By Fineline Cube 
Lepu Biopharma Co., Ltd. (HKG: 2157) announced today that it has successfully enrolled the first patient in the Phase II clinical study of its internally developed MRG006A, a next‑generation GPC3‑targeting Antibody‑Drug Conjugate (ADC) for advanced hepatocellular carcinoma (HCC). The milestone marks MRG006A as the world’s first GPC3‑directed ADC to enter Phase II development.
Key Announcements
| Item | Detail |
|---|---|
| First‑Patient Enrollment | 16 Oct 2025, Phase II study of MRG006A in advanced HCC |
| Technology Platform | Hi‑TOPi ADC, enabling precise tumor‑cell targeting and toxin release |
| Regulatory Status | IND approval by the National Medical Products Administration (NMPA) – July 2024 |
| Preclinical Profile | Significant tumor‑growth inhibition in CDX and HCC PDX models; favorable tolerability in toxicology studies |
About MRG006A
MRG006A couples a monoclonal antibody that binds specifically to Glypican‑3 (GPC3), a cell‑surface protein over‑expressed in >70 % of HCC tumors, with a potent cytotoxic payload. The ADC delivers the toxin directly into GPC3‑positive tumor cells, sparing healthy tissue and achieving high therapeutic indices. Leveraging Lepu’s proprietary Hi‑TOPi platform, MRG006A offers a refined linker chemistry that optimizes drug‑to‑antibody ratio and release kinetics.
Strategic Significance
- First‑Mover Advantage – No other GPC3‑targeted ADC has advanced beyond preclinical stages, positioning Lepu at the forefront of precision oncology for HCC.
- Pipeline Expansion – Successful Phase II data will support accelerated development of additional Hi‑TOPi ADC candidates across solid tumors.
- Market Opportunity – HCC remains a leading cause of cancer mortality worldwide; MRG006A addresses an unmet need for targeted, high‑efficacy therapy.
Forward‑Looking Statements
This release contains forward‑looking statements that involve risks and uncertainties. Actual results may differ materially.-Fineline Info & Tech