An update on the importance of plasma protein binding in drug discovery and development
L Di - Expert Opinion on Drug Discovery, 2021 - Taylor & Francis
Introduction: Plasma protein binding (PPB) remains a controversial topic in drug discovery
and development. Fraction unbound (fu) is a critical parameter that needs to be measured …
and development. Fraction unbound (fu) is a critical parameter that needs to be measured …
Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data
J Yadav, M El Hassani, J Sodhi… - Drug metabolism …, 2021 - Taylor & Francis
Improved pharmacokinetics/pharmacodynamics (PK/PD) prediction in the early stages of
drug development is essential to inform lead optimization strategies and reduce attrition …
drug development is essential to inform lead optimization strategies and reduce attrition …
Evolving approaches on measurements and applications of intracellular free drug concentration and Kpuu in drug discovery
L Di, K Riccardi, D Tess - Expert Opinion on Drug Metabolism & …, 2021 - Taylor & Francis
Introduction: Intracellular-free drug concentration (Cu, cell) and unbound partition coefficient
(Kpuu) are two important parameters to develop pharmacokinetic and pharmacodynamic …
(Kpuu) are two important parameters to develop pharmacokinetic and pharmacodynamic …
Non-specific binding of compounds in in vitro metabolism assays: a comparison of microsomal and hepatocyte binding in different species and an assessment of the …
I Gardner, M Xu, C Han, Y Wang, X Jiao, M Jamei… - Xenobiotica, 2022 - Taylor & Francis
Non-specific binding in in vitro metabolism systems leads to an underestimation of the true
intrinsic metabolic clearance of compounds being studied. Therefore in vitro binding needs …
intrinsic metabolic clearance of compounds being studied. Therefore in vitro binding needs …
Successful prediction of human hepatic concentrations of transported drugs using the proteomics‐informed relative expression factor approach
Tissue drug concentrations determine the efficacy and toxicity of drugs. When a drug is the
substrate of transporters that are present at the blood: tissue barrier, the steady‐state …
substrate of transporters that are present at the blood: tissue barrier, the steady‐state …
Transplacental passage of hyperforin, hypericin, and valerenic acid
D Spiess, VF Abegg, A Chauveau, J Rath… - Frontiers in …, 2023 - frontiersin.org
Safe medications for mild mental diseases in pregnancy are needed. Phytomedicines from
St. John's wort and valerian are valid candidates, but safety data in pregnancy are lacking …
St. John's wort and valerian are valid candidates, but safety data in pregnancy are lacking …
Comparison of Tumor Binding Across Tumor Types and Cell Lines to Support Free Drug Considerations for Oncology Drug Discovery
S Jordan, S Ryu, W Burchett, C Davis, R Jones… - Journal of …, 2024 - Elsevier
Tumor binding is an important parameter to derive unbound tumor concentration to explore
pharmacokinetics (PK) and pharmacodynamics (PD) relationships for oncology disease …
pharmacokinetics (PK) and pharmacodynamics (PD) relationships for oncology disease …
Placental passage of protopine in an ex vivo human perfusion system
D Spiess, VF Abegg, A Chauveau, A Treyer… - Planta …, 2023 - thieme-connect.com
The placental passage of protopine was investigated with a human ex vivo placental
perfusion model. The model was first validated with diazepam and citalopram, 2 compounds …
perfusion model. The model was first validated with diazepam and citalopram, 2 compounds …
[CITATION][C] Impact of plasma protein binding in drug clearance prediction: a database analysis of published studies and implications for in vitro-in vivo extrapolation
LJ Francis, JB Houston, D Hallifax - Drug Metabolism and Disposition, 2021 - ASPET
Determination of fraction unbound and unbound partition coefficient to estimate intracellular free drug concentration
S Ryu, K Riccardi, S Jordan, N Johnson… - Quantitative analysis of …, 2021 - Springer
Intracellular free drug concentrations are critical to develop pharmacokinetic and
pharmacodynamic relationships, estimate therapeutic indices, and predict drug–drug …
pharmacodynamic relationships, estimate therapeutic indices, and predict drug–drug …