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WR-1065, a dephosphorylated metabolite of amifostine?(Ethyol), can protect against the immediate and delayed effects of radiation exposure.

WR-1065 can protect against zidovudine (AZT) – induced genetoxicity. The lymphoblastoid cell line MOLT-3 cells were exposed to 0/10μM AZT for 96h. In the first 24h 0/5?μM WR-1065 was added and Cyt B was added in 76h in the cells, the viability of AZT treated MOLT-3 cells did not altered.[1] Moreover, in RKO36 cell lines (derivative RKO human colorectal carcinoma carrying a GFP-pCMV-EGFP2Xho), 4 mM final concentration (EC50) WR-1065 treatment for 30min immediately before irradiation showed protective effects against cell chromosomal damage and death induced by ionizing radiation and delayed genomic instability. But 40??M WR-1065 did not show immediate radio-protective effects in irradiated RKO36 cells.[2] WR-1065 acts as radioprotective agents mainly through suppression of the homologous recombination pathway. In SPD8 Chinese hamster cell line, both 4 mM WR-1065 for 30min and 10 ?M for 24h significantly reduced the homologous recombination induced by 0.2 mM Hydroxyurea for 24h or 100 nM camptothecin for 1h. While WR-1065 did not show its radioprotective effects in irradiated homologous recombination-deficient irs 1SF cells compared with homologous recombination-proficient cells AA8/CXR3(P＜0.05).[3]

With spray drying technique using PLGA (polylactide co-glycolide) as the polymer matrix, WR-1065 were prepared into nanoparticles. 500mg/kg WR-1065/PLGA nanoparticles in which containing 21.7(w/w WR-1065) were administrated orally in mice to determined its radio-protective role. WR-1065PLGA nanoparticles treatment mice showed noteworthy higher 30-day survival, less bone marrow suppression and less intestinal injury compared non-treated control mice, indicated its significant radio-protective effects.[4]

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