The introduction of in vivo microdialysis (MD) to clinical pharmacological studies has opened the opportunity to obtain previously inaccessible information about the drug distribution process to the clinically relevant target site. The aim of this review is to provide a comprehensive overview of the current literature about MD in drug delivery studies from a clinical perspective. In particular the application of MD in clinical--antimicrobial, oncological and transdermal--and neurological research will be described and the scope of MD in pharmacokinetic-pharmacodynamic (PK-PD) studies will be discussed. It is concluded that MD has a great potential for both academic and industrial research, and may become the method of choice for drug distribution studies in humans.