A freeze-dried kit formulation for the preparation of Lys(27)(99mTc-EDDA/HYNIC)-Exendin(9-39)/99mTc-EDDA/HYNIC-Tyr3-Octreotide to detect benign and malignant insulinomas

Nucl Med Biol. 2015 Dec;42(12):911-6. doi: 10.1016/j.nucmedbio.2015.08.001. Epub 2015 Aug 8.

Abstract

About 90% of insulinomas are benign and 5%-15% are malignant. Benign insulinomas express the glucagon-like peptide-1 receptor (GLP-1R) and low levels of somatostatin receptors (SSTR), while malignant insulinomas over-express SSTR or GLP-1R in low levels. A kit for the preparation of Lys(27)((99m)Tc-EDDA/HYNIC)-Exendin(9-39)/(99m)Tc-EDDA/HYNIC-Tyr(3)Octreotide was formulated to detect 100% of insulinomas. The formulation showed radiochemical purity of 97±1%, high stability in human serum, and GLP-1R and SSTR affinity. The biodistribution and imaging studies demonstrated properties suitable for its use as a target-specific agent for the simultaneous molecular imaging of GRP-1R- and/or SSTR-positive tumors.

Keywords: Glucagon-like peptide 1 receptor; Insulinomas; Lys(27)((99m)Tc-EDDA/HYNIC)-Exendin(9-39); Somatostatin receptor.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Edetic Acid / analogs & derivatives*
  • Edetic Acid / chemistry
  • Freeze Drying
  • Humans
  • Insulinoma / diagnostic imaging*
  • Insulinoma / pathology
  • Male
  • Mice
  • Mice, Nude
  • Organotechnetium Compounds / chemistry*
  • Organotechnetium Compounds / pharmacokinetics*
  • Pancreatic Neoplasms / diagnostic imaging*
  • Pancreatic Neoplasms / pathology
  • Radiochemistry
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats
  • Tissue Distribution
  • Tumor Cells, Cultured

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • EDDA
  • Edetic Acid