The potential health hazards involved with antineoplastic agents have been known for decades. Many anticancer drugs are recognized as carcinogens and genotoxins in experimental assays. Second cancers have been recorded in follow-up studies with treated patients. The first findings on occupational exposures among hospital personnel administering chemotherapy were reported only in 1979. Since that time a magnitude of studies have been published using various chemical and biological exposure measurements. These findings prompted improvements in the handling practices of personnel working with anticancer drugs. In spite of strict guidelines for the safe handling of cancer chemotherapeutic agents and extensive improvements in the handling facilities in hospitals, also recent studies have revealed detectable, even if generally much decreased, amounts of indicator drugs in air and surface wipe samples, also including biological samples of personnel in hospital pharmacies and cancer therapy wards. Follow-up measurements show that application of strict safety precautions in hospitals decreases the biological exposure and/or effect markers to the level of unexposed referents. Open information and constant tutoring of personnel to avoid the hazards when working with anticancer drugs is absolutely necessary with the increasing use of these important drugs.