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GenSci139 is a **bispecific antibody-drug conjugate (ADC)** targeting both the **epidermal growth factor receptor (EGFR)** and **human epidermal growth factor receptor 2 (HER2)**, conjugated to a potent **topoisomerase 1 inhibitor payload** (GSC5181), via a highly stable but cleavable linker. Developed using proprietary platform technologies by Changchun Genescience Pharmaceuticals, GenSci139 is designed to co-target EGFR and HER2, which are co-expressed in a range of solid tumors and often implicated in tumor growth, resistance, and recurrence. By dual targeting, GenSci139 aims to overcome resistance seen with HER2-only therapies and expand therapeutic benefit to HER2-low and EGFR/HER2–co-expressing cancers. Preclinical data demonstrate superior in vitro stability, tumor cell binding, internalization, cytotoxicity, and in vivo efficacy versus single-target comparators such as trastuzumab deruxtecan (DS-8201). The topoisomerase 1 inhibitor payload GSC5181 promotes DNA damage and apoptosis with demonstrated bystander killing effects. GenSci139 is in preclinical or early development for a range of solid tumors, including breast, lung, gastric, colorectal, ovarian, and urothelial cancers.
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