W. Griffith Humphreys
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View article: Data from The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone: A First in Class Epothilone B Analogue in Late-Phase Clinical Development
Data from The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone: A First in Class Epothilone B Analogue in Late-Phase Clinical Development Open
Purpose: To determine if ixabepilone is a substrate for cytochrome P450 3A4 (CYP3A4) and if its metabolism by this cytochrome is clinically important, we did a clinical drug interaction study in humans using ketoconazole as an inhibitor of…
View article: Data from The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone: A First in Class Epothilone B Analogue in Late-Phase Clinical Development
Data from The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone: A First in Class Epothilone B Analogue in Late-Phase Clinical Development Open
Purpose: To determine if ixabepilone is a substrate for cytochrome P450 3A4 (CYP3A4) and if its metabolism by this cytochrome is clinically important, we did a clinical drug interaction study in humans using ketoconazole as an inhibitor of…
View article: HARMONI at ELT: Towards a final design for the natural guide star sensors system
HARMONI at ELT: Towards a final design for the natural guide star sensors system Open
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View article: PCM-net: A refractive index database of chalcogenide phase change\n materials for tunable nanophotonic device modelling
PCM-net: A refractive index database of chalcogenide phase change\n materials for tunable nanophotonic device modelling Open
Recently, chalcogenide glass based phase change materials (PCMs) have shown\nutility as a tuning material for a range of nanophotonic devices. Owing to\ntheir low loss, ultrafast switching speeds and wide waveband operation, PCMs\nare inte…
View article: Advances in the study of drug metabolism – symposium report of the 12th Meeting of the International Society for the Study of Xenobiotics (ISSX)
Advances in the study of drug metabolism – symposium report of the 12th Meeting of the International Society for the Study of Xenobiotics (ISSX) Open
The 12th International Society for the Study of Xenobiotics (ISSX) meeting, held in Portland, OR, USA from July 28 to 31, 2019, was attended by diverse members of the pharmaceutical sciences community. The ISSX New Investigators Group prov…
View article: Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells
Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells Open
Antibody-drug conjugates (ADCs) are composed of an antibody linked to cytotoxic anticancer payloads. ADCs recognize tumor-specific cell surface antigens and are internalized into lysosomes where proteolytic enzymes release the cytotoxic pa…
View article: Organic Anion Transporter Polypeptide 1B1 Polymorphism Modulates the Extent of Drug–Drug Interaction and Associated Biomarker Levels in Healthy Volunteers
Organic Anion Transporter Polypeptide 1B1 Polymorphism Modulates the Extent of Drug–Drug Interaction and Associated Biomarker Levels in Healthy Volunteers Open
Understanding transporter‐mediated drug–drug interactions is an integral part of risk assessment in drug development. Recent studies support the use of hexadecanedioate ( HDA ), tetradecanedioate ( TDA ), coproporphyrin ( CP )‐I, and CP ‐ …
View article: Physiologically‐based pharmacokinetic modelling of a CYP2C19 substrate, BMS‐823778, utilizing pharmacogenetic data
Physiologically‐based pharmacokinetic modelling of a CYP2C19 substrate, BMS‐823778, utilizing pharmacogenetic data Open
Aims Previous studies demonstrated direct correlation between CYP2C19 genotype and BMS‐823778 clearance in healthy volunteers. The objective of the present study was to develop a physiologically‐based pharmacokinetic (PBPK) model for BMS‐8…
View article: Gaining Mechanistic Insight Into Coproporphyrin I as Endogenous Biomarker for OATP1B‐Mediated Drug–Drug Interactions Using Population Pharmacokinetic Modeling and Simulation
Gaining Mechanistic Insight Into Coproporphyrin I as Endogenous Biomarker for OATP1B‐Mediated Drug–Drug Interactions Using Population Pharmacokinetic Modeling and Simulation Open
This study evaluated coproporphyrin I (CPI) as a selective endogenous biomarker of OATP1B‐mediated drug–drug interactions (DDIs) relative to clinical probe rosuvastatin using nonlinear mixed‐effect modeling. Plasma and urine CPI data in th…
View article: Clinical significance of CYP2C19 polymorphisms on the metabolism and pharmacokinetics of 11β‐hydroxysteroid dehydrogenase type‐1 inhibitor BMS‐823778
Clinical significance of CYP2C19 polymorphisms on the metabolism and pharmacokinetics of 11β‐hydroxysteroid dehydrogenase type‐1 inhibitor BMS‐823778 Open
Aims BMS‐823778 is an inhibitor of 11β‐hydroxysteroid dehydrogenase type‐1, and thus a potential candidate for Type 2 diabetes treatment. Here, we investigated the metabolism and pharmacokinetics of BMS‐823778 to understand its pharmacokin…