Abstract: A radioactive labeled long-acting peptide-targeting pharmaceutical and production method, in which the peptide targeted pharmaceutical is firstly dissolved in a solution, followed by labeling the radioactive at a high temperature, and the dosage of the pharmaceutical with radioactive labeling is expected to be reduced and labeling efficiency is improved, and no further purification by filtration is required, which shortens the preparation process and reduces personnel exposure in the working environment. The radioactive labeled long-acting peptide-targeting pharmaceutical can increase the specific binding capacity of tumors and reduce the non-specific accumulation in normal tissues. It can be applied to the field of tumor and nuclear medicine for diagnosis and treatment of tumors and/or tumor metastases with efficacy and precision treatment.

Abstract: A PSMA targeting peptide derivative for radiotherapy, which is a structural molecule developed for diagnosis or treatment of prostate cancer, as prostate-specific membrane antigen (PSMA) is a protein present on the surface of healthy prostate cells, which is often at a high level of expression on the surface of prostate cancer cells, and the molecular composition of PSMA inhibitor is mainly composed of glutamic acid, urea and lysine, in addition to the linker of the present invention, PSMA inhibitor can be combined with a chelating agent and truncated Evans Blue, which can be labeled with radionuclides Ga-67, Ga-68, In-111, Lu-177, Cu-64 or Y-90, used for image analysis and analysis of human prostate cancer tumor pattern as a new PSMA targeting peptide receptor radionuclide therapy (PRRT), and which has a longer half-life in vivo and is featured by specific binding of PSMA for radiotherapy diagnosis or treatment.