Platinum (Pt)-based pharmaceutical drugs are among the most active agents utilized for the therapy of cancer. Carboplatin, cisplatin and oxaliplatin are three members of the platinum anticancer drug family approved by Food and Drug Administration (FDA). Despite gaining enormous success, the extensive application and efficacy of these drugs are often impeded by toxic side effects, their susceptibility to acquired drug resistance, and limited activity against many human cancers. These compounds are known to induce the apoptosis of tumor cells by binding to nuclear DNA, forming a variety of structural adducts to trigger cellular responses. To better understand the anticancer treatment with Pt-based chemotherapeutics, pharmaceutical formulations in perfect quality are required and the behavior of the drugs must be studied at therapeutically relevant levels by separation and detection of the intact drug and its individual biotransformation species in clinical samples. In this review, Pt-based drugs are introduced and the detection methods of Ptbased adduct with DNA and protein have been discussed.