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Gastrin releasing peptide receptors (GRPRs) are over expressed in various types of cancer cells including prostate and breast cancer. Bombesin is an analogue of the mammalian GRP that binds with high specificity and affinity to GRPRs. Significant research efforts have been devoted to the design and radiolabel bombesin peptides for the diagnostic of prostatic and breast cancer using SPECT e PET, with radionuclides like In e Ga. The objective of this work was to study the labeling with In of a new bombesin series and evaluate the potential for diagnostic application using animal model. Several studies were evaluated to optimize the labelling conditions of BBN derivatives with In using different temperature, time, mass of peptide and radionuclide activity. High radiochemical purity and high specific activity were obtained for all the peptides labeled with 111-indium. Biodistribution studies in normal mices showed that the BBN derivative with Gly5 as aminoacidic spacer presented high uptake on pancreas and intestines that suggests that is the best peptide. Two DOTA-derivatives with Gly5 as spacer were radiolabelled with 68gallium and evaluated in tumor model animals of human prostatic cancer and showed high potential for clinical application in diagnostic procedures with PET.

Estudo da marcação com Indio-111 e Gálio-68 de derivados da bombesina e avaliação das propriedades biológicas para aplicação em SPECT e PET