<p>The development of antibody–drug conjugates for cancer therapy has shown great potential in improving targeted treatment efficacy. This study explores the conjugation of daratumumab, a monoclonal antibody targeting CD38, with protoporphyrin IX and subsequent radiolabeling with terbium-161 (<sup>161</sup>Tb) for potential use as a targeted immunotherapeutic agent in multiple myeloma. The conjugation process involves stable linkage to retain the therapeutic properties of daratumumab, and <sup>161</sup>Tb radiolabeling offers enhanced cytotoxicity through localized beta-emission and Auger electron effects. In vitro studies demonstrate significant inhibition of myeloma cell growth and increased apoptosis, providing a foundation for further preclinical investigation of this conjugate as a targeted radionuclide therapy in hematologic malignancies.</p>

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Radiolabeling of protoporphyrin-daratumumab conjugate with 161Tb as a CD38 immunotherapeutic agent for multiple myeloma

  • Mohamed A. Gizawy,
  • Hanan M. El-Shershaby,
  • E. H. Borai,
  • Hesham A. Shamsel-Din

摘要

The development of antibody–drug conjugates for cancer therapy has shown great potential in improving targeted treatment efficacy. This study explores the conjugation of daratumumab, a monoclonal antibody targeting CD38, with protoporphyrin IX and subsequent radiolabeling with terbium-161 (161Tb) for potential use as a targeted immunotherapeutic agent in multiple myeloma. The conjugation process involves stable linkage to retain the therapeutic properties of daratumumab, and 161Tb radiolabeling offers enhanced cytotoxicity through localized beta-emission and Auger electron effects. In vitro studies demonstrate significant inhibition of myeloma cell growth and increased apoptosis, providing a foundation for further preclinical investigation of this conjugate as a targeted radionuclide therapy in hematologic malignancies.