Drug intelligence / Profile preview

edelfosine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

Edelfosine is a **synthetic alkyl-lysophospholipid** (ALP) with significant antineoplastic (anti-cancer) and immunomodulatory activity. It incorporates into cellular membranes, preferentially accumulating in **tumor cells**, where it induces **apoptosis** selectively by activating the Fas/CD95 cell death receptor and recruiting this receptor into lipid rafts. Edelfosine inhibits multiple survival and proliferative signaling pathways, including the MAPK/ERK and Akt pathways, and has been shown to modulate gene expression and transcription factor function. It **does not target DNA** directly. In addition to antitumor effects, edelfosine has been investigated for its ability to modulate immune cell proliferation and function, including potential use in autoimmune diseases like multiple sclerosis, and for purging leukemic cells from bone marrow transplants. Clinical trials have included studies in leukemia, non-small cell lung cancer (NSCLC), and brain tumors. Major adverse effects observed are gastrointestinal and hemolytic toxicity, primarily with oral or intravenous routes[1][2][3][4][5].

Other names
1-octadecyl-2-O-methyl-glycero-3-phosphocholine1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine
02

Targets

MHC II (Major histocompatibility complex class II receptor)TNFR (TNF receptor family)AKT (RAC-alpha serine/threonine-protein kinase)AR (Adrenergic receptors)

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