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YL242 + 5-fluorouracil + leucovorin is a combination therapy regimen being evaluated for the treatment of various advanced solid tumors. YL242 is an antibody-drug conjugate (ADC) developed by MediLink Therapeutics using its proprietary TMALIN (Tumor Microenvironment Activable LINker-payload) technology. It targets Vascular Endothelial Growth Factor (VEGF) and consists of an anti-VEGF antibody conjugated to a novel DNA topoisomerase I inhibitor payload via a protease-cleavable tripeptide linker. The combination includes 5-fluorouracil (5-FU), a pyrimidine analog antimetabolite that inhibits thymidylate synthase and incorporates into RNA and DNA, and leucovorin (LV), which stabilizes the binding of 5-FU to its target. This therapeutic approach combines anti-angiogenic effects and targeted cytotoxic delivery from the ADC with the established chemotherapeutic activity of the 5-FU/LV backbone to treat cancers such as colorectal, gastric, and non-small cell lung cancer.
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