P-glycoprotein-mediated transport of itraconazole across the blood-brain barrier

…, H Takanaga, H Matsuo, K Yamano… - Antimicrobial agents …, 1998 - Am Soc Microbiol
The mechanism for the accumulation of itraconazole (ITZ) in its elimination from the brain
was studied in rats and mice. The concentration of ITZ in liver tissue declined in parallel with …

Prediction of midazolam—cyp3a inhibitors interaction in the human liver from in vivo/in vitro absorption, distribution, and metabolism data

K Yamano, K Yamamoto, M Katashima, H Kotaki… - Drug Metabolism and …, 2001 - ASPET
The extent of decreases in apparent hepatic clearance and intrinsic hepatic clearance of
midazolam (MDZ) after intravenous administration of MDZ with concomitant oral administration …

Quantitative prediction of metabolic inhibition of midazolam by itraconazole and ketoconazole in rats: implication of concentrative uptake of inhibitors into liver

K Yamano, K Yamamoto, H Kotaki, Y Sawada… - Drug Metabolism and …, 1999 - ASPET
To evaluate the extent of drug-drug interaction concerning metabolic inhibition in the liver
quantitatively, we tried to predict the plasma concentration increasing ratio of midazolam (MDZ…

Species differences in intestinal glucuronidation activities between humans, rats, dogs and monkeys

…, K Tetsuka, F Nakamori, H Moriguchi, K Yamano… - Xenobiotica, 2014 - Taylor & Francis
Glucuronidation via UDP-glucuronosyltransferase (UGT) in the intestine has been reported
to influence the pharmacokinetics (PK) of drugs; however, information concerning the …

Quantitative prediction of metabolic inhibition of midazolam by erythromycin, diltiazem, and verapamil in rats: implication of concentrative uptake of inhibitors into liver

K Yamano, K Yamamoto, H Kotaki, S Takedomi… - … of Pharmacology and …, 2000 - ASPET
To evaluate the degree of drug-drug interaction concerning metabolic inhibition in the liver
quantitatively, we tried to predict the plasma concentration increasing ratio (R) of midazolam (…

Identification of human UDP-glucuronosyltransferase and sulfotransferase as responsible for the metabolism of dotinurad, a novel selective urate reabsorption …

…, K Motoki, S Kobashi, K Miyata, K Yamano… - Drug Metabolism and …, 2021 - ASPET
Dotinurad, a novel selective urate reabsorption inhibitor, is used to treat hyperuricemia. In
humans, orally administered dotinurad is excreted mainly as glucuronide and sulfate …

Correlation between in vivo and in vitro hepatic uptake of metabolic inhibitors of cytochrome P-450 in rats

K Yamano, K Yamamoto, H Kotaki, S Takedomi… - Drug metabolism and …, 1999 - ASPET
To predict the degree of accumulation of hepatic metabolic inhibitors in the liver from the in
vitro data, we investigated the relationship between cell/medium concentration ratios (C/M …

Quantitative prediction of intestinal glucuronidation of drugs in rats using in vitro metabolic clearance data

…, K Tetsuka, Y Naritomi, H Moriguchi, K Yamano… - Drug metabolism and …, 2012 - Elsevier
UDP-glucuronosyltransferase (UGT) is highly expressed in the small intestine and catalyzes
the glucuronidation of small molecules, which may affect the oral bioavailability of drugs. …

Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data

…, K Tetsuka, T Furukawa, K Kadono, K Yamano… - Drug Metabolism and …, 2012 - ASPET
We investigated whether the effects of intestinal glucuronidation on the first-pass effect can
be predicted from in vitro data for UDP-glucuronosyltransferase (UGT) substrates. Human in …

Method for predicting human intestinal first-pass metabolism of UGT substrate compounds

T Furukawa, K Yamano, Y Naritomi, K Tanaka… - Xenobiotica, 2012 - Taylor & Francis
As intestinal glucuronidation has been suggested to generate the low oral bioavailability (F)
of drugs, estimating its effects would be valuable for selecting drug candidates. Here, we …