Interpretation of non-clinical data for prediction of human pharmacokinetic parameters: in vitro-in vivo extrapolation and allometric scaling

GW Choi, YB Lee, HY Cho - Pharmaceutics, 2019 - mdpi.com
Extrapolation of pharmacokinetic (PK) parameters from in vitro or in vivo animal to human is
one of the main tasks in the drug development process. Translational approaches provide …

Drug disposition classification systems in discovery and development: a comparative review of the BDDCS, ECCS and ECCCS concepts

GP Camenisch - Pharmaceutical research, 2016 - Springer
Abstract BDDCS, ECCS and ECCCS are compound disposition classification concepts that
aim to streamline, de-risk and speed-up drug development. Although all three systems have …

InVitro-InVivo Extrapolation and Scaling Factors for Clearance of Human and Preclinical Species with Liver Microsomes and Hepatocytes

D Tess, GC Chang, C Keefer, A Carlo, R Jones, L Di - The AAPS journal, 2023 - Springer
In vitro-in vivo extrapolation ((IVIVE) and empirical scaling factors (SF) of human intrinsic
clearance (CLint) were developed using one of the largest dataset of 455 compounds with …

Database of pharmacokinetic time-series data and parameters for 144 environmental chemicals

RR Sayre, JF Wambaugh, CM Grulke - Scientific data, 2020 - nature.com
Time courses of compound concentrations in plasma are used in chemical safety analysis to
evaluate the relationship between external administered doses and internal tissue …

Metabolic Profiling of Human Long-Term Liver Models and Hepatic Clearance Predictions from In Vitro Data Using Nonlinear Mixed-Effects Modeling

NA Kratochwil, C Meille, S Fowler, F Klammers… - The AAPS journal, 2017 - Springer
Early prediction of human clearance is often challenging, in particular for the growing
number of low-clearance compounds. Long-term in vitro models have been developed …

Pharmacokinetic parameters explain the therapeutic activity of antimicrobial agents in a silkworm infection model

A Paudel, S Panthee, M Urai, H Hamamoto… - Scientific reports, 2018 - nature.com
Poor pharmacokinetic parameters are a major reason for the lack of therapeutic activity of
some drug candidates. Determining the pharmacokinetic parameters of drug candidates at …

Current in vitro methods to determine hepatic Kpuu: a comparison of their usefulness and limitations

J Riede, G Camenisch, J Huwyler, B Poller - Journal of pharmaceutical …, 2017 - Elsevier
Unbound intrahepatic drug concentrations determine the interaction potential with
intracellular targets related to toxicity, pharmacokinetics, or pharmacodynamics. Recently …

Use of imaging to assess the activity of hepatic transporters

I Hernández Lozano, O Langer - Expert opinion on drug …, 2020 - Taylor & Francis
Introduction: Membrane transporters of the SLC and ABC families are abundantly expressed
in the liver, where they control the transfer of drugs/drug metabolites across the sinusoidal …

Porcine prediction of pharmacokinetic parameters in people: a pig in a poke?

H Tang, M Mayersohn - Drug Metabolism and Disposition, 2018 - ASPET
The minipig has become an animal of considerable interest in preclinical drug development.
It has been used in toxicology research and in examining/establishing regulatory guidelines …

Prediction and quantification of hepatic transporter-mediated uptake of pitavastatin utilizing a combination of the relative activity factor approach and mechanistic …

P Mitra, S Weinheimer, M Michalewicz… - Drug Metabolism and …, 2018 - ASPET
Quantification of the fraction transported (ft) by a particular transporter will facilitate more
robust estimations of transporter interactions. Using pitavastatin as a model uptake …