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Review

Advances in radiolabeled antibody technology: optimization strategies for precision medicine.

Oct 2026 · International journal of pharmaceutics · pp. 127497 · 0 citations · 96 references
Medicine

Abstract

Radiolabeled antibody technology couples radionuclides with the target specificity of antibodies and has become an important platform for tumor imaging and therapy. However, its clinical application still faces multiple challenges. For example, production challenges include low radiochemical yield, poor homogeneity, and limited product stability. In addition, biological challenges include nonspecific accumulation, which results from unfavorable pharmacokinetics and the mismatch between the half-lives of radionuclides and antibodies. This review summarizes optimization strategies aimed at improving product quality and reducing nonspecific accumulation. These approaches include optimization basic parameters, site-specific conjugation, development of novel chelators, antibody engineering, Fc-region modification, and pretargeting strategies. Collectively, these studies demonstrate that synergistic multi-strategy optimization has substantially improved the targeting specificity and safety of radioimmunoconjugates while reducing their non-specific accumulation. With continued advances in radionuclide-labeled antibody technology, progressive refinement of regulatory frameworks and standards, and implementation of patient-specific dosimetry, this field is expected to play an increasingly pivotal role in precision medicine.

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