Bioactivation of Tegafur to 5-Fluorouracil Is Catalyzed by Cytochrome P-450 2A6 in Human Liver Microsomes in Vitro

K Ikeda, K Yoshisue, E Matsushima, S Nagayama… - Clinical cancer …, 2000 - AACR
Tegafur is a prodrug of 5-fluorouracil (5-FU) consisting of a new class of oral chemotherapeutic
agents, tegafur/uracil and S-1, which are classified as dihydropyrimidine dehydrogenase …

The quantitative prediction of CYP-mediated drug interaction by physiologically based pharmacokinetic modeling

M Kato, Y Shitara, H Sato, K Yoshisue, M Hirano… - Pharmaceutical …, 2008 - Springer
Purpose The objective is to confirm if the prediction of the drug–drug interaction using a
physiologically based pharmacokinetic (PBPK) model is more accurate. In vivo K i values were …

First-in-human, phase I dose-escalation study of single and multiple doses of a first-in-class enhancer of fluoropyrimidines, a dUTPase inhibitor (TAS-114) in healthy …

K Saito, H Nagashima, K Noguchi, K Yoshisue… - Cancer chemotherapy …, 2014 - Springer
Purpose TAS-114 is a first-in-class oral deoxyuridine triphosphatase (dUTPase) inhibitor,
which acts as a modulator of the pyrimidine nucleotide metabolic pathway. This was a first-in-…

Simultaneous expression of guinea pig UDP-glucuronosyltransferase 2B21 and 2B22 in COS-7 cells enhances UDP-glucuronosyltransferase 2B21-catalyzed …

…, M Tsuda, Y Yamaguchi-Nagamatsu, K Yoshisue… - Molecular …, 2001 - ASPET
Although UDP-glucuronosyltransferases (UGTs) act as an important detoxification system
for many endogenous and exogenous compounds, they are also involved in the metabolic …

TAS-114, a first-in-class dual dUTPase/DPD inhibitor, demonstrates potential to improve therapeutic efficacy of fluoropyrimidine-based chemotherapy

…, T Wakasa, K Yamamura, A Fujioka, K Yoshisue… - Molecular cancer …, 2018 - AACR
5-Fluorouracil (5-FU) is an antimetabolite and exerts antitumor activity via intracellularly and
physiologically complicated metabolic pathways. In this study, we designed a novel small …

Tissue distribution and biotransformation of potassium oxonate after oral administration of a novel antitumor agent (drug combination of tegafur, 5-chloro-2, 4 …

K Yoshisue, H Masuda, E Matsushima, K Ikeda… - Drug metabolism and …, 2000 - ASPET
S-1, a new oral 5-fluorouracil (5-FU)-derivative antitumor agent, is composed of tegafur, 5-chloro-2,4-dihydropyridine,
and potassium oxonate (Oxo). Oxo, which inhibits the …

Exposure-dependent incorporation of trifluridine into DNA of tumors and white blood cells in tumor-bearing mouse

…, M Takeuchi, F Nakagawa, K Yoshisue… - Cancer chemotherapy …, 2015 - Springer
Purpose Trifluridine (TFT) is an antitumor component of a novel nucleoside antitumor agent,
TAS-102, which consists of TFT and tipiracil hydrochloride (thymidine phosphorylase …

Purification of a phenobarbital-inducible UDP-glucuronosyltransferase isoform from dog liver which catalyzes morphine and testosterone glucuronidation

…, A Kurogi, K Yamabe, M Tanaka, K Yoshisue… - Archives of Biochemistry …, 1996 - Elsevier
A morphine UDP-glucuronosyltransferase (UGT) which could belong to the UGT2B subfamily
was isolated from liver microsomes of a male beagle dog treated with phenobarbital. …

Reduction of 5-fluorouracil (5-FU) gastrointestinal (GI) toxicity resulting from the protection of thymidylate synthase (TS) in GI tissue by repeated simultaneous …

K Yoshisue, K Hironaga, S Yamaguchi… - Cancer chemotherapy …, 2000 - Springer
Purpose: An important cytotoxic effect of 5-fluorouracil (5-FU) is the inactivation of thymidylate
synthase (TS) (EC 2.1.1.45) activity by the formation of a ternary complex consisting of …

Pharmacokinetics and biological fate of 3-(2, 2, 2-trimethylhydrazinium) propionate dihydrate (MET-88), a novel cardioprotective agent, in rats

K Yoshisue, Y Yamamoto, KI Yoshida, M Saeki… - Drug metabolism and …, 2000 - ASPET
In this study, we examined the disposition, metabolism, and excretion of a novel cardioprotective
agent, 3-(2,2,2-trimethylhydrazinium)propionate dihydrate (MET-88), in rats. The …