Recently, it has been reported that LEPU BIO-B (02157) has successfully completed the enrollment of the first patient in its Phase II clinical trial for the targeted GPC3 antibody-drug conjugate (ADC) MRG006A in advanced hepatocellular carcinoma (HCC). MRG006A is the world's first targeted GPC3 ADC to enter Phase II clinical trials. Developed based on LEPU BIO's next-generation Hi-TOPi ADC technology platform, MRG006A specifically targets GPC3-positive tumor cells, releasing toxins within the tumor to effectively kill cancer cells. HCC is a widely prevalent malignant tumor, with most patients diagnosed at advanced stages. After first-line treatment failure, options for subsequent therapies and their efficacy are limited. In this context, the innovative ADC drug MRG006A, which targets the GPC3-specific site associated with liver cancer, has attracted significant attention. According to a report, at the "GPC3-AD Hepatocellular Carcinoma Expert Advisory Meeting" on July 15, Zhao Hong, an attending physician at the Hepatobiliary Surgery Department of the Chinese Academy of Medical Sciences Cancer Hospital, stated in an interview, "GPC3 is an oncogenic embryonic antigen involved in cell proliferation, differentiation, migration, and apoptosis. It is almost not expressed in normal tissues but is highly expressed in 70%-80% of hepatocellular carcinoma cases, making it a 'golden' target for precise targeting of liver cancer cells." He noted that "the innovative value of the clinical-phase ADC drug MRG006A is also reflected in the technological breakthroughs it represents." Dr. Zhao explained that MRG006A, developed on the Hi-TOPi technology platform, operates like an "accurately guided missile"—utilizing monoclonal antibodies targeting GPC3 as a "navigation system" to precisely locate liver cancer cells, while a payload containing the cytotoxic drug (topoisomerase I inhibitor) serves as the "warhead" to achieve specific destruction of tumor cells. This mechanism retains strong anti-tumor effects while reducing damage to normal cells due to its targeting capability, addressing the high toxicity issues associated with traditional cytotoxic drugs. Clinical data indicate that adverse reactions primarily involve abnormal liver function (elevated bilirubin and transaminases) and mild bone marrow suppression which are overall manageable, further validating the feasibility of its clinical application. From the perspective of clinical progress, MRG006A has shown significant potential. Huang Zhen, an associate chief physician at the Hepatobiliary Surgery Department of the Chinese Academy of Medical Sciences Cancer Hospital, mentioned, "In the Phase I clinical trial, the dose escalation study achieved results beyond expectations. Among the dose groups, two GPC3-positive patients showed significant tumor shrinkage after enrollment, and the treatment effect is encouraging." The advancement of this Phase II clinical trial for MRG006A not only marks an important breakthrough in the development of LEPU BIO's ADC pipeline but also holds promise to fill the clinical gap in the treatment of liver cancer.