Active tumor targeting drug delivery system(ATTDDS) can selectively combine with and react to the target tissue at the cellular or subcellular level,making it possible for drugs to be distributed in a controlled manner and released in a slow and continuous manner, subsequently resulting in enhanced anticancer drugs effects and reduced adverse effects on normal tissues. Although there are many problems need to be solved in research on ATTDDS,and there is still a long way to go before it can be used clinically,its roles in overcoming adverse effects of cancer treatment and improving the therapeutic effect are valuable. Generally,ATTDDS is an ideal antitumor drug dosage and has a promising prospect. This paper introduces the effects and characteristics of various types of ATTDDS as well as their problems and countermeasures, hoping to provide research ideas and methods for the antitumor targeted drug delivery.