Transferrin/Transferrin Receptor mediated endocytosis process is a major pathway of entry of iron into mammalian cells.Intensive studies have been directed to greatly understand it in the past decades. As a target oriented ligand,Transferrin/Transferrin Receptor mediated endocytosis process provides a specific pathway for delivery a variety of metals .In the past few years,many considerable reasearches have shown that Transferrin conjugated with anticancer,proteins and genes can target into tumor cell,the bloods brain barrian and proliferating tissues which overexpress Transferring Receptor. Drugs coupled to Transferrin have many good features for high targeting and low toxin sides.This review conludes the recent progress in Transferrin/Transferrin Receptor mediated drug delivery.