Background: The chemotherapy medication cisplatin has been used to treat a variety of human cancers, including ovarian, lung, head and neck, testicular, and bladder tumors. Cisplatin has shown effectiveness against a number of cancer types, including lymphomas, sarcomas, germ cell tumors, and carcinomas. The mechanism of action of cisplatin has been associated with ability to crosslink with the urine bases on the DNA to form DNA adducts. This prevents DNA damage from being repaired, which in turn causes cancer cells to undergo apoptosis. However, the medication shows certain signs of resistance, such as enhanced DNA damage repair, decreased drug accumulation intracellularly, and cisplatin cytosolic inactivation. Aim: The current review presents a pharmacological review on the cisplatin including its mechanism of action, resistance mechanism, and toxicity as well as its clinical applications. Conclusion: in summary, researchers have frequently emphasized the significance of Cisplatin therapy as the cornerstone of the treatment of various cancers. Strong evidence from research has shown that cisplatin-based chemotherapy regimens combined with other medications are more effective at reducing toxic side effects and overcoming drug resistance.