In vivo microdialysis technique has become one of the major tools to sample endogenous and exogenous substances in extracellular spaces. As a well-validated sampling technique, microdialysis has been frequently employed for quantifying drug disposition at the desired target in both preclinical and clinical settings. This review addresses general methodological considerations critical to performing microdialysis in tumors, highlights selected preclinical and clinical studies that characterized drug disposition in tumors by the use of microdialysis, and illustrates the potential application of microdialysis in the assessment of tumor response to cancer treatment.
