Hugues Dolgos
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Author Swipe
View article: Prediction of active human dose: learnings from 20 years of Merck KGaA experience, illustrated by case studies
Prediction of active human dose: learnings from 20 years of Merck KGaA experience, illustrated by case studies Open
High-quality dose predictions based on a good understanding of target engagement is one of the main translational goals in drug development. Here, we systematically evaluate active human dose predictions for 15 Merck KGaA/EMD Serono assets…
View article: Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling
Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling Open
Poor aqueous solubility and dissolution of drug candidates drive key decisions on lead series optimization during drug discovery, on formulation optimization, and clinical studies planning during drug development. The interpretation of the…
View article: Prediction of volume of distribution in humans: analysis of eight methods and their application in drug discovery
Prediction of volume of distribution in humans: analysis of eight methods and their application in drug discovery Open
The performance of eight different methods to predict human volume of distribution (VDss) using a large data set (N > 100) was evaluated.The accuracy was assessed by the end points % within two-fold and absolute average fold error (AAFE). …
View article: A Novel <scp>PBPK</scp> Modeling Approach to Assess Cytochrome P450 Mediated Drug‐Drug Interaction Potential of the Cytotoxic Prodrug Evofosfamide
A Novel <span>PBPK</span> Modeling Approach to Assess Cytochrome P450 Mediated Drug‐Drug Interaction Potential of the Cytotoxic Prodrug Evofosfamide Open
Evofosfamide is a cytotoxic small‐molecule prodrug preferentially activated under hypoxic conditions. The cytotoxicity of evofosfamide impacted the generation of in vitro drug‐drug interaction ( DDI ) data, especially in vitro induction re…
View article: A comparative evaluation of models to predict human intestinal metabolism from nonclinical data
A comparative evaluation of models to predict human intestinal metabolism from nonclinical data Open
Extensive gut metabolism is often associated with the risk of low and variable bioavailability. The prediction of the fraction of drug escaping gut wall metabolism as well as transporter‐mediated secretion ( F g ) has been challenged by th…
View article: In vitro and in vivo drug disposition of cilengitide in animals and human
In vitro and in vivo drug disposition of cilengitide in animals and human Open
Cilengitide is very low permeable (1.0 nm/sec) stable cyclic pentapeptide containing an Arg‐Gly‐Asp motif responsible for selective binding to α v β 3 and α v β 5 integrins administered intravenously (i.v.). In vivo studies in the mouse an…
View article: Translational Medicine Guide transforms drug development processes: the recent Merck experience
Translational Medicine Guide transforms drug development processes: the recent Merck experience Open
Merck is implementing a question-based Translational Medicine Guide (TxM Guide) beginning as early as lead optimization into its stage-gate drug development process. Initial experiences with the TxM Guide, which is embedded into an integra…