The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions

…, EA Gaman, JB Houston, LM Tremaine - … of Pharmacology and …, 2006 - ASPET
The accuracy of in vitro inhibition parameters in scaling to in vivo drug-drug interactions (DDI)
was examined for over 40 drugs using seven human P450-selective marker activities in …

Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study

RS Obach, LM Cox, LM Tremaine - Drug metabolism and disposition, 2005 - ASPET
The oxidative and conjugative metabolism of sertraline was examined in vitro to identify the
enzymes involved in the generation of N-desmethyl, deaminated, and N-carbamoyl-…

Pharmacokinetics of Sertraline and its N-Demethyl Metabolite in Elderly and Young Male and Female Volunteers

RA Ronfeld, LM Tremaine, KD Wilner - Clinical pharmacokinetics, 1997 - Springer
A nonblinded study was conducted to compare the pharmacokinetic properties of the selective
serotonin reuptake inhibitor sertraline in 22 young (aged 18 to 45 years) and 22 elderly (> …

Deuterium isotope effects on drug pharmacokinetics. I. System-dependent effects of specific deuteration with aldehyde oxidase cleared drugs

…, RS Obach, SL Ripp, DK Spracklin, LM Tremaine… - Drug metabolism and …, 2012 - ASPET
The pharmacokinetic properties of drugs may be altered by kinetic deuterium isotope effects.
With specifically deuterated model substrates and drugs metabolized by aldehyde oxidase, …

A novel relay method for determining low-clearance values

…, B Tan, TS McDonald, Y Lai, LM Tremaine - Drug metabolism and …, 2012 - ASPET
A novel relay method has been developed using cryopreserved human hepatocytes to measure
intrinsic clearance of low-clearance compounds. The relay method involved transferring …

[PDF][PDF] In vitro cytochrome P450 inhibition data and the prediction of drug‐drug interactions: qualitative relationships, quantitative predictions, and the rank‐order …

…, JB Houston, LM Tremaine - Clinical Pharmacology …, 2005 - academia.edu
Drug-drug interactions (DDIs) represent a serious problem in clinical practice. However,
with knowledge gained over the past 15 years on the human drugmetabolizing enzymes, a …

[PDF][PDF] Metabolism and disposition of the 5-hydroxytryptamine uptake blocker sertraline in the rat and dog.

LM Tremaine, WM Welch, RA Ronfeld - Drug metabolism and disposition, 1989 - Citeseer
Materials and Methods Chemicals. Glusulase (NEE-154) was purchased from Du Pont
Pharmaceuticals(Garden City, NY). o-Saccharic acid 1, 4-lactone was purchased from Sigma …

Quantitative contribution of six major transporters to the hepatic uptake of drugs:“SLC-phenotyping” using primary human hepatocytes

…, E Kimoto, DA Tess, B Feng, LM Tremaine… - … of Pharmacology and …, 2019 - ASPET
Hepatic uptake transporters [solute carriers (SLCs)], including organic anion transporting
polypeptide (OATP) 1B1, OATP1B3, OATP2B1, sodium-dependent taurocholate cotransporting …

Hepatobiliary clearance prediction: species scaling from monkey, dog, and rat, and in vitro–in vivo extrapolation of sandwich-cultured human hepatocytes using 17 …

E Kimoto, YA Bi, RE Kosa, LM Tremaine… - Journal of …, 2017 - Elsevier
Hepatobiliary elimination can be a major clearance pathway dictating the pharmacokinetics
of drugs. Here, we first compared the dose eliminated in bile in preclinical species (monkey, …

Prediction of drug-drug interactions from in vitro induction data: application of the relative induction score approach using cryopreserved human hepatocytes

…, S Boldt, M Kish, RS Obach, LM Tremaine - Drug Metabolism and …, 2008 - ASPET
Cytochrome P450 induction-mediated drug-drug interaction (DDI) is one of the major concerns
in clinical practice and for the pharmaceutical industry. Previously, a novel approach [the …