Several anticancer drugs such as cisplatin, and its analogues, epirubicin, and doxorubicin are well known for their anticancer activity but the therapeutic value of these drugs comes with certain side effects and they cannot distinguish between normal and cancer cells. Thus, a major challenge for researchers around the world is to develop an anticancer drug with the least toxicity and more target specificity. With the successful reporting of NAMI-A and KP1019, a new path has emerged in the anticancer field. Recently, several Ru(II) complexes have been reported for their anticancer activity due to their enhanced cellular uptake and selectivity towards cancer cells. Apart from the Ru(II) complexes, a large amount of research has been carried out with Ir(III), Re(I), and Rh(III) based complexes, which exhibited promising anticancer activity. The present review reports various Ru(II), Ir(III), Re(I), and Rh(III) based complexes for their anticancer activity based on their cytotoxicity profiles, biological targets and mechanism of action.