Cisplatin, cisplatinum, or cis-diamminedichloroplatinum (II), is really a well-known chemotherapeutic drug. It’s been used to treat numerous human cancers including bladder, mind and neck, lung, ovarian, and testicular cancers. It’s effective against various cancers, including carcinomas, germ cell tumors, lymphomas, and sarcomas. Its mode of action continues to be associated with being able to crosslink using the purine bases around the DNA disturbing DNA repair mechanisms, causing DNA damage, and subsequently inducing apoptosis in cancer cells. However, due to drug resistance and various undesirable negative effects for example severe kidney problems, allergy symptoms, decrease immunity to infections, gastrointestinal disorders, hemorrhage, and hearing problems particularly in more youthful patients, other platinum-that contains anti-cancer drugs for example carboplatin, oxaliplatin yet others, are also used. In addition, combination therapies of cisplatin along with other drugs happen to be highly thought to overcome drug-resistance and lower toxicity. This comprehensive review highlights the physicochemical qualities of cisplatin and related platinum-based drugs, and discusses its uses (either alone or in conjunction with other drugs) to treat various human cancers. A unique attention is compensated to the molecular mechanisms of action, and it is undesirable negative effects.