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Anti-human CTLA-4 refers to a class of monoclonal antibodies designed to target and inhibit the human cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), a key immune checkpoint molecule. CTLA-4 is expressed on T cells and acts as a negative regulator of T-cell activation by competing with the costimulatory receptor CD28 for binding to B7 ligands (CD80 and CD86) on antigen-presenting cells. By blocking this interaction, anti-human CTLA-4 antibodies enhance T-cell priming, proliferation, and effector function, while also potentially depleting immunosuppressive regulatory T cells (Tregs) within the tumor microenvironment. This therapeutic platform includes the first-in-class agent ipilimumab and the later-approved tremelimumab, which are used primarily in oncology to treat various solid tumors, often in combination with PD-1/PD-L1 inhibitors. Investigational efforts in this space include the development of next-generation antibodies with enhanced Fc-mediated effector functions, tumor-selective activation (e.g., masked antibodies), and bispecific formats to improve efficacy and reduce the incidence of systemic immune-related adverse events.
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