List of works - Gordon L. Amidon

A mechanistic approach to understanding the factors affecting drug absorption: a review of fundamentals

scientific article

Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis.

scientific article published on September 2003

An improved synthesis of a fluorophosphonate–polyethylene glycol–biotin probe and its use against competitive substrates ⬇️

scientific article published on January 15, 2013

Applying the biopharmaceutics classification system to veterinary pharmaceutical products. Part II. Physiological considerations

scientific article

Biphasic Dissolution as an Exploratory Method During Early Drug Product Development

scientific article published on 02 May 2020

Blockade of interleukin-6 receptor suppresses the proliferation of H460 lung cancer stem cells

scientific article published on 26 April 2012

Carrier-Mediated Prodrug Uptake to Improve the Oral Bioavailability of Polar Drugs: An Application to an Oseltamivir Analogue

scientific article (publication date: February 2016)

Comparative gene expression profiles of intestinal transporters in mice, rats and humans

scientific article published on 23 June 2007

Comparison of the permeability of metoprolol and labetalol in rat, mouse, and Caco-2 cells: use as a reference standard for BCS classification

scientific article published on 4 February 2013

Cytomegalovirus Protease Targeted Prodrug Development ⬇️

scientific article published on March 20, 2013

Dedication to Professor Leslie Z. Benet: 50 Years of Scientific Excellence and Still Going Strong! ⬇️

scientific article published on July 20, 2012

Dipeptidyl peptidase IV as a potential target for selective prodrug activation and chemotherapeutic action in cancers

scientific article

Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability

scientific article

Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach

scientific article published in January 2010

Evaluation and optimized selection of supersaturating drug delivery systems of posaconazole (BCS class 2b) in the gastrointestinal simulator (GIS): An in vitro-in silico-in vivo approach.

scientific article published on 25 January 2018

Evaluation of a three compartment in vitro gastrointestinal simulator dissolution apparatus to predict in vivo dissolution

scientific article

Exploring Bioequivalence of Dexketoprofen Trometamol Drug Products with the Gastrointestinal Simulator (GIS) and Precipitation Pathways Analyses

scientific article published on 15 March 2019

Exploring gastrointestinal variables affecting drug and formulation behavior: Methodologies, challenges and opportunities

scientific article published on 30 November 2016

Fetal and maternal tissue distribution of the new fluoroquinolone DW-116 in pregnant rats

scientific article (publication date: September 2003)

Formulation predictive dissolution (fPD) testing to advance oral drug product development: An introduction to the US FDA funded '21st Century BA/BE' project

scientific article published on 23 June 2018

Functional expression and characterization of a sodium-dependent nucleoside transporter hCNT2 cloned from human duodenum.

scientific article published in August 2003

G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability, Pharm Res 12, 413-420, 1995--backstory of BCS.

scientific article

Gastric emptying and intestinal appearance of nonabsorbable drugs phenol red and paromomycin in human subjects: A multi-compartment stomach approach

scientific article published on 29 May 2018

Hierarchical Mass Transfer Analysis of Drug Particle Dissolution, Highlighting the Hydrodynamics, pH, Particle Size and Buffer Effects for Dissolution of Ionizable and non-Ionizable Drugs in a Compendial Dissolution Vessel

scientific article published on 04 September 2020

Improved Protease-Targeting and Biopharmaceutical Properties of Novel Prodrugs of Ganciclovir.

scientific article published on 18 December 2017

In Vitro Characterization of the Biomimetic Properties of Poly(dimethylsiloxane) To Simulate Oral Drug Absorption.

scientific article

In Vitro Dissolution of Fluconazole and Dipyridamole in Gastrointestinal Simulator (GIS), Predicting in Vivo Dissolution and Drug-Drug Interaction Caused by Acid-Reducing Agents

scientific article published on 27 May 2015

In Vivo Predictive Dissolution and Simulation Workshop Report: Facilitating the Development of Oral Drug Formulation and the Prediction of Oral Bioperformance

scientific article published on 06 September 2018

In Vivo Predictive Dissolution: Comparing the Effect of Bicarbonate and Phosphate Buffer on the Dissolution of Weak Acids and Weak Bases.

scientific article published on 15 May 2015

In Vivo Predictive Dissolution: Transport Analysis of the CO2, Bicarbonate In Vivo Buffer System

scientific article (publication date: November 2014)

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib.

scientific article

In vitro testing of drug absorption for drug 'developability' assessment: forming an interface between in vitro preclinical data and clinical outcome

scientific article

Lessons learned from marketed and investigational prodrugs

scientific article published on May 2004

Linking the Gastrointestinal Behavior of Ibuprofen with The Systemic Exposure Between and Within Humans - Part 1: Fasted State

scientific article published on 12 November 2018

Linking the Gastrointestinal Behavior of Ibuprofen with the Systemic Exposure between and within Humans-Part 2: Fed State

scientific article published on 12 November 2018

Magnetic Resonance Imaging Quantification of Fasted State Colonic Liquid Pockets in Healthy Humans.

scientific article

Mass Transport Analysis of Bicarbonate Buffer: Effect of the CO2-H2CO3 Hydration-Dehydration Kinetics in the Fluid Boundary Layer and the Apparent Effective p Ka Controlling Dissolution of Acids and Bases

scientific article published on 13 May 2019

Mass Transport Analysis of the Enhanced Buffer Capacity of the Bicarbonate-CO Buffer in a Phase-Heterogenous System: Physiological and Pharmaceutical Significance

scientific article published on 26 October 2018

Measurement of fasted state gastric antral motility before and after a standard bioavailability and bioequivalence 240 mL drink of water: Validation of MRI method against concomitant perfused manometry in healthy participants

scientific article published on 11 November 2020

Mechanistic Analysis of Cocrystal Dissolution as a Function of pH and Micellar Solubilization

scientific article published on 15 February 2016

Mechanistic Basis of Cocrystal Dissolution Advantage

scientific article

Mechanistic Understanding of Food Effects: Water Diffusivity in Gastrointestinal Tract Is an Important Parameter for the Prediction of Disintegration of Solid Oral Dosage Forms ⬇️

scientific article published on May 8, 2013

Mechanistic analysis of solute transport in an in vitro physiological two-phase dissolution apparatus ⬇️

scientific article published on 4 September 2012

Mechanistic enhancement of the intestinal absorption of drugs containing the polar guanidino functionality ⬇️

scientific article published on January 14, 2011

Molecular Basis of Prodrug Activation by Human Valacyclovirase, an -Amino Acid Ester Hydrolase

scientific article

N-methylpurine DNA glycosylase and 8-oxoguanine dna glycosylase metabolize the antiviral nucleoside 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole

scientific article published on 24 March 2006

Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability

scientific article published in July 2005

Physiological parameters for oral delivery and in vitro testing

scientific article

Potential of Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine in Facilitating Enhanced Delivery of Active Drug to Interior Sites of Tumors: A Two-Tier Monolayer In Vitro Study ⬇️

scientific article published on June 14, 2011

Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs

scientific article published on 30 October 2009

Prolidase, a potential enzyme target for melanoma: design of proline-containing dipeptide-like prodrugs

scientific article (publication date: 2005)

Proline prodrug of melphalan targeted to prolidase, a prodrug activating enzyme overexpressed in melanoma

scientific article published on 22 March 2007

Pulse Packet Stochastic Model for Gastric Emptying in the Fasted State: A Physiological Approach

scientific article published on 5 March 2018

Puromycin-sensitive aminopeptidase: an antiviral prodrug activating enzyme

scientific article published on 5 December 2009

Quantification of gastrointestinal liquid volumes and distribution following a 240 mL dose of water in the fasted state

scientific article

Selection of suitable prodrug candidates for in vivo studies via in vitro studies; the correlation of prodrug stability in between cell culture homogenates and human tissue homogenates

scientific article published on January 2012

Specificity of a prodrug-activating enzyme hVACVase: the leaving group effect

scientific article

Substrate-Competitive Activity-Based Profiling of Ester Prodrug Activating Enzymes

scientific article

Summary of the National Institute of Child Health and Human Development–Best Pharmaceuticals for Children Act Pediatric Formulation Initiatives Workshop–Pediatric Biopharmaceutics Classification System Working Group ⬇️

scientific article published on November 1, 2012

Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond

scientific article published on June 2008

The Biopharmaceutics Classification System: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC

scientific article published on 28 January 2014

The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene

scientific article

The Evaluation of In Vitro Drug Dissolution of Commercially Available Oral Dosage Forms for Itraconazole in Gastrointestinal Simulator With Biorelevant Media.

scientific article

The Feasibility of Enzyme Targeted Activation for Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine; Cathepsin D as a Potential Targeted Enzyme ⬇️

scientific article published on March 26, 2012

The Solubility–Permeability Interplay: Mechanistic Modeling and Predictive Application of the Impact of Micellar Solubilization on Intestinal Permeation ⬇️

scientific article published on August 11, 2011

The achievement of mass balance by simultaneous quantification of floxuridine prodrug, floxuridine, 5-fluorouracil, 5-dihydrouracil, α-fluoro-β-ureidopropionate, α-fluoro-β-alanine using LC–MS ⬇️

scientific article published on March 5, 2011

The development of orally administrable gemcitabine prodrugs with D-enantiomer amino acids: enhanced membrane permeability and enzymatic stability

scientific article

The dipeptide monoester prodrugs of floxuridine and gemcitabine-feasibility of orally administrable nucleoside analogs.

scientific article published on 27 January 2014

The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS)

scientific article published on 03 March 2017

The solubility-permeability interplay in using cyclodextrins as pharmaceutical solubilizers: mechanistic modeling and application to progesterone

scientific article published in June 2010

The use of BDDCS in classifying the permeability of marketed drugs

scientific article published on 31 January 2008

Toward an in vivo dissolution methodology: a comparison of phosphate and bicarbonate buffers

scientific article

Ultra-Thin, Large-Area Membrane Diffusion Cell for pH-Dependent Simultaneous Dissolution and Absorption Studies

scientific article published on 05 June 2020

Utilization of Gastrointestinal Simulator, an in Vivo Predictive Dissolution Methodology, Coupled with Computational Approach To Forecast Oral Absorption of Dipyridamole.

scientific article

Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model.

scientific article published on August 2006

List of works by Gordon L. Amidon

A mechanistic approach to understanding the factors affecting drug absorption: a review of fundamentals

Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis.

An improved synthesis of a fluorophosphonate–polyethylene glycol–biotin probe and its use against competitive substrates ⬇️

Applying the biopharmaceutics classification system to veterinary pharmaceutical products. Part II. Physiological considerations

Biphasic Dissolution as an Exploratory Method During Early Drug Product Development

Blockade of interleukin-6 receptor suppresses the proliferation of H460 lung cancer stem cells

Carrier-Mediated Prodrug Uptake to Improve the Oral Bioavailability of Polar Drugs: An Application to an Oseltamivir Analogue

Comparative gene expression profiles of intestinal transporters in mice, rats and humans

Comparison of the permeability of metoprolol and labetalol in rat, mouse, and Caco-2 cells: use as a reference standard for BCS classification

Cytomegalovirus Protease Targeted Prodrug Development ⬇️

Dedication to Professor Leslie Z. Benet: 50 Years of Scientific Excellence and Still Going Strong! ⬇️

Dipeptidyl peptidase IV as a potential target for selective prodrug activation and chemotherapeutic action in cancers

Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability

Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach

Evaluation and optimized selection of supersaturating drug delivery systems of posaconazole (BCS class 2b) in the gastrointestinal simulator (GIS): An in vitro-in silico-in vivo approach.

Evaluation of a three compartment in vitro gastrointestinal simulator dissolution apparatus to predict in vivo dissolution

Exploring Bioequivalence of Dexketoprofen Trometamol Drug Products with the Gastrointestinal Simulator (GIS) and Precipitation Pathways Analyses

Exploring gastrointestinal variables affecting drug and formulation behavior: Methodologies, challenges and opportunities

Fetal and maternal tissue distribution of the new fluoroquinolone DW-116 in pregnant rats

Formulation predictive dissolution (fPD) testing to advance oral drug product development: An introduction to the US FDA funded '21st Century BA/BE' project

Functional expression and characterization of a sodium-dependent nucleoside transporter hCNT2 cloned from human duodenum.

G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability, Pharm Res 12, 413-420, 1995--backstory of BCS.

Gastric emptying and intestinal appearance of nonabsorbable drugs phenol red and paromomycin in human subjects: A multi-compartment stomach approach

Hierarchical Mass Transfer Analysis of Drug Particle Dissolution, Highlighting the Hydrodynamics, pH, Particle Size and Buffer Effects for Dissolution of Ionizable and non-Ionizable Drugs in a Compendial Dissolution Vessel

Improved Protease-Targeting and Biopharmaceutical Properties of Novel Prodrugs of Ganciclovir.

In Vitro Characterization of the Biomimetic Properties of Poly(dimethylsiloxane) To Simulate Oral Drug Absorption.

In Vitro Dissolution of Fluconazole and Dipyridamole in Gastrointestinal Simulator (GIS), Predicting in Vivo Dissolution and Drug-Drug Interaction Caused by Acid-Reducing Agents

In Vivo Predictive Dissolution and Simulation Workshop Report: Facilitating the Development of Oral Drug Formulation and the Prediction of Oral Bioperformance

In Vivo Predictive Dissolution: Comparing the Effect of Bicarbonate and Phosphate Buffer on the Dissolution of Weak Acids and Weak Bases.

In Vivo Predictive Dissolution: Transport Analysis of the CO2, Bicarbonate In Vivo Buffer System

In vitro dissolution methodology, mini-Gastrointestinal Simulator (mGIS), predicts better in vivo dissolution of a weak base drug, dasatinib.

In vitro testing of drug absorption for drug 'developability' assessment: forming an interface between in vitro preclinical data and clinical outcome

Lessons learned from marketed and investigational prodrugs

Linking the Gastrointestinal Behavior of Ibuprofen with The Systemic Exposure Between and Within Humans - Part 1: Fasted State

Linking the Gastrointestinal Behavior of Ibuprofen with the Systemic Exposure between and within Humans-Part 2: Fed State

Magnetic Resonance Imaging Quantification of Fasted State Colonic Liquid Pockets in Healthy Humans.

Mass Transport Analysis of Bicarbonate Buffer: Effect of the CO2-H2CO3 Hydration-Dehydration Kinetics in the Fluid Boundary Layer and the Apparent Effective p Ka Controlling Dissolution of Acids and Bases

Mass Transport Analysis of the Enhanced Buffer Capacity of the Bicarbonate-CO Buffer in a Phase-Heterogenous System: Physiological and Pharmaceutical Significance

Measurement of fasted state gastric antral motility before and after a standard bioavailability and bioequivalence 240 mL drink of water: Validation of MRI method against concomitant perfused manometry in healthy participants

Mechanistic Analysis of Cocrystal Dissolution as a Function of pH and Micellar Solubilization

Mechanistic Basis of Cocrystal Dissolution Advantage

Mechanistic Understanding of Food Effects: Water Diffusivity in Gastrointestinal Tract Is an Important Parameter for the Prediction of Disintegration of Solid Oral Dosage Forms ⬇️

Mechanistic analysis of solute transport in an in vitro physiological two-phase dissolution apparatus ⬇️

Mechanistic enhancement of the intestinal absorption of drugs containing the polar guanidino functionality ⬇️

Molecular Basis of Prodrug Activation by Human Valacyclovirase, an -Amino Acid Ester Hydrolase

N-methylpurine DNA glycosylase and 8-oxoguanine dna glycosylase metabolize the antiviral nucleoside 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole

Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability

Physiological parameters for oral delivery and in vitro testing

Potential of Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine in Facilitating Enhanced Delivery of Active Drug to Interior Sites of Tumors: A Two-Tier Monolayer In Vitro Study ⬇️

Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs

Prolidase, a potential enzyme target for melanoma: design of proline-containing dipeptide-like prodrugs

Proline prodrug of melphalan targeted to prolidase, a prodrug activating enzyme overexpressed in melanoma

Pulse Packet Stochastic Model for Gastric Emptying in the Fasted State: A Physiological Approach

Puromycin-sensitive aminopeptidase: an antiviral prodrug activating enzyme

Quantification of gastrointestinal liquid volumes and distribution following a 240 mL dose of water in the fasted state

Selection of suitable prodrug candidates for in vivo studies via in vitro studies; the correlation of prodrug stability in between cell culture homogenates and human tissue homogenates

Specificity of a prodrug-activating enzyme hVACVase: the leaving group effect

Substrate-Competitive Activity-Based Profiling of Ester Prodrug Activating Enzymes

Summary of the National Institute of Child Health and Human Development–Best Pharmaceuticals for Children Act Pediatric Formulation Initiatives Workshop–Pediatric Biopharmaceutics Classification System Working Group ⬇️

Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond

The Biopharmaceutics Classification System: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC

The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene

The Evaluation of In Vitro Drug Dissolution of Commercially Available Oral Dosage Forms for Itraconazole in Gastrointestinal Simulator With Biorelevant Media.

The Feasibility of Enzyme Targeted Activation for Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine; Cathepsin D as a Potential Targeted Enzyme ⬇️

The Solubility–Permeability Interplay: Mechanistic Modeling and Predictive Application of the Impact of Micellar Solubilization on Intestinal Permeation ⬇️

The achievement of mass balance by simultaneous quantification of floxuridine prodrug, floxuridine, 5-fluorouracil, 5-dihydrouracil, α-fluoro-β-ureidopropionate, α-fluoro-β-alanine using LC–MS ⬇️

The development of orally administrable gemcitabine prodrugs with D-enantiomer amino acids: enhanced membrane permeability and enzymatic stability

The dipeptide monoester prodrugs of floxuridine and gemcitabine-feasibility of orally administrable nucleoside analogs.

The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS)

The solubility-permeability interplay in using cyclodextrins as pharmaceutical solubilizers: mechanistic modeling and application to progesterone

The use of BDDCS in classifying the permeability of marketed drugs

Toward an in vivo dissolution methodology: a comparison of phosphate and bicarbonate buffers

Ultra-Thin, Large-Area Membrane Diffusion Cell for pH-Dependent Simultaneous Dissolution and Absorption Studies

Utilization of Gastrointestinal Simulator, an in Vivo Predictive Dissolution Methodology, Coupled with Computational Approach To Forecast Oral Absorption of Dipyridamole.

Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model.