Chapter 9 - Radioprotectors

Amifostine (cont.)
Is a phosphorothioate that does not
permeate cells due to its terminal
phosphorothioic acid group and is used
as a “prodrug”.
– Administered in inactive form
– Converted into drug in metabolic process
When dephosphorylated by enzyme
alkaline phosphatase, aminofostine is
converted to active metabolite designate
WR-1065
WR-1065 enters normal cells by diffusion
to scavenge free radicals generated by
ionzing radiations.
Optimized high dose for cytoprotection is
400 mg/kg → significant side effects
– Hypocalcemia: low serium calcium in
blood
– Nausea/vomiting
More info http://www.nlm.nih.gov/