On October 21, 2024 CStone Pharmaceuticals (stock code: 2616.HK), an innovation-driven biopharmaceutical company focused on the research and development of anti-cancer drugs, reported that the patent (WO/2024/208354) for the company’s independently developed antibody-drug conjugate (ADC) CS5006 was published on October 10, 2024 (Press release, CStone Pharmaceauticals, OCT 21, 2024, View Source [SID1234656226]).
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CS5006 is a first-in-class antibody-drug conjugate (ADC) with a novel target: integrin β4 (ITGB4). ITGB4 is a transmembrane protein that exclusively binds to integrin α6 (ITGA6) to form a heterodimer (α6β4), with laminin as its extracellular ligand. ITGB4 is considered a biomarker for various tumors, with elevated expression correlating with aggressiveness and poor prognosis. Using our in-house bioinformatics platform, combined with cutting-edge AI algorithms and comprehensive comparisons with published literature, we have identified ITGB4 as highly expressed in multiple indications, including non-small cell lung cancer, colorectal cancer, esophageal squamous cell carcinoma, and head and neck squamous cell carcinoma, making it an ideal candidate for targeted therapy.
During the development of CS5006, CStone Pharmaceuticals combined candidate monoclonal antibodies with clinically validated linkers and drug payloads, including GGFG-DXd and VC-MMAE, as model ADC molecules to support the project’s proof-of-concept studies. In vitro results demonstrated that both CS5006-GGFG-DXd and CS5006-VC-MMAE ADCs, upon internalization into tumor cells, efficiently released cytotoxins, rapidly killing tumor cells. In vivo results further validated the potent anti-tumor activity and expected tolerability of these two ADCs, providing strong data support for their next clinical development steps. Currently, CS5006 utilizes a proprietary linker and is nearing completion of preclinical candidate molecule (PCC) screening. An Investigational New Drug (IND) application is expected to be submitted in 2025.
Dr. Jianxin Yang, CEO, President of R&D, and Executive Director of CStone Pharmaceuticals, said, "The publication of the CS5006 patent not only demonstrates our innovative achievements in the ADC field, but also highlights CStone’s comprehensive capabilities from R&D to commercialization. We are excited about the clinical potential of CS5006 and other innovative ADC programs and hope they will bring groundbreaking treatment options to cancer patients worldwide."
CStone Pharmaceuticals is also actively developing next-generation linkers with proprietary intellectual property rights to enhance the hydrophilicity and tumor selectivity of currently used linkers, such as the GGFG tetrapeptide linker and the VA/C dipeptide linker. These novel linkers will maximize the safety and efficacy of ADCs, significantly increase the flexibility of linker adaptation for targets and antibody molecules, and support multiple ADC programs in CStone’s pipeline 2.0, including CS5005 targeting SSTR2, CS5006 targeting ITGB4, and CS5007 targeting EGFR/HER3.