Photo‐induced chemotherapy offers the best option for the selective treatment of cancer among all the prevailing modalities. Iridium (III) complexes, flourished with excellent photophysical and photochemical properties, have been considered to be superior for undergoing photo‐responsive cancer therapy. Large Stokes shift, long‐lived triplet excited state, photostability, and tuneable emission have rendered its excellence as a phototheranostic agent. In particular, the cyclometalated Ir (III) complexes and their respective nanoparticles have made a strong niche in the arena of cancer therapy. In recent years, Ir (III) based complexes have shown promising utilities as both imaging and therapeutic agents as well. Therefore, this review summarises the recent advances in the strategic designing of cyclometalated Ir(III) complexes to augment their phototheranostic applications in precision medicine.