Toxicity-related problems, drug resistance and broad spectrum of action have hindered the success pathway of platinum antitumor chemotherapeutic drugs, although the survival rates for patients suffering from solid cancers treated by platinum drugs, notably ‘cisplatin’ is considerably high. Therefore, many non-platinum metal-based chemical entities are gaining attention and have also entered preclinical testing and clinical trails, yet at a later stage they fail to qualify as drugs and consequently, there is lot of setback to pharmaceutical R&D’s. Thus, there is a quest for the design of novel metal-based efficacious cancer chemotherapeutics exhibiting a different mode of action of cell death at the molecular level. Among the non-platinum metal-based drugs, organotin compounds have proven their worth in effective management of toxicity issues and specific targeted drug uptake only by the cancerous cells leaving the healthy cells unaffected (apoptosis). Herein, we reflect the progress made in the past decade by organotin compounds as antitumor chemotherapeutic agents (it was observed that more than 50% of organotin compounds show high cytotoxic activity but surprisingly have not entered clinical trails) and explore the landmarks for their future projections in drug industry.