Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging

Abstract

A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with 99mTc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined.