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CS5006 is a first-in-class antibody-drug conjugate (ADC) developed by CStone Pharmaceuticals. It targets integrin β4 (ITGB4), a transmembrane protein overexpressed in several solid tumors, including non-small cell lung cancer (NSCLC), colorectal cancer, esophageal squamous cell carcinoma (ESCC), and head and neck squamous cell carcinoma (HNSCC). ITGB4 is associated with tumor aggressiveness and poor prognosis. The ADC consists of a monoclonal antibody against ITGB4 conjugated to cytotoxic payloads via proprietary linkers—specifically GGFG-DXd or VC-MMAE—enabling targeted delivery of the cytotoxin to tumor cells. Preclinical studies have demonstrated potent antigen-dependent cytotoxicity, robust antitumor activity in vitro and in vivo models, favorable pharmacokinetics, and good tolerability. As of June 2025, CS5006 remains in preclinical development with an IND application anticipated for 2025[1][2][3][5][7].
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