Developing an intelligent targeted molecular nanocarrier in cancer therapeutics is one of the research hotspots in the field of biomedicine. Based on the properties of the drug biomolecules or carriers themselves, chemodrugs can reach specific tissues. This therapeutics nanocarrier is also known as “molecular train”. The research of nanocarriers has been developed from single target to multitarget, and from single function to multifunction. Simply passive drug releasing carriers do not allow for more precise treatment in complex cellular microenvironment. However, with the controllable releasing nanocarriers, the drug concentration at the targeted sites can be effectively increased and the drug efficacy can be enhanced. In addition, it can reduce the toxic and side effects on nontargeted tissues， improving the safety of nanocarriers. The ways to control the release of nanocarriers include pH, enzyme, light, magnetic field and etc. This review mainly introduces the research progress in the construction of controllable drug release nanocarriers.