The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans

F Storelli, M Yin, AR Kumar, MK Ladumor… - Pharmacology & …, 2022 - Elsevier
Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …

Multi-factorial pharmacokinetic interactions: unraveling complexities in precision drug therapy

B Bechtold, J Clarke - Expert opinion on drug metabolism & …, 2021 - Taylor & Francis
Introduction: Precision drug therapy requires accounting for pertinent factors in
pharmacokinetic (PK) inter-individual variability (ie., pharmacogenetics, diseases …

Diagnosing intake and rationalizing toxicities associated with 5F-MDMB-PINACA and 4F-MDMB-BINACA abuse

W Lie, EJY Cheong, EML Goh, HY Moy… - Archives of …, 2021 - Springer
Abstract 5F-MDMB-PINACA and 4F-MDMB-BINACA are synthetic cannabinoids (SCs) that
elicit cannabinoid psychoactive effects. Defining pharmacokinetic–pharmacodynamic (PK …

Physiologically based pharmacokinetic (PBPK) modeling to predict the pharmacokinetics of irbesartan in different CYP2C9 genotypes

CK Cho, P Kang, CG Jang, SY Lee, YJ Lee… - Archives of Pharmacal …, 2023 - Springer
Irbesartan, a potent and selective angiotensin II type-1 (AT1) receptor blocker (ARB), is one
of the representative medications for the treatment of hypertension. Cytochrome P450 (CYP) …

Dissecting the contribution of OATP1B1 to hepatic uptake of statins using the OATP1B1 selective inhibitor estropipate

Y Zhang, E Panfen, M Fancher, M Sinz… - Molecular …, 2019 - ACS Publications
Identification of a selective inhibitor of organic anion transporting polypeptide (OATP) 1B1 is
critical in order to determine the contribution of OATP1B1-mediated uptake of investigational …

Hepatocyte Uptake and Loss Assay (HUpLA): Proof-of-Concept of an All-in-One System for Measuring Hepatic Influx, Egress, and Metabolic Clearance Based on the …

JAS Pauly, E Sande, M Feng… - Drug Metabolism …, 2024 - dmd.aspetjournals.org
Hepatic clearance (CL H) prediction is a critical parameter to estimate human dose.
However, CL H underpredictions are common, especially for slowly metabolized drugs, and …

Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion …

Y Nozaki, S Izumi - Drug Metabolism and Pharmacokinetics, 2020 - Elsevier
Hepatic uptake mediated by organic anion transporting polypeptide (OATP) 1B1 and 1B3
can serve as a major elimination pathway for various anionic drugs and as a site of drug …

Examination of physiologically‐based pharmacokinetic models of rosuvastatin

CM Bowman, F Ma, J Mao… - CPT: Pharmacometrics & …, 2021 - Wiley Online Library
Physiologically‐based pharmacokinetic (PBPK) modeling is increasingly used to predict
drug disposition and drug–drug interactions (DDIs). However, accurately predicting the …

Genetic polymorphisms of human hepatic OATPs: functional consequences and effect on drug pharmacokinetics

Y Nie, J Yang, S Liu, R Sun, H Chen, N Long… - Xenobiotica, 2020 - Taylor & Francis
Organic anion transporting polypeptides (OATPs) belong to the superfamily of solute carriers
(SLC), which are important membrane transporters in animals and humans. Liver is an …

Evaluation of the selectivity of several organic anion transporting polypeptide 1B biomarkers using relative activity factor method

GH Chan, R Houle, J Zhang, R Katwaru, Y Li… - Drug Metabolism and …, 2023 - ASPET
In recent years, some endogenous substrates of organic anion transporting polypeptide 1B
(OATP1B) have been identified and characterized as potential biomarkers to assess …