Pollution of the environment with toxic metals has increased dramatically since the beginning of the industrial revolution. Cadmium is of particular concern because it accumulates in the human body with a half-life exceeding IO years and has been Jinked with a number of health problems including renal tubular dysfunction, pulmonary emphysema, significant kidney damage, and possibly osteoporosis. Moreover, in 1993 the International Agency for Research on Cancer (IARC) classified cadmium and compounds containing cadmium as human carcinogens. The field of cadmium intoxication therapy has seen increases in interest due to its poignant toxicity in both humans and animals. Preliminary attempts to combat acute cadmium poisoning included the use of the chelating agents ethylenediaminetetraacetic acid (EDTA) and British anti-Lewisite (BAL). This review will focus on the chemistry, biology, and effectiveness of cadmium intoxication therapy to date. The toxicokinetics of cadmium mammals will be discussed briefly to understand the extent and severity of overexposure. An overview of cadmium chelation therapy will be given with an e_mphasis on the measurable effectiveness of each and significant structure activity relationships. Cadmium intoxication therapy will be reviewed by their indicated routes of action: direct (chelation and antagonism), indirect (induction), and symptom alleviation. The methods by which cadmium therapeutics are evaluated (in vivo, in vitro) are to be discussed. An evaluation of the clinical potential for promising therapeutics will be given.