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These agents restore T cell\u2010mediated antitumor immune responses by targeting key immune checkpoint molecules, thereby suppressing or eliminating tumors. However, their clinical application still faces multiple challenges, mainly including efficacy heterogeneity, drug resistance, immune\u2010related adverse events. Furthermore, there is still a lack of reliable biomarkers for predicting efficacy and toxicity. More critically, there is absence of precise predictive models that can systematically integrate multiomics features, dynamic tumor microenvironment evolution, and patient individual differences to comprehensively address the above issues. This review systematically summarizes the latest advancements in this field. 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