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YL201 is an investigational antibody-drug conjugate (ADC) targeting B7-H3 (CD276), a transmembrane glycoprotein overexpressed in various solid tumors. Developed by MediLink Therapeutics using its proprietary TMALIN (Tumor Microenvironment Activable LINker-payload) platform, YL201 consists of a human anti-B7-H3 monoclonal antibody conjugated to a camptothecin-derived topoisomerase 1 inhibitor payload. The drug features a high drug-to-antibody ratio (DAR) of 8 and utilizes a protease-cleavable linker designed for a dual-release mechanism, allowing for payload cleavage both extracellularly within the tumor microenvironment and intracellularly within lysosomes. YL201 is currently being evaluated in Phase I/II clinical trials for advanced solid tumors, including metastatic castration-resistant prostate cancer (mCRPC), small cell lung cancer (SCLC), and non-small cell lung cancer (NSCLC). Roche has secured exclusive global rights for the development and commercialization of YL201 outside of mainland China, Hong Kong, and Macau.
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