Raymond Evers

Harnessing human colonoid-derived monolayers as an in vitro platform for investigating accumulation, toxicity, and pharmacodynamics of small molecules

Pedro G.M. Canhão, Anny Smeuninx, Suzy Geerinckx, Raymond Evers et autres

The purpose of this study was to evaluate differentiated human colonoid-derived monolayers (hCDMs) as an in vitro platform for investigating small molecule accumulation, toxicity, and pharmacodynamics (PD), in comparison to Caco-2 monolayers. Differentiated hCDMs formed polarized monolayers with a physiological barrier function …

be, us (code pays fourni par la source)

Application of modelling of cell monolayer permeation data to generate input parameters compatible with in vitro-in vivo translation of blood-brain-barrier disposition of drugs

J.C. Hogan, Yukiko Murata, Zubida M. Al-Majdoub, Jonathan Cheong et autres

Adequate translation of parameters from in vitro experiments to in vivo requires a proper characterisation and mechanistic representation of the systems. The aim of this study was to apply a mechanistic model to better characterise the data from experiments involving in vitro …

us, gb, jp (code pays fourni par la source)

Deconvoluting the in vitro to in vivo drug clearance gap: Questioning the predictive performance of traditional hepatic clearance models

Sofie Heylen, Johan Nicolaï, Stijn Van Asten, Katie De Wagter et autres

In vitro to in vivo extrapolation (IVIVE) methods for hepatic clearance (CL H ) prediction often underpredict, partly due to reliance on mathematical liver disposition models such as the well-stirred model (WSM) or parallel tube model (PTM). The ex vivo isolated perfused …

be, us (code pays fourni par la source)

Deconvoluting the in vitro to in vivo drug clearance gap: questioning the predictive performance of traditional hepatic clearance models

Sofie Heylen, Johan Nicolaï, Stijn Van Asten, Katie De Wagter et autres

Background and Purpose: In vitro to in vivo extrapolation (IVIVE) methods for hepatic clearance (CL H ) prediction often underpredict. This is partly due to reliance on mathematical models such as the well-stirred model (WSM) or the parallel tube model (PTM). The …

be, il (code pays fourni par la source)

Canine Mdr1 Knockout MDCK Cells Reliably Estimate Human Small Intestinal Permeability (Peff) and Fraction Absorbed (fa)

Kristian Beran, Seong Hee Park, An Van den Bergh, Jennifer Dressman et autres

High Resolution Image Download MS PowerPoint Slide Human intestinal permeability is a key determinant of the oral fraction absorbed ( f a ) of active pharmaceutical ingredients (APIs). This study evaluated the ability of an in-house canine Mdr1 (cMdr1) knockout (KO) Madin-Darby …

us, de, il, dk, ch, br (code pays fourni par la source)

Stability testing and metabolite profiling to support optimization of cyclic peptides for oral delivery

Ramaswamy A. Iyer, Shaofei Ji, Jianyao Wang, Saro Mardirosian et autres

us (code pays fourni par la source)

Toward improved clearance predictions and distribution profiles employing the isolated perfused rat liver model: Experimental optimization

Sofie Heylen, Johan Nicolaï, Stijn Van Asten, An Tuytelaars et autres

To reduce the drug attrition due to failure in clinical trials, an early accurate hepatic clearance (CL H ) prediction for small molecule drugs is critical. However, the routinely used in vitro to in vivo extrapolation (IVIVE) methods to predict human CL …

be, us (code pays fourni par la source)

Human organotypic colon in vitro microtissue: unveiling a new window into colonic drug disposition

Pedro G.M. Canhão, Jan Snoeys, Suzy Geerinckx, Marjolein van Heerden et autres

: goblet cell/mucus). In conclusion, EpiColon is a promising platform that offers a valuable complement to conventional Caco-2 monolayers for studying colonic drug disposition. However, the presence of flat and some cuboidal cells, along with low throughput, must be addressed to improve …

be, us, sk (code pays fourni par la source)

Membrane transporters in drug development and as determinants of precision medicine

Aleksandra Galetin, Kim L. R. Brouwer, Donald Tweedie, Kenta J. Yoshida et autres

gb, us, fi, se (code pays fourni par la source)

The Current Status and Use of Microphysiological Systems by the Pharmaceutical Industry: The International Consortium for Innovation and Quality Microphysiological Systems Affiliate Survey and Commentary

Thomas K. Baker, Terry R. Van Vleet, Prathap Kumar S. Mahalingaiah, Taraka Sai Pavan Grandhi et autres

us (code pays fourni par la source)

Is Overexpression of the Plasma Membrane Transporter (SLC29A4) a New Option to Stratify Patients with High-Risk Neuroblastoma for Treatment with 131I-mIBG?

Raymond Evers

us (code pays fourni par la source)

Toward improved predictions of pharmacokinetics of transported drugs in hepatic impairment: Insights from the extended clearance model

Flavia Storelli, Mayur K. Ladumor, Xiaomin Liang, Yurong Lai et autres

Abstract Hepatic impairment (HI) moderately (<5‐fold) affects the systemic exposure (i.e., area under the plasma concentration–time curve [AUC]) of drugs that are substrates of the hepatic sinusoidal organic anion transporting polypeptide (OATP) transporters and are excreted unchanged in the bile and/or urine. …

us, be (code pays fourni par la source)