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The diversity in co-ordination number, geometries, redox states, thermodynamics, and kinetic and intrinsic properties of the metal ion are some special characteristic of organometallic complexes. Organotin (IV) complexes have been the subject of interest because of their biomedical and commercial applications. Nowadays, the need of novel biological active compounds is growing as there is tremendous increase in antibiotic resistance.Metals are known as essential cellular components to function in a number of vital enzymatic and biochemical activities of the cells. Ongoing recent investigations have reported that metal complexes with organic compounds can not only increase the potency of organic compounds but can also lower down the required dosages of action as complexation increases the lipophilic character.This review summarizes the synthesis, and structural and biological application of organotin compounds. Furthermore, the crossing points between organic compounds and their metal ion interactions can help the scientific community to design novel therapeutic molecules.