Drug intelligence / Profile preview

erufosine

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Erufosine** is a synthetic alkylphosphocholine (APC) antineoplastic agent, structurally a derivative of erucylphosphocholine, and known for its intravenous administration and ability to cross the blood-brain barrier[4][7][10]. Mechanistically, erufosine induces apoptosis and autophagy in tumor cells, primarily by modulating multiple signal transduction pathways, notably **PI3K/Akt/mTOR**, **Raf/MEK/ERK**, and **JNK 1/2**[1][2][6][7][10]. It disrupts membrane lipid order and can evoke endoplasmic reticulum and mitochondrial stress, leading to generation of reactive oxygen species, autophagy, and cell death[4][6]. Erufosine shows antitumor activity in vitro and in vivo against various malignancies, including **acute myeloid leukemia**, **chronic lymphocytic leukemia**, **multiple myeloma**, **breast carcinoma**, **bladder carcinoma**, **oral squamous cell carcinoma**, **glioblastoma**, and **prostate cancer**[1][2][3][7][9][10]. It is differentiated from other alkylphospholipids such as edelfosine or perifosine by favorable pharmacokinetics, intravenous administration, and lack of bone marrow toxicity, supporting its ongoing investigation in clinical trials (including phase II for chronic lymphocytic leukemia)[2][7].

Brand names
erufosine
Other names
erucylphospho-N,N,N-trimethylpropanolamineerucylphosphocholine
02

Targets

Cholesterol

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