Hepatocellular carcinoma (HCC) is one of the most commonly diagnosed cancers causing death worldwide. It is difficult to detect at an early stage and most patients with advanced HCC rarely achieve satisfying therapeutic results. Accordingly, researchers have been trying to find new biomarkers for diagnosis and new methods of treatment. OCT1, a member of solute carrier super family, is highly expressed in normal liver tissues, and predominantly transports endogenous and exogenous substances, such as metabolites, drugs and toxins to hepatocytes. Studies have demonstrated that the expression of OCT1 is related to the progression and survival of HCC patients. Furthermore, sorafenib, which is regarded as the only effective molecular targeting drug for advanced HCC, is affected by OCT1 variants. In the current review, we summarized the reports about OCT1 and HCC in order to present a comprehensive overview of the relationship between OCT1 and HCC.