Antineoplastic drugs and/or their metabolites are very reactive chemically and easily react with cell components, both those neoplastic and healthy, which leads to uncontrolled cell damage. Research is being carried out to discover new drugs preventing those destructive changes in healthy cells. Amifostine is one of the few drugs with protective abilities in regard to healthy tissues during antineoplastic therapy. Amifostine alone is inactive chemically, but active metabolite amifostine WR-1065 has been assumed to protect the healthy tissues during antineoplastic therapy by bounding of anticancer drug, causing their detoxification and/or eliminating the free radicals generated during radiation and cytostatic therapy. WR-1065 also protects the healthy tissues by inhibition of apoptosis caused by irradiation and/or alkylating compounds. However, the protective mechanism of amifostine influence on healthy cells has not been fully comprehended, and the research is still being carried out.