Abstract: Asialoglycoprotein receptor(ASGPR)is a receptor expressed mainly on the surface of liver sinusoidal and basolateral cells. It can exclusively identity, combine and clear desialylated glycoproteins with exposed non-reducing D-galactose(Gal)or nacetylgalactosamine(GalNAc)as end groups. Based on this characteristic, ASGPR-mediated targeted liver cancer therapy has drawn extensive attention. The present review details the latest research progress of this field in three aspects, glycosylated prodrug, small molecular nanocarriers, and glycosylated gene complex therapy system.