Development of a method for preparing octreotide derivative for diagnosis of neuroendocrine tumors

M. S. Larkina, E. V. Podrezova, O. D. Bragina, E. A. Tagirova, V. I. Chernov, M. S. Yusubov, E. A. Nesterov, V. S. Skuridin, S. V. Krivoshchekov, E. A. Yanovskaya, R. V. Gurto, M. V. Belousov

Research output: Contribution to journalArticlepeer-review


Currently the development of technologies for labeling somatostatin with technetium-99m for diagnosing radionuclide neuroendocrine tumors is under way. Somatostatin analogues are binded with technetium- 99m only by the preliminary addition of a chelating agent. Therefore, it is important to develop a method for preparation of an octreotide derivative by modifying octreotide with precursors: ligands with high chelating ability for its tight binding with technetium-99m. ω-Bis(pyridin-2-ylmethyl)amino)aliphatic acids can be used successfully as such precursors. The purpose of the study was to develop a method for obtaining a new octreotide derivative for diagnosing neuroendocrine tumors. Materials and methods. The somatostatin octreotide analogue was used as the object of the study; succinimid-1-yl 6-(bis(pyridin-2-ylmethyl)amino)hexanoate was used as a chelating agent. Methods of high performance liquid chromatography and mass spectrometry were used to separate and analyze the synthesized compounds. Results. A method to produce an original octreotide derivative using a succinimid-1-yl 6-(bis(pyridin- 2-ylmethyl)amino)hexanoate as a chelating agent was proposed. The conditions of analytical and semipreparative HPLC for the analysis and purification of the active octreotide derivative (a monosubstituted derivative of the amino acid residue of D-phenylalanine) were suggested. Conclusion. The synthesized derivative of octreotide has a chelating center for strong binding to technetium-99m in its structure, which can be useful for diagnosing neuroendocrine tumors.

Original languageEnglish
Pages (from-to)72-80
Number of pages9
JournalBulletin of Siberian Medicine
Issue number3
Publication statusPublished - 2019


  • Chelating agent
  • Neuroendocrine tumors
  • Octreotide
  • Somatostatin receptors
  • Technetium-99m

ASJC Scopus subject areas

  • Molecular Medicine

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