Tributylotin (TBT) compounds are lipophilic substances having low vapour pressure TBT have been used as an active ingredient in molluscicides, antifoulants and wood preservatives, disinfectants and as biocides used in cooling systems, pulp and paper mills, leather processing, and textile mills. TBT acute poisoning in humans were manifested by hepatic functional changes, hypoglycemia, glycosuria, and respiratory system disturbances, similar to asthma. In experimental animals these compounds exerted mainly immunosuppressive, endocrinopathic, neurotoxic, hepatotoxic, nephrotoxic, and skin and eye irritative effects. Mutagenic, genotoxic and carcinogenic activity of TBT have not been confirmed. However gonadotoxic, embryotoxic, fetotoxic, and developmental effects were observed. In this article the actual views on the mechanisms of TBT toxic effects have been described. In conclusion, TBT may be a potential hazardous to human health.