The right compound in the right assay at the right time: an integrated discovery DMPK strategy

Role of Phase II Drug Metabolizing Enzymes in Cancer Chemoprevention

(2012) Snehasis Jana et al.   CURRENT DRUG METABOLISM

Physiologically-Based Pharmacokinetics in Drug Development and Regulatory Science

(2011) Malcolm Rowland et al.   Annual Review of Pharmacology and Toxicology

Interplay of Metabolism and Transport in Determining Oral Drug Absorption and Gut Wall Metabolism: A Simulation Assessment Using the “Advanced Dissolution, Absorption, Metabolism (ADAM)” Model

(2011) A. S. Darwich et al.   CURRENT DRUG METABOLISM

Controversies in Allometric Scaling for Predicting Human Drug Clearance: An Historical Problem and Reflections on What Works and What Does Not

(2011) Huadong Tang et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Influence of Drug Transport Proteins on the Pharmacokinetics and Drug Interactions of Hiv Protease Inhibitors

(2011) Latoya Griffin et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Phase II failures: 2008–2010

(2011) John Arrowsmith   NATURE REVIEWS DRUG DISCOVERY

The evolution of the OATP hepatic uptake transport protein family in DMPK sciences: from obscure liver transporters to key determinants of hepatobiliary clearance

(2011) Katherine S. Fenner et al.   XENOBIOTICA

Risk assessment and mitigation strategies for reactive metabolites in drug discovery and development

(2010) Richard A. Thompson et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Measurement of Unbound Drug Exposure in Brain: Modeling of pH Partitioning Explains Diverging Results between the Brain Slice and Brain Homogenate Methods

(2010) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Prediction of Human Intestinal First-Pass Metabolism of 25 CYP3A Substrates from In Vitro Clearance and Permeability Data

(2010) M. Gertz et al.   DRUG METABOLISM AND DISPOSITION

Pharmacokinetic modeling of the hepatobiliary transport mediated by cooperation of uptake and efflux transporters

(2010) Hiroyuki Kusuhara et al.   DRUG METABOLISM REVIEWS

Regulation of hepatic ABCC transporters by xenobiotics and in disease states

(2010) Xinsheng Gu et al.   DRUG METABOLISM REVIEWS

Lipophilicity in drug discovery

(2010) Michael J Waring   Expert Opinion on Drug Discovery

Assessing brain free fraction in early drug discovery

(2010) Kevin D Read et al.   Expert Opinion on Drug Metabolism & Toxicology

Renal clearance in drug discovery and development: molecular descriptors, drug transporters and disease state

(2010) Bo Feng et al.   Expert Opinion on Drug Metabolism & Toxicology

A rapid computational filter for predicting the rate of human renal clearance

(2010) Stuart W. Paine et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

(2010) Dennis A. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

Optimising in vivo pharmacology studies—Practical PKPD considerations

(2010) Johan Gabrielsson et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Using the Golden Triangle to optimize clearance and oral absorption

(2009) Ted W. Johnson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Defining optimum lipophilicity and molecular weight ranges for drug candidates—Molecular weight dependent lower logD limits based on permeability

(2009) Michael J. Waring   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Influence of CYP2C19 polymorphism on the pharmacokinetics of nelfinavir and its active metabolite

(2009) Bharat D. Damle et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Structure-based Drug Metabolism Predictions for Drug Design

(2009) Hao Sun et al.   Chemical Biology & Drug Design

Predicting Circulating Human Metabolites: How Good Are We?

(2009) Shelby Anderson et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Drug Metabolism for the Perplexed Medicinal Chemist

(2009) Bernard Testa   CHEMISTRY & BIODIVERSITY

Polymorphism of Human Cytochrome P450 2D6 and Its Clinical Significance

(2009) Shu-Feng Zhou   CLINICAL PHARMACOKINETICS

Polymorphism of Human Cytochrome P450 2D6 and Its Clinical Significance

(2009) Shu-Feng Zhou   CLINICAL PHARMACOKINETICS

Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds: strategic considerations

(2009) Johan Gabrielsson et al.   DRUG DISCOVERY TODAY

In Silico Prediction of Biliary Excretion of Drugs in Rats Based on Physicochemical Properties

(2009) G. Luo et al.   DRUG METABOLISM AND DISPOSITION

Contrasting Influence of NADPH and a NADPH-Regenerating System on the Metabolism of Carbonyl-Containing Compounds in Hepatic Microsomes

(2009) C. S. Mazur et al.   DRUG METABOLISM AND DISPOSITION

Evaluation of Multiple in Vitro Systems for Assessment of CYP3A4 Induction in Drug Discovery: Human Hepatocytes, Pregnane X Receptor Reporter Gene, and Fa2N-4 and HepaRG Cells

(2009) D. F. McGinnity et al.   DRUG METABOLISM AND DISPOSITION

Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

(2009) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Human clearance prediction: shifting the paradigm

(2009) Thierry Lavé et al.   Expert Opinion on Drug Metabolism & Toxicology

Improved Measurement of Drug Exposure in the Brain Using Drug-Specific Correction for Residual Blood

(2009) Markus Fridén et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

In Silico Prediction of Volume of Distribution in Human Using Linear and Nonlinear Models on a 669 Compound Data Set

(2009) Giuliano Berellini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Brain Exposure Relationships in Rat and Human Using a Novel Data Set of Unbound Drug Concentrations in Brain Interstitial and Cerebrospinal Fluids

(2009) Markus Fridén et al.   JOURNAL OF MEDICINAL CHEMISTRY

Physicochemical Determinants of Human Renal Clearance

(2009) Manthena V. S. Varma et al.   JOURNAL OF MEDICINAL CHEMISTRY

The species differences of intestinal drug absorption and first-pass metabolism between cynomolgus monkeys and humans

(2009) Masayuki Takahashi et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Development of a novel method for predicting human volume of distribution at steady-state of basic drugs and comparative assessment with existing methods

(2009) Patrick Poulin et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Quantitative Pharmacology or Pharmacokinetic Pharmacodynamic Integration Should Be a Vital Component in Integrative Pharmacology

(2009) J. Gabrielsson et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Impact of Hepatic Uptake Transporters on Pharmacokinetics and Drug−Drug Interactions: Use of Assays and Models for Decision Making in the Pharmaceutical Industry

(2009) Mathew G. Soars et al.   MOLECULAR PHARMACEUTICS

Quantitative Expression Profile of Hepatobiliary Transporters in Sandwich Cultured Rat and Human Hepatocytes

(2009) Na Li et al.   MOLECULAR PHARMACEUTICS

Drug interactions at the blood-brain barrier: Fact or fantasy?☆

(2009) Sara Eyal et al.   PHARMACOLOGY & THERAPEUTICS

Monoamine oxidase inactivation: From pathophysiology to therapeutics☆

(2008) Marco Bortolato et al.   ADVANCED DRUG DELIVERY REVIEWS

Nuclear receptor mediated induction of cytochrome P450 3A4 by anticancer drugs: a key role for the pregnane X receptor

(2008) S. Harmsen et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Pharmacokinetic and Pharmacodynamic Data to be Derived from Early-Phase Drug Development

(2008) Adam Cohen   CLINICAL PHARMACOKINETICS

The role of ABC transporters in drug absorption, distribution, metabolism, excretion and toxicity (ADME–Tox)

(2008) Gergely Szakács et al.   DRUG DISCOVERY TODAY

PREDICTION OF DRUG-DRUG INTERACTIONS FROM IN VITRO INDUCTION DATA: Application of the Relative Induction Score Approach Using Cryopreserved Human Hepatocytes

(2008) O. A. Fahmi et al.   DRUG METABOLISM AND DISPOSITION

Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 670 Drug Compounds

(2008) R. S. Obach et al.   DRUG METABOLISM AND DISPOSITION

Mechanism-based inhibition of cytochrome P450 enzymes: An evaluation of early decision making in vitro approaches and drug–drug interaction prediction methods

(2008) Kenneth H. Grime et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Strategies to assess blood–brain barrier penetration

(2008) Li Di et al.   Expert Opinion on Drug Discovery

The utility of microdosing over the past 5 years

(2008) Graham Lappin et al.   Expert Opinion on Drug Metabolism & Toxicology

Role of flavin-containing monooxgenase in drug development

(2008) John R Cashman   Expert Opinion on Drug Metabolism & Toxicology

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

(2008) Aleksandra Galetin et al.   Expert Opinion on Drug Metabolism & Toxicology

New Era in Drug Interaction Evaluation: US Food and Drug Administration Update on CYP Enzymes, Transporters, and the Guidance Process

(2008) Shiew-Mei Huang et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Prediction of human pharmacokinetics-biliary and intestinal clearance and enterohepatic circulation

(2008) Urban Fagerholm   JOURNAL OF PHARMACY AND PHARMACOLOGY

Prodrugs: design and clinical applications

(2008) Jarkko Rautio et al.   NATURE REVIEWS DRUG DISCOVERY

Characterisation of human tubular cell monolayers as a model of proximal tubular xenobiotic handling

(2008) Colin D.A. Brown et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Importance of Drug Transporters in Pharmacokinetics and Drug Safety

(2008) Peter Ward   TOXICOLOGY MECHANISMS AND METHODS

Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition

(2008) S.-F. Zhou   XENOBIOTICA