Antitumor Benzothiazoles. 8. Synthesis, Metabolic Formation, and Biological Properties of the C- and N-Oxidation Products of Antitumor 2-(4-Aminophenyl) …
E Kashiyama, I Hutchinson, MS Chua… - Journal of medicinal …, 1999 - ACS Publications
2-(4-Aminophenyl)benzothiazoles 1 and their N-acetylated forms have been converted to C-
and N-hydroxylated derivatives to investigate the role of metabolic oxidation in the mode of …
and N-hydroxylated derivatives to investigate the role of metabolic oxidation in the mode of …
Role of CYP1A1 in modulation of antitumor properties of the novel agent 2-(4-amino-3-methylphenyl) benzothiazole (DF 203, NSC 674495) in human breast cancer …
MS Chua, E Kashiyama, TD Bradshaw, SF Stinson… - Cancer research, 2000 - AACR
2-(4-Amino-3-methylphenyl)benzothiazole (DF 203, NSC 674495) is a candidate antitumor
agent with potent and selective activity against human-derived tumor cell lines in vitro and in …
agent with potent and selective activity against human-derived tumor cell lines in vitro and in …
High performance liquid chromatographic methods for the determination of aripiprazole with ultraviolet detection in rat plasma and brain: application to the …
Y Shimokawa, H Akiyama, E Kashiyama, T Koga… - … of Chromatography B, 2005 - Elsevier
High performance liquid chromatographic (HPLC) methods were validated for the determination
of aripiprazole (OPC-14597, Abilify™) in rat plasma and brain. Separation was by Nova-…
of aripiprazole (OPC-14597, Abilify™) in rat plasma and brain. Separation was by Nova-…
Feature importance of machine learning prediction models shows structurally active part and important physicochemical features in drug design
…, K Takeuchi, K Umehara, E Kashiyama - Drug Metabolism and …, 2021 - Elsevier
The objective of this study was to obtain the indicators of physicochemical parameters and
structurally active sites to design new chemical entities with desirable pharmacokinetic …
structurally active sites to design new chemical entities with desirable pharmacokinetic …
In vitro P‐glycoprotein interactions and steady‐state pharmacokinetic interactions between tolvaptan and digoxin in healthy subjects
…, M Furukawa, P Bricmont, E Kashiyama… - The Journal of …, 2011 - Wiley Online Library
Interactions between tolvaptan and digoxin were determined in an open‐label, sequential
study where 14 healthy subjects received tolvaptan 60 mg once daily (QD) on days 1 and 12 …
study where 14 healthy subjects received tolvaptan 60 mg once daily (QD) on days 1 and 12 …
Comparison of p450 enzymes between cynomolgus monkeys and humans: p450 identities, protein contents, kinetic parameters, and potential for inhibitory profiles
…, K Iwasaki, K Umehara, E Kashiyama… - Current drug …, 2013 - ingentaconnect.com
Cynomolgus monkeys are used to predict human pharmacokinetic and/or toxic profiles in the
drug developmental stage. Cynomolgus P450s exhibit a high degree of identity (more than …
drug developmental stage. Cynomolgus P450s exhibit a high degree of identity (more than …
In vitro evaluations for pharmacokinetic drug-drug interactions of a novel serotonin-dopamine activity modulator, brexpiprazole
…, I Amunom, M Torii, K Umehara, E Kashiyama… - Xenobiotica, 2021 - Taylor & Francis
Brexpiprazole, a serotonin-dopamine activity modulator, is indicated for the treatment of
schizophrenia and also adjunctive therapy to antidepressants for the treatment of Major …
schizophrenia and also adjunctive therapy to antidepressants for the treatment of Major …
Two novel CYP2D6* 10 haplotypes as possible causes of a poor metabolic phenotype in Japanese
…, A Soyama, S Ozawa, JI Sawada, E Kashiyama… - Drug metabolism and …, 2009 - ASPET
During the course of sequencing for the CYP2D6 gene, we found a novel single nucleotide
polymorphism of g.3318G>A (E383K) associated with CYP2D6*10, termed as CYP2D6*72. …
polymorphism of g.3318G>A (E383K) associated with CYP2D6*10, termed as CYP2D6*72. …
Predicting drug metabolism and pharmacokinetics features of in-house compounds by a hybrid machine-learning model
…, K Takeuchi, K Umehara, E Kashiyama - Drug Metabolism and …, 2021 - Elsevier
We constructed machine learning-based pharmacokinetic prediction models with very high
performance. The models were trained on 26138 and 16613 compounds involved in …
performance. The models were trained on 26138 and 16613 compounds involved in …
Pharmacokinetics and metabolism of brexpiprazole, a novel serotonin-dopamine activity modulator and its main metabolite in rat, monkey and human
…, Y Hirao, H Akazawa, M Kawabata, E Kashiyama… - Xenobiotica, 2021 - Taylor & Francis
The pharmacokinetics of brexpiprazole were investigated in the in vitro and in vivo. The total
body clearance of brexpiprazole in rat and monkey was 2.32 and 0.326 L/h/kg, respectively, …
body clearance of brexpiprazole in rat and monkey was 2.32 and 0.326 L/h/kg, respectively, …