Asialoglycoprotein receptor （ASGPR） , also called galactose receptor, is predominantly expressed on the sinusoidal surface of mammalian hepatocytes and is involved in many physiological functions. For many years ASGPR has been applied for targeting hepatocytes in drug and gene delivery and for functional mapping of the liver, and considerable progress has been made. ASGPR-mediated liver-targeted drug delivery mainly involved anti-tumor drugs and cholesterol-lowering drugs,etc. Liver-targeted gene delivery was often seen in antisense drugs. The research of hepatic imaging mainly involved the evaluation of liver function and identification between hepatocellular carcinoma and hepatic metastasis of tumors. In addition, researchers have also extended its applications to some new fields, such as three-dimension culture of hepatocytes, hepatocytes screening, and hepatocytes transplantation. New achievements in studies of ASGPR-mediated liver targeting are reviewed in this article