Development of 4-hexadecyl-4,7-diaza-1,10-decanedithiol (HDD) kit for the preparation of the liver cancer therapeutic agent Re-188-HDD/lipiodol

Vinay Kumar Banka, Sung Hyun Moon, Jae Min Jeong, Sudhakara Reddy Seelam, Yun Sang Lee, Young Joo Kim, Dong Soo Lee, June Key Chung

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Introduction: A lipiodol solution of 188 Re-4-hexadecyl-2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol (HTDD) has been successfully developed for liver cancer therapy; however, its preparation requires a multi-step synthesis and it is characterized by a low labeling yield. Methods: We synthesized a new compound, 4-hexadecyl-4,7-diaza-1,10-decanedithioacetate (AHDD), without gem dimethyl groups to address these issues. AHDD was formulated into a kit and was labeled with 188 Re. Biodistribution study was performed using normal BALB/c mice. Results: The kit was labeled with 188 Re with a high efficiency (98.8±0.2%). After extraction with lipiodol, the overall yield of 188 Re-HDD/lipiodol was as high as 90.2±2.6%. A comparative biodistribution study of 188 Re-HTDD and 188 Re-HDD was performed in normal mice after intravenous injection. The lungs were identified as the main uptake site due to capillary-blockage. 188 Re-HDD/lipiodol showed a significantly higher lung uptake than that of 188 Re-HTDD/lipiodol (p<0.05). Conclusion: The newly synthesized 188 Re-HDD/lipiodol showed improved radiolabeling yield and biodistribution results compared to 188 Re-HTDD/lipiodol, and may therefore be more suitable for liver cancer therapy.

Original languageEnglish
Pages (from-to)317-322
Number of pages6
JournalNuclear Medicine and Biology
Issue number3
StatePublished - 1 Mar 2015


  • N2S2
  • Re
  • Rhenium
  • TACE
  • TAE
  • Transarterial embolism

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