Radiolabeled peptides are promising pharmaceuticals for cancer diagnosis and therapy. However, high kidney uptake of peptide radiopharmaceuticals is frequently observed due to specific and/or nonspecific interactions. High kidney uptake of radiopharmaceuticals hinders the detection of cancer lesions adjacent to kidneys, and reduces the therapeutic dose which can be safely administered into patients.
Our lab is developing a general strategy to minimize the accumulation of peptide radiopharmaceuticals in kidneys. The strategy utilizes linkers which can be cleaved by enzymes present in abundance in kidneys, and the facts that the radiolabeled fragments are not retained by kidneys. If successful, our strategy will greatly enhance detection sensitivity and therapeutic index of peptide radiopharmaceuticals.