Drug intelligence / Profile preview

amifostine

Development stage
Approved
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Amifostine is a cytoprotective adjuvant and organic thiophosphate used to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer and to decrease the incidence of moderate to severe xerostomia (dry mouth) in patients undergoing post-operative radiation treatment for head and neck cancer[1][2][3][4][5]. It is a prodrug that is dephosphorylated by alkaline phosphatase in normal tissues to its active free thiol metabolite (WR-1065), which acts as a free radical scavenger, repairs damaged DNA, and protects healthy cells from the harmful effects of chemotherapy or radiation[6][8]. Amifostine preferentially protects normal tissues due to higher concentrations achieved in these cells compared to tumor cells. The drug was developed as the first selective-target and broad-spectrum radioprotector[8].

Brand names
Ethyol
Other names
WR-2721WR2721WR 2721Ethyolamifostine
02

Targets

DNA

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