Objective: To systematically review recent advances in the pharmacotherapy of Graves’ disease (GD) and provide evidence-based recommendations for individualized clinical management. Methods: We conducted a comprehensive literature search of PubMed, Cochrane Library, and CNKI databases for studies published within the past ten years focusing on antithyroid drugs (ATDs), biologics, and small-molecule targeted therapies. Results: Traditional ATDs remain first-line therapy for GD; however, relapse rates following discontinuation approach 50%. Novel targeted therapies—including anti-CD20 monoclonal antibodies (rituximab), anti-CD40 monoclonal antibodies (iscalimab), and neonatal Fc receptor (FcRn) antagonists—have demonstrated potential in reducing thyrotropin receptor antibody (TRAb) titers and improving remission rates in refractory GD. TSH receptor (TSHR) blocking antibodies and small-molecule antagonists represent promising etiological treatment strategies. Conclusion: GD pharmacotherapy is transitioning from empirical immunosuppression to precision-targeted interventions. Future therapeutic paradigms should emphasize individualized treatment protocols and discontinuation strategies guided by dynamic TRAb monitoring.
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