Shanghai, China, October 12^th, 2021 – Shanghai Henlius Biotech, Inc. (2696.HK) announced that the first subject has been dosed with HLX26 (recombinant anti-LAG-3 human monoclonal antibody injection) for the Phase 1 clinical trial in patients with advanced/metastatic solid tumours or lymphomas. Lymphocyte-activation gene 3 (LAG-3) is an immune checkpoint receptor and is regarded as a new generation of immunotherapy target after PD-1/L1 and CTLA-4. There is no product approved for this target around the globe. Clinical studies show that LAG-3 inhibitors are effective against lung cancer, breast cancer, melanoma, head and neck cancer, and hematological malignancy. Clinical studies reveal that LAG-3 inhibitors are effective against lung cancer, breast cancer, melanoma, head and neck cancer, and hematological malignancy. In a Phase 3 clinical study, the LAG-3 inhibitors in conjunction with the PD-1 inhibitor magnify the synergistic immune response effects. Recently, the study-related Biologics License Application has been accepted by the FDA, demonstrating the promising prospect of this product.

LAG-3 is mainly expressed on human immune cells, including activated T cells and part of NK cells, and negatively regulates T cells' proliferation, activation, and homeostasis^-1. HLX26 is a human mAb targeting LAG-3 extracellular domains, can block the LAG-3-mediated signalling pathway to restore the killing function of T-cell. Pre-clinical studies have proved that HLX26 has the anti-tumour effect and favourable tolerability and safety. HLX26 in combination with Henlius' proprietary anti-PD-1 mAb serplulimab creates synergistic effects in anti-tumour. These results lay the foundation for further clinical studies. HLX26 is expected to play an essential role in treating solid tumours and lymphomas and expand the company's therapeutic area.

Underpinned by the patient-centric strategy, Henlius has achieved an overall layout of the immune checkpoint products of PD-1/L1, CTLA-4, LAG-3, etc., proactively exploring immuno-oncology combination therapy. The company has also built an innovative product pipeline with many emerging targets, including c-MET, LAG-3, TROP2, BRAF, etc. and has been developing a forward-looking presence in bispecific antibodies and the antibody-drug conjugates (ADC), committing to bringing affordable and high-quality innovative biologics to patients around the world.

This is an open-label, dose-escalation, first-in-human Phase 1 study which aims to evaluate the safety, tolerability and pharmacokinetic characteristics of HLX26 in patients with advanced/metastatic solid tumours or lymphomas. Eligible patients are enrolled and given different doses of HLX26 intravenously following accelerated titration and 3+3 dose-escalation design. The primary endpoints of this study are the dose-limiting toxicity (DLT) and maximum tolerated dose (MTD) determined within three weeks after the initial dose. The secondary endpoints include adverse events, pharmacokinetic parameters, immunogenicity and preliminary efficacy outcomes.

Henlius (2696.HK) is a global biopharmaceutical company with the vision to offer high-quality, affordable and innovative biologic medicines for patients worldwide with a focus on oncology, autoimmune diseases and ophthalmic diseases. Up to date, 3 products have been launched in China, 1 in the European Union (EU), the New Drug Applications (NDAs) of 3 products accepted for review in China. Since its inception in 2010, Henlius has built an integrated biopharmaceutical platform with core capabilities of high-efficiency and innovation embedded throughout the whole product life cycle including R&D, manufacturing and commercialisation. It has established global R&D centres and a Shanghai-based manufacturing facility certificated by China and the EU Good Manufacturing Practice (GMP).

Henlius has proactively built a diversified and high-quality product pipeline covering over 20 innovative monoclonal antibodies (mAbs) and has continued to explore immuno-oncology combination therapies with proprietary serplulimab (anti-PD-1 mAb) as backbone. Apart from the launched products 汉利康^® (rituximab), the first China-developed biosimilar, 汉曲优^® (trastuzumab, Zercepac^® in the EU), the first China-developed mAb biosimilar approved both in China and in the EU and 汉达远^® (adalimumab), the Company's first product indicated for autoimmune diseases, the NDA of innovative product serplulimab indicated for MSI-H solid tumors has been granted priority review, and the NDAs of HLX04 (bevacizumab), HLX01 (rituximab) for the treatment of rheumatoid arthritis and serplulimab for the treatment of squamous non-small cell lung cancer are also under review. What's more, Henlius has conducted over 20 clinical studies for 11 products and 8 combination therapies worldwide, expanding its presence in major market as well as emerging market.