Development of novel radiopharmaceuticals for the diagnosis and treatment of cancer

The abundant expression of the gastrin releasing peptide receptor (GRPR) in many frequently occurring human cancers provides the opportunity to use radiolabeled bombesin receptor antagonists, interesting for not eliciting adverse effects after intravenous injection, for tumor visualization and treatment. This article reports the design, synthesis and biological evaluation of three radiopharmaceutical compounds, based on the GRPR-antagonist JMV594, with an increasing number of β-alanine residues in the spacer sequence and coupled to the chelator DOTA. This study aimed to determine the best linker length to optimize the biological properties. (authors)