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PK-PD modeling of 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine and the enhanced antitumor effect of its phospholipid derivatives in long-circulating liposomes

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Title: PK-PD modeling of 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine and the enhanced antitumor effect of its phospholipid derivatives in long-circulating liposomes
Authors: Takada, Akitsugu Browse this author
Kamiya, Hiroyuki Browse this author
Shuto, Satoshi Browse this author
Matsuda, Akira Browse this author →KAKEN DB
Harashima, Hideyoshi Browse this author →KAKEN DB
Keywords: 3'-ethynylcytidine
antitumor effect
PK-PD modeling
phospholipid derivatives
liposome
minimum effective concentration
Issue Date: 30-Jul-2009
Publisher: Elsevier
Journal Title: International Journal of Pharmaceutics
Volume: 377
Issue: 1-2
Start Page: 52
End Page: 59
Publisher DOI: 10.1016/j.ijpharm.2009.04.039
PMID: 19426792
Abstract: The efficacy of an antitumor nucleoside, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine (3'-ethynylcytidine, ECyd), was analyzed in vitro and in vivo. The in vivo antitumor effect of ECyd encapsulated into long-circulating liposomes was also examined. Based on pharmacokinetic (PK) and pharmacodynamic (PD) analyses, a model that quantitatively explains the in vivo effects of ECyd was proposed, using the concept of minimum effective concentration. The model suggests that ECyd followed a time-dependent mechanism of action in vivo, and that availability of ECyd in tumor tissue was highly important. To improve the availability of ECyd, its phospholipid derivatives were synthesized and encapsulated into long-circulating liposomes, which increased the antitumor effect. These results indicate that it is very important to design carriers of antitumor drugs based on PK-PD modeling.
Type: article (author version)
URI: http://hdl.handle.net/2115/38949
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 紙谷 浩之

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