Abstract: OBJECTIVE To introduce asialoglycoprotein receptor(ASGPR) and the latest experimental progress on ASGPR-mediated drug/gene hepatic targeting for the treatment of liver cancer and hepatitis B virus(HBV). METHODS Based on the relevant literatures, new achievements in studies of ASGPR-mediated drug/gene liver targeting for the treatment of liver cancer and HBV are reviewed. RESULTS ASGPR is predominantly expressed on the sinusoidal surface of mammalian hepatocytes and is involved in many physiological functions, which could be used for drug/gene liver-targeting delivery. CONCLUSION ASGPR-mediated drug/gene hepatic targeting against liver cancer and HBV is expected to be an effective means of treatment.