Cisplatin, a well-known chemotherapeutic drug, is effective against various cancers, including carcinomas, germ cell tumors, lymphomas, and sarcomas. Its mechanism of action involves crosslinking with DNA, interfering with DNA repair, and inducing apoptosis. However, due to drug resistance and side effects, other platinum-based drugs like carboplatin and oxaliplatin have been developed. Combination therapies with cisplatin and other drugs are also widely used to overcome resistance and reduce toxicity. This review highlights the physicochemical properties of cisplatin and related drugs, their uses in cancer treatment, molecular mechanisms of action, and side effects. Cisplatin's cytotoxicity is primarily due to its ability to form DNA adducts, induce oxidative stress, modulate calcium signaling, and trigger apoptosis through various signaling pathways. Computational studies have contributed to understanding cisplatin's chemistry and interactions with DNA.Cisplatin, a well-known chemotherapeutic drug, is effective against various cancers, including carcinomas, germ cell tumors, lymphomas, and sarcomas. Its mechanism of action involves crosslinking with DNA, interfering with DNA repair, and inducing apoptosis. However, due to drug resistance and side effects, other platinum-based drugs like carboplatin and oxaliplatin have been developed. Combination therapies with cisplatin and other drugs are also widely used to overcome resistance and reduce toxicity. This review highlights the physicochemical properties of cisplatin and related drugs, their uses in cancer treatment, molecular mechanisms of action, and side effects. Cisplatin's cytotoxicity is primarily due to its ability to form DNA adducts, induce oxidative stress, modulate calcium signaling, and trigger apoptosis through various signaling pathways. Computational studies have contributed to understanding cisplatin's chemistry and interactions with DNA.