Metal complexes and organo-metallic compounds have a growing importance in medicine, particularly in oncology. Cisplatin is among the most widely used anticancer agents, but other platinum (PtII) complexes are being introduced in the therapy of tumours. Cell resistance to cisplatin and its analogues is the main reason for treatment failure and clinical relapse. In order to overcome this issue, novel PtII and PtIV as well as non-platinum metal complexes have been developed, with encouraging results. Organotin derivatives have caught much attention during the last two decades for their potential biocidal activities. In recent years several organotin compounds have been synthesised, some with interesting cytotoxic properties. Little is known about the exact mechanisms by which these agents induce cell growth inhibition, although macromolecular synthesis and mitochondrial energy metabolism appear to be the targets. This article will focus on the relevance of organotin derivatives as very promising potential candidates in anticancer therapy.