Development of therapeutic radiopharmaceutical of 90Y-DOTA-[Pro1, Tyr4]-bombesin : a preliminary study

Name: Wiranee Sriwiang

Organization : Thailand Institute of Nuclear Technology (Public Organization). Research and Development Division

Email : wiranee@tint.or.th

Name: Sudkhanung Phumkhem

Organization : Thailand Institute of Nuclear Technology (Public Organization). Radioisotope Center

Name: Tippanan Ngamprayad

Organization : Thailand Institute of Nuclear Technology (Public Organization). Radioisotope Center

ThaSH: Radiopharmaceuticals

ThaSH: Medical radiology

ThaSH: Prostate -- Cancer -- Treatment

Abstract: Overexpression of peptide hormone receptors on cancer cell surface is useful for specific targeting by diagnostic or therapeutic medical agents. Gastrin Releasing Peptide Receptors (GRPRs) are transmembrane protein receptors distributed in central nervous system, gastrointestinal tract and predominantly overexpressed on the prostate and breast human cancer cells. This study aimed to develop a therapeutic radiopharmaceutical for prostate cancer treatment by radiolabeling the bombesin peptide analogue, DOTA-[Pro1, Tyr4]-bombesin, with a beta-emitting radionuclide, 90Y. The optimum condition that yielded the highest radiochemical purity (RCP) was studied and validated. The RCP of the labelled product, 90Y-DOTA-bombesin (90Y-DTBBN), was >95 percent and stable for more than 24 hours at 37 degrees without loss of free 90Y from the labelled complex. However, the percentage of degradation products of 90Y-DTBBN increased with time and activity of 90Y. Diluting the labelled product and adding the antioxidant were performed to reduce the degradation of peptide caused by the high-energy beta radiation of 90Y. Biodistribution of the labelled peptide was tested in normal mice with blocked and unblocked GRP receptors. Radioactivity count rate of the mice with blocked receptors was decreased about 4 times compared to the mice with unblocked receptors. This result indicated that the radiopharmaceutical of 90Y-DTBBN is specific binding to the GRPs receptors and has potential to further study as a therapeutic radiopharmaceutical for prostate cancer.

King Mongkut's University of Technology North Bangkok. Central Library

Address: BANGKOK

Email: library@kmutnb.ac.th

Created: 2020

Modified: 2024-10-17

Issued: 2024-10-17

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BibliograpyCitation : In the Chemical Society of Thailand under the Patronage of Professor Dr. HRH Princess Chulabhorn in association, Thammasat University Faculty of Science and Technology. The Pure and Applied Chemistry International Conference 2020 (PACCON 2020) (OM16-21). Bangkok : Thammasat University

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