Disposition of a New Tamibarotene Prodrug in Mice
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概要
- 論文の詳細を見る
Recently, a new compound IT-M-07000 was designed as a prodrug of tamibarotene, one of the therapeutic agents for acute promyelocytic leukemia. In the present study, IT-M-07000 was administered to mice to investigate whether it is actually metabolized to tamibarotene. Its metabolic pathway and the utility as a tamibarotene prodrug were also evaluated. After oral administration of IT-M-07000, IT-M-07000, tamibarotene and two compounds that were supposed to be metabolic intermediates in a β-oxidation pathway of IT-M-07000 to tamibarotene were detected in mouse plasma. It was thus shown that IT-M-07000 is probably β-oxidized to tamibarotene in mice. Comparison of tamibarotene concentration profiles after oral administration of IT-M-07000 or tamibarotene showed that the plasma tamibarotene concentration increased slower and was retained stable, and the area under the plasma concentration–time curve (AUC) of tamibarotene was larger in mice administered IT-M-07000 than tamibarotene. These results indicate that IT-M-07000 is possibly useful as a prodrug of tamibarotene.
- 公益社団法人 日本薬学会の論文
著者
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SHUDO Koichi
Research Foundation Itsuu Laboratory
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Ikarashi Nobutomo
Department of Clinical Pharmacokinetics, School of Pharmacy and Pharmaceutical Sciences, Hoshi Unive
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Ito Kiyomi
Department Of Clinical Pharmacokinetics Hoshi University
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MURATAKE Hideaki
Research Foundation Itsuu Laboratory
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Sugiyama Kiyoshi
Department Of Clinical Pharmacokinetics Hoshi University
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Sugitani Megumi
Department of Clinical Pharmacokinetics, Hoshi University
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Abe Rieko
Department of Clinical Pharmacokinetics, Hoshi University
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Ikarashi Nobutomo
Department of Clinical Pharmacokinetics, Hoshi University
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