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5-FU + pembrolizumab is a combination regimen consisting of the fluoropyrimidine chemotherapy agent fluorouracil (5-FU) and the immune checkpoint inhibitor pembrolizumab. Fluorouracil is a small molecule that acts as a thymidylate synthase inhibitor, disrupting DNA and RNA synthesis to inhibit cancer cell proliferation. Pembrolizumab is a humanized IgG4 monoclonal antibody that targets the programmed death-1 (PD-1) receptor on T cells, preventing its interaction with PD-L1 and PD-L2 ligands, thereby restoring the anti-tumor immune response. This combination is being investigated in neoadjuvant settings, such as for locally advanced rectal cancer, often in conjunction with radiotherapy or as part of personalized treatment strategies guided by tumor organoid sensitivity testing.
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