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Belrestotug is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that targets TIGIT (T cell immunoreceptor with Ig and ITIM domains), an immune checkpoint receptor expressed on T cells and natural killer cells. By antagonizing TIGIT, belrestotug is designed to enhance antitumor immune responses through multiple mechanisms including blocking the inhibitory TIGIT pathway, stimulating T lymphocyte activity via the CD226 pathway, and inducing antibody-dependent cellular cytotoxicity (ADCC) through FcγR engagement. Developed as an immunotherapy for cancer—primarily non-small cell lung cancer and head and neck squamous cell carcinoma—it was investigated in combination with other checkpoint inhibitors such as dostarlimab. The development program was discontinued in May 2025 after phase II/III trials failed to meet efficacy criteria[2][4][5][6].
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