Chelation therapy is a consolidated medical procedure used primarily to reduce the toxic effects of metal ions on human tissues. Its application spans a broad spectrum of disorders, ranging from acute metal intoxication to genetic metal-overload. The use of chelating agents is compromised by a number of serious side effects, mainly attributable to perturbed equilibrium of essential metal ion homeostasis and dislocation of complexed metal ions to dangerous body sites. For this reason, chelation therapy has been limited to specific critical and otherwise untreatable conditions and needs to be monitored within an appropriate clinical context. An alarming issue today is that fraudsters use the term “chelation therapy” to take advantage of and make profit from people with tragic health problems. We believe that scientists working in this field have the obligation to deter these frauds and to inform the scientific community of the possible side effects and complications of chelation therapy. This duty is all the more important if we consider the detrimental and even life threatening consequences that can occur in subjects with no clear clinical and laboratory evidence of metal intoxication. The aim of this review is to discuss how this “false chelation therapy” developed and in which diseases it is currently applied.