Renal drug transporters and drug interactions

A Ivanyuk, F Livio, J Biollaz, T Buclin - Clinical pharmacokinetics, 2017 - Springer
Transporters in proximal renal tubules contribute to the disposition of numerous drugs.
Furthermore, the molecular mechanisms of tubular secretion have been progressively …

Regulation of drug transport proteins—From mechanisms to clinical impact: A white paper on behalf of the international transporter consortium

KLR Brouwer, R Evers, E Hayden, S Hu… - Clinical …, 2022 - Wiley Online Library
Membrane transport proteins are involved in the absorption, disposition, efficacy, and/or
toxicity of many drugs. Numerous mechanisms (eg, nuclear receptors, epigenetic gene …

Human kidney proximal tubule-on-a-chip for drug transport and nephrotoxicity assessment

KJ Jang, AP Mehr, GA Hamilton, LA McPartlin… - Integrative …, 2013 - academic.oup.com
Kidney toxicity is one of the most frequent adverse events reported during drug
development. The lack of accurate predictive cell culture models and the unreliability of …

[HTML][HTML] A 3D microfluidic liver model for high throughput compound toxicity screening in the OrganoPlate®

KM Bircsak, R DeBiasio, M Miedel, A Alsebahi… - Toxicology, 2021 - Elsevier
We report the development, automation and validation of a 3D, microfluidic liver-on-a-chip
for high throughput hepatotoxicity screening, the OrganoPlate LiverTox™. The model is …

Brain exposure of two selective dual CDK4 and CDK6 inhibitors and the antitumor activity of CDK4 and CDK6 inhibition in combination with temozolomide in an …

TJ Raub, GN Wishart, P Kulanthaivel, BA Staton… - Drug Metabolism and …, 2015 - ASPET
Effective treatments for primary brain tumors and brain metastases represent a major unmet
medical need. Targeting the CDK4/CDK6-cyclin D1-Rb-p16/ink4a pathway using a potent …

Advances in predictive in vitro models of drug-induced nephrotoxicity

JYC Soo, J Jansen, R Masereeuw… - Nature Reviews …, 2018 - nature.com
In vitro screens for nephrotoxicity are currently poorly predictive of toxicity in humans.
Although the functional proteins that are expressed by nephron tubules and mediate drug …

In Vitro Methods to Support Transporter Evaluation in Drug Discovery and Development

KLR Brouwer, D Keppler, KA Hoffmaster… - Clinical …, 2013 - Wiley Online Library
This white paper addresses current approaches and knowledge gaps concerning methods
to assess the role of transport proteins in drug/metabolite disposition in humans. The …

Predicting oral drug absorption: mini review on physiologically-based pharmacokinetic models

L Lin, H Wong - Pharmaceutics, 2017 - mdpi.com
Most marketed drugs are administered orally, despite the complex process of oral
absorption that is difficult to predict. Oral bioavailability is dependent on the interplay …

Organs-on-a-chip: a new tool for drug discovery

A Polini, L Prodanov, NS Bhise… - Expert opinion on …, 2014 - Taylor & Francis
Introduction: The development of emerging in vitro tissue culture platforms can be useful for
predicting human response to new compounds, which has been traditionally challenging in …

Clearance in drug design: miniperspective

DA Smith, K Beaumont, TS Maurer… - Journal of Medicinal …, 2018 - ACS Publications
Due to its implications for both dose level and frequency, clearance rate is one of the most
important pharmacokinetic parameters to consider in the design of drug candidates …