Multiparametric assay using HepaRG cells for predicting drug-induced liver injury

T Tomida, H Okamura, M Satsukawa, T Yokoi, Y Konno - Toxicology letters, 2015 - Elsevier
The utility of HepaRG cells as an in vitro cell-based assay system for assessing drug-induced
liver injury (DILI) risk was investigated. Seventeen DILI-positive and 15 DILI-negative …

Assessment of intestinal availability of various drugs in the oral absorption process using portal vein-cannulated rats

Y Matsuda, Y Konno, M Satsukawa, T Kobayashi… - Drug Metabolism and …, 2012 - ASPET
To understand the rate-limiting process of oral drug absorption, not only total bioavailability (F)
but also intestinal (F a · F g ) and hepatic (F h ) availability after oral administration should …

Molecular cloning and functions of rat liver hydroxysteroid sulfotransferases catalysing covalent binding of carcinogenic polycyclic arylmethanols to DNA

T Watabe, K Ogura, M Satsukawa, H Okuda… - Chemico-biological …, 1994 - Elsevier
Three sulfotransferases (STs) catalysing the metabolic activation of potent carcinogenic
polycyclic arylmethanols were purified from female Sprague-Dawley (SD) rat liver cytosol …

Usefulness of minipigs for predicting human pharmacokinetics: prediction of distribution volume and plasma clearance

H Yoshimatsu, Y Konno, K Ishii, M Satsukawa… - Drug Metabolism and …, 2016 - Elsevier
In this study, advantages of minipigs to use in preclinical study for new drug development
were evaluated in terms of prediction of human pharmacokinetic (PK) parameters of various …

In Vivo assessment of the impact of efflux transporter on oral drug absorption using portal vein–cannulated rats

…, T Hashimoto, M Nagai, T Taguchi, M Satsukawa… - Drug Metabolism and …, 2013 - ASPET
The purpose of this study was to evaluate the impact of intestinal efflux transporters on the
in vivo oral absorption process. Three model drugs—fexofenadine (FEX), sulfasalazine (SASP…

Quantitative assessment of intestinal first-pass metabolism of oral drugs using portal-vein cannulated rats

…, T Hashimoto, M Nagai, T Taguchi, M Satsukawa… - Pharmaceutical …, 2015 - Springer
Purpose To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome
P4503A (CYP3A) and uridine 5’-diphosphate-glucuronosyltransferases (UGT) on in vivo oral …

Prediction of human percutaneous absorption from in vitro and in vivo animal experiments

H Yoshimatsu, K Ishii, Y Konno, M Satsukawa… - International Journal of …, 2017 - Elsevier
Although anatomical and structural similarities between the skin of minipigs and humans are
often reported, few percutaneous pharmacokinetic studies have been conducted in minipigs…

Lead evaluation of tetrahydroquinolines as nonsteroidal selective androgen receptor modulators for the treatment of osteoporosis

…, N Yamamoto, Y Ohyabu, M Satsukawa… - …, 2014 - Wiley Online Library
Tetrahydroquinoline (THQ) was deemed to be a suitable scaffold for our nonsteroidal selective
androgen receptor modulator (SARM) concept. We adapted the strategy of switching the …

Evaluation of 89 compounds for identification of substrates for cynomolgus monkey CYP2C76, a new bupropion/nifedipine oxidase

S Hosaka, N Murayama, M Satsukawa… - Drug Metabolism and …, 2015 - ASPET
Cynomolgus monkeys are widely used in preclinical studies during drug development
because of their evolutionary closeness to humans, including their cytochrome P450s (P450s). …

Characterization of CYP2C induction in cryopreserved human hepatocytes and its application in the prediction of the clinical consequences of the induction

M Nagai, T Hosaka, M Satsukawa… - Journal of Pharmaceutical …, 2018 - Elsevier
CYP2C enzymes play key roles in drug metabolism, and clinical drug-drug interactions caused
by CYP2C induction have been reported. The aim of this study was to establish a method …