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Anti-CTLA4 monoclonal antibodies (mAbs) are a class of immune checkpoint inhibitors that target the Cytotoxic T-Lymphocyte-Associated Antigen 4 (CTLA-4) receptor, also known as CD152. CTLA-4 is a protein receptor that functions as an immune checkpoint, downregulating immune responses by competing with the costimulatory receptor CD28 for binding to ligands CD80 (B7-1) and CD86 (B7-2) on antigen-presenting cells. By blocking the CTLA-4 signaling pathway, these antibodies enhance T-cell activation, proliferation, and anti-tumor effector functions. Ipilimumab (Yervoy) was the first-in-class anti-CTLA4 mAb to receive regulatory approval, followed by others like tremelimumab. These agents are used as monotherapy or in combination with PD-1/PD-L1 inhibitors for various malignancies, including melanoma, non-small cell lung cancer, and renal cell carcinoma.
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