Organotin(IV) complexes have a wide range of different applications. They are highly involved in pharmaceutical applications and have shown anticancer activity against various cancer cell lines. They act as antioxidants and can scavenge free radical species. The biological activity of organotin complexes depends on the organic moiety, type of substituents, number, type, and content of heteroatoms, and their geometry. The current review aimed to discuss using organotin complexes against different cancer cells.