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Pembrolizumab is a humanized monoclonal IgG4 kappa antibody that functions as an immune checkpoint inhibitor targeting the programmed cell death protein 1 (PD-1) receptor on lymphocytes. By binding to PD-1 and blocking its interaction with ligands PD-L1 and PD-L2, pembrolizumab prevents the inhibitory signaling that normally dampens T-cell activity. This blockade enhances T-cell–mediated immune responses against tumor cells, allowing the immune system to recognize and destroy cancer cells more effectively. Pembrolizumab was developed by Merck & Co and first approved in 2014 for metastatic melanoma; it has since been approved for a wide range of cancers including non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma, classical Hodgkin lymphoma, urothelial carcinoma (bladder cancer), renal cell carcinoma, colorectal cancer with microsatellite instability or mismatch repair deficiency, gastric cancer, esophageal cancer, cervical cancer, endometrial carcinoma, hepatocellular carcinoma (HCC), biliary tract cancers (BTC), triple-negative breast cancer (TNBC), Merkel cell carcinoma (MCC), cutaneous squamous cell carcinoma (CSCC), primary mediastinal large B-cell lymphoma (PMBCL) and others.
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