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edelfosine : ウィキペディア英語版
edelfosine

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Edelfosine (ET-18-O-CH3 ; 1-octadecyl-2-''O''-methyl-glycero-3-phosphocholine) is a synthetic alkyl-lysophospholipid (ALP). It has antineoplastic (anti-cancer) effects.
Like all ALPs, it incorporates into the cell membrane and does not target the DNA. In many tumor cells, it causes selective apoptosis, sparing healthy cells. Edelfosine can activate the Fas/CD95 cell death receptor, can inhibit the MAPK/ERK mitogenic pathway and the Akt/protein kinase B (PKB) survival pathway.〔 Aside from these plasma-level effects, edelfosine also affects gene expression by modulating the expression and activity of transcription factors.〔〔
It has immune modulating properties.
These characteristics cause edelfosine also to affect HIV, parasitic,〔 and autoimmune diseases.〔

It can complement classic anti-cancer drugs such as cisplatin.
It can be administered orally, intraperitoneally (IP) and intravenously (IV).
Edelfosine and other ALPs can be used for purging residual leukemic cells from bone marrow transplants.〔
It is an analog of miltefosine and perifosine.
==''In vitro'' and ''in vivo'' results==
Edelfosine apoptosis-inducing abilities were studied with several types of cancer, among them multiple myeloma and non-small and small cell lung carcinoma cell lines. ''In vivo'' activity against human solid tumors in mice was shown against malignant gynecological tumor cells,〔 like ovarian cancer, and against breast cancer. ''In vivo'' biodistribution studies demonstrated a “considerably higher” accumulation of Edelfosine in tumor cells than in other analyzed organs. It remained undergraded for a long time.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
ウィキペディアで「edelfosine」の詳細全文を読む



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