絞り込み

16404

広告

目標上積みの「タラノア対話」合意 (毎日新聞)

[PR] 温室ガス削減 「パリ協定」控え18年の1年間かけ実施へ 【ボン五十嵐和大】ドイツのボンで開催中の国連気候変動枠組み条約第23回締約国会議(COP23)...

  1. ドイツの温暖化会議で決議採択 - 福井新...
  2. 国内初の種類 恐竜の卵の化石を展示 山口...
  3. 温暖化、COP23大筋合意 先進国の削減...
  4. 本人望めば蘇生中止 消防庁委託研究班提言...

ニュース一覧

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1.

著者 Koide H , Tsujimoto M , Takeuchi A , Tanaka M , Ikegami Y , Tagami M , Abe S , Hashimoto M , Minegaki T , Nishiguchi K
Xenobiotica.2017 Oct 16 ; ():1-37.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

スターを付ける スターを付ける     (12view , 0users)

Full Text Sources

1. Organic anion-transporting polypeptide 1B1 (OATP1B1) plays an important role in the hepatic uptake of a broad range of substrate drugs. In vitro experiments show that molecular-targeted agents do not always have similar effects on OATP1B1 activity. 2. The purpose of this study was to clarify whether the effects of molecular-targeted agents on OATP1B1 are substrate-dependent. We used OATP1B1-transfected cells to compare the effects of molecular-targeted agents on OATP1B1-mediated uptake of fluorescein (FL), 2',7'-dichlorofluorescein (DCF), atorvastatin, SN-38, and valsartan. 3. Cabozantinib, cediranib, neratinib, pazopanib, regorafenib, sorafenib, and tivantinib did not affect or only slightly affected OATP1B1-mediated substrate uptake. Nilotinib and lenvatinib moderately and strongly inhibited OATP1B1-mediated substrate uptake, respectively. In contrast, afatinib stimulated OATP1B1-mediated uptake of fluorescein and SN-38, ceritinib stimulated that of valsartan, and nintedanib stimulated that of fluorescein and valsartan. In addition, the effects of afatinib, ceritinib, and nintedanib on OATP1B1 activity differed markedly depending on the type of substrate. Afatinib, ceritinib, and nintedanib had a substrate-dependent effect on OATP1B1 activity. 4. We conclude that the evaluation of OATP1B1 activity using only a single probe substrate for some molecular-targeted agents may lead to a faulty understanding of their mechanisms of drug interactions.
PMID: 29034773 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード