Endosulfan is an organochlorine insecticide, widely used in insect control. Unfortunately, it is also an acute neurotoxic compound to both insects and mammals, including humans, and has been responsible for many severe poisonings and several fatal cases. Endosulfan also imitates or enhances the effect of the female hormone estrogen, having the capability of causing reproductive and developmental damage in both, animals and humans, and its exposure has been linked to liver tissue injury. This persistent lipophilic compound is one of the most abundant organochlorine pesticides in the environment, capable of undergoing long range transport to remote locations such as the Arctic. It is practically water-insoluble, but readily adheres to clay particles and persists in soil and water for several years. Its indiscriminate and injudicious use in the control of insects on a wide range of agricultural products and in the extermination of house-hold pests, has considerably increased the hazard risk for human health. Also, this compound has a high fatality rate in humans when ingested accidentally, from food or water contaminated, or in suicidal cases. The aim of this article is to review and summarize chemical, biochemical, environmental, and toxicological data of endosulfan and draw attention to its toxicological potential risk to human health.