVE in drug discovery: an evaluation of 173 drugs

(2022) Robert S Jones et al.   DRUG METABOLISM AND DISPOSITION

In Vitro - in Vivo Extrapolation of Hepatic Clearance in Preclinical Species

(2022) David A. Tess et al.   PHARMACEUTICAL RESEARCH

Effects of Low Temperature on Blood‐to‐Plasma Ratio Measurement

(2021) Jonathan J. Novak et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Global Analysis of Models for Predicting Human Absorption: QSAR, In Vitro, and Preclinical Models

(2021) Edward Price et al.   JOURNAL OF MEDICINAL CHEMISTRY

Humans are animals, but are animals human enough? A systematic review and meta-analysis on interspecies differences in renal drug clearance

(2020) Katja Jansen et al.   DRUG DISCOVERY TODAY

The Critical Role of Passive Permeability in Designing Successful Drugs

(2020) Li Di et al.   ChemMedChem

Improving the Accuracy of Predicted Human Pharmacokinetics: Lessons Learned from the AstraZeneca Drug Pipeline Over Two Decades

(2020) Michael Davies et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Cell-to-Medium Concentration Ratio Overshoot in the Uptake of Statins by Human Hepatocytes in Suspension, but Not in Monolayer: Kinetic Analysis Suggesting a Partial Loss of Functional OATP1Bs

(2020) Wooin Lee et al.   AAPS Journal

Clearance prediction for Amgen molecules against Extended Clearance Classification System (ECCS) and future directions

(2020) Prashant Agarwal et al.   DRUG DISCOVERY TODAY

Prediction of Transporter-Mediated Rosuvastatin Hepatic Uptake Clearance and Drug Interaction in Humans Using Proteomics-Informed REF Approach

(2020) Vineet Kumar et al.   DRUG METABOLISM AND DISPOSITION

Evaluation of the Disconnect between Hepatocyte and Microsome Intrinsic Clearance and In Vitro In Vivo Extrapolation Performance

(2020) Beth Williamson et al.   DRUG METABOLISM AND DISPOSITION

Predicting the Human Hepatic Clearance of Acidic and Zwitterionic Drugs

(2020) David A. Tess et al.   JOURNAL OF MEDICINAL CHEMISTRY

Impact of plasma protein binding in drug clearance prediction: a database analysis of published studies and implications for in vitro in vivo extrapolation

(2020) Laura Jane Francis et al.   DRUG METABOLISM AND DISPOSITION

Mechanistic insights on clearance and inhibition discordance between liver microsomes and hepatocytes when clearance in liver microsomes is higher than in hepatocytes

(2020) Christopher Keefer et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Evaluation of Hepatic Uptake of OATP1B Substrates by Short Term-Cultured Plated Human Hepatocytes: Comparison With Isolated Suspended Hepatocytes

(2020) Takashi Yoshikado et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Evaluation of Prediction Accuracy for Volume of Distribution in Rat and Human Using In Vitro, In Vivo, PBPK and QSAR Methods

(2020) Shibin Mathew et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Physicochemical Properties, Biotransformation, and Transport Pathways of Established and Newly Approved Medications: A Systematic Review of the Top 200 Most Prescribed Drugs vs. the FDA-Approved Drugs Between 2005 and 2016

(2019) Anitha Saravanakumar et al.   CLINICAL PHARMACOKINETICS

Prediction of volume of distribution in preclinical species and humans: application of simplified physiologically based algorithms

(2018) Prashant B. Nigade et al.   XENOBIOTICA

TREND ANALYSIS OF A DATABASE OF INTRAVENOUS PHARMACOKINETIC PARAMETERS IN HUMANS FOR 1352 DRUG COMPOUNDS

(2018) Franco Lombardo et al.   DRUG METABOLISM AND DISPOSITION

Clearance in Drug Design

(2018) Dennis A. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Relevance of Half-Life in Drug Design

(2017) Dennis A. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

New IVIVE method for the prediction of total human clearance and relative elimination pathway contributions from in vitro hepatocyte and microsome data

(2016) Julia Riede et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Volume of Distribution in Drug Design

(2015) Dennis A. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS)

(2015) Manthena V. Varma et al.   PHARMACEUTICAL RESEARCH

Permeability Comparison between Hepatocyte and Low Efflux MDCKII Cell Monolayer

(2014) Rui Li et al.   AAPS Journal

The application of allometric scaling principles to predict pharmacokinetic parameters across species

(2014) Qingbiao Huang et al.   Expert Opinion on Drug Metabolism & Toxicology

The role of drug metabolizing enzymes in clearance

(2014) Li Di   Expert Opinion on Drug Metabolism & Toxicology

A “middle-out” approach to human pharmacokinetic predictions for OATP substrates using physiologically-based pharmacokinetic modeling

(2014) Rui Li et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

Toward a new paradigm for the efficient in vitro–in vivo extrapolation of metabolic clearance in humans from hepatocyte data

(2013) Patrick Poulin et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Application of IVIVE and PBPK modeling in prospective prediction of clinical pharmacokinetics: strategy and approach during the drug discovery phase with four case studies

(2012) Yuan Chen et al.   BIOPHARMACEUTICS & DRUG DISPOSITION

Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design

(2012) Li Di et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Demystifying Brain Penetration in Central Nervous System Drug Discovery

(2012) Li Di et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comparative Assessment of In Vitro–In Vivo Extrapolation Methods used for Predicting Hepatic Metabolic Clearance of Drugs

(2012) Patrick Poulin et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Prediction of Human Renal Clearance from Preclinical Species for a Diverse Set of Drugs That Exhibit Both Active Secretion and Net Reabsorption

(2011) S. W. Paine et al.   DRUG METABOLISM AND DISPOSITION

PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 2: Comparative assessment of prediction methods of human volume of distribution

(2011) Rhys Do Jones et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Development of a new permeability assay using low‐efflux MDCKII cells

(2011) Li Di et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Prediction of Human Metabolic Clearance from In Vitro Systems: Retrospective Analysis and Prospective View

(2010) David Hallifax et al.   PHARMACEUTICAL RESEARCH

Modelling and PBPK Simulation in Drug Discovery

(2009) Hannah M. Jones et al.   AAPS Journal

Modulation of the Partition Coefficient between Octanol and Buffer at pH 7.4 and pKa to Achieve the Optimum Balance of Blood Clearance and Volume of Distribution for a Series of Tetrahydropyran Histamine Type 3 Receptor Antagonists

(2009) T. Hay et al.   DRUG METABOLISM AND DISPOSITION

Prediction of Human Pharmacokinetics From Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches

(2009) Natilie A. Hosea et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Measurement of Dissociation Constants (pKa Values) of Organic Compounds by Multiplexed Capillary Electrophoresis Using Aqueous and Cosolvent Buffers**Advanced Analytical Technologies, Inc. (Formerly CombiSep), 2711 South Loop Drive, Suite 4200, Ames, IA 50010.

(2008) Marina Shalaeva et al.   JOURNAL OF PHARMACEUTICAL SCIENCES