Solid tumors have several barriers that may limit drug penetration and provide inherent mechanisms of resistance. Therefore, the evaluation of antineoplastic agents should base on tumor drug exposure and antitumor activity. Owing to selective access to the extracellular space of the tumor, which acts as target site for most antineoplastic drugs, monitoring drug disposition and corresponding antitumor activity, microdialysis (MD), a probe-based sampling technique, satisfies regulatory requirements for pharmacokinetic- pharmacodynamic (PK-PD) studies. MD is a powerful tool for PK-PD studies of oncological drugs, which would allow better understanding of exposure-response relationships and contributes to the research and development of oncological drugs. Recent progresses in the development of MD for estimating PK-PD studies of oncological drugs are summarized in this review. Special preclinical application examples of MD for PK-PD studies of oncological drugs organized by types of antineoplastic drugs and informations collected are also described. In conclusion, the role of MD in preclinical PK-PD studies of oncological drugs has been confirmed and it has provided a strong foundation for further clinical research.