DS-8201a, a novel HER2-targeting ADC with a novel DNA topoisomerase I inhibitor, demonstrates a promising antitumor efficacy with differentiation from T-DM1

…, M Oitate, S Arakawa, T Hirai, R Atsumi… - Clinical Cancer …, 2016 - AACR
Purpose: An anti-HER2 antibody–drug conjugate with a novel topoisomerase I inhibitor, DS-8201a,
was generated as a new antitumor drug candidate, and its preclinical pharmacologic …

Establishment and functional characterization of an in vitro model of the blood–brain barrier, comprising a co-culture of brain capillary endothelial cells and astrocytes

…, LH Voorwinden, JL Nielsen, A Ivanov, R Atsumi… - European journal of …, 2001 - Elsevier
Objective: The aim was to establish a flexible, abundantly available, reproducible and
functionally characterized in vitro model of the blood–brain barrier (BBB). Methods: In a first step, …

A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding

S Nakayama, R Atsumi, H Takakusa… - Drug Metabolism and …, 2009 - ASPET
The risk of idiosyncratic drug toxicity (IDT) is of great concern to the pharmaceutical industry.
Current hypotheses based on retrospective studies suggest that the occurrence of IDT is …

Metabolic activation of CPT-11, 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin, a novel antitumor agent, by carboxylesterase

T SATOH, M HOSOKAWA, R ATSUMI… - Biological and …, 1994 - jstage.jst.go.jp
We measured the plasma concentrations of 7-ethyl-10-[4-(1-piperidino)-1-piperidine]
carbonyloxycamptothecin (CPT-11) and the active metabolite 7-ethyl-10-hydroxycamptothecin (SN-…

Identification of influx transporter for the quinolone antibacterial agent levofloxacin

…, N Ohtsu, T Oguma, T Ohnishi, R Atsumi… - Molecular …, 2007 - ACS Publications
Quinolone antibacterial agents exhibit high intestinal absorption, selective tissue distribution,
and renal and biliary excretion. Several ATP-binding cassette transporters are involved in …

Metabolism-dependent hepatotoxicity of amodiaquine in glutathione-depleted mice

S Shimizu, R Atsumi, K Itokawa, M Iwasaki, T Aoki… - Archives of …, 2009 - Springer
We investigated the hepatotoxicity induced by AQ using a glutathione (GSH)-depleted mice
model. Although sole administration of either AQ or l-buthionine-S,R-sulfoxinine (BSO), a …

[HTML][HTML] First-in-human study of the EZH1/2 dual inhibitor valemetostat in relapsed or refractory Non-Hodgkin Lymphoma (NHL)-updated results focusing on adult T …

…, K Araki, N Adachi, T Yamashita, R Atsumi… - Blood, 2019 - Elsevier
Introduction: Enhancer of zeste homolog 2 (EZH2) and EZH1 are alternative subunits of
polycomb repressive complex 2 that catalyze the tri-methylation of lysine 27 residue of histone …

Development of a novel polymeric prodrug of mitomycin C, mitomycin C-dextran conjugate with anionic charge. II. Disposition and pharmacokinetics following …

Y Takakura, R Atsumi, M Hashida, H Sezaki - International journal of …, 1987 - Elsevier
Disposition and pharmacokinetics of a novel polymeric prodrug of mitomycin C (MMC),
mitomycin C-dextran conjugate with anionic charge (MMC-Dan.), following intravenous (iv) and …

Ticlopidine-induced hepatotoxicity in a GSH-depleted rat model

S Shimizu, R Atsumi, T Nakazawa, T Izumi, K Sudo… - Archives of …, 2011 - Springer
We investigated hepatotoxicity induced by ticlopidine (TIC) in glutathione (GSH)-depleted
rats by pre-treatment of a well-known GSH synthesis inhibitor, l-buthionine-S,R-sulfoxinine (…

Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenylpiperazine moiety of 1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3 …

H Naito, S Ohsuki, M Sugimori, R Atsumi… - Chemical and …, 2002 - jstage.jst.go.jp
A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes
in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-…