The invention belongs to the technical field of radiopharmaceutical
chemistry, and particularly relates to a
programmed death ligand-1 (PD-L1) targeted radioactive polypeptide probe as well as a preparation method and application thereof. The PD-L1 targeted radioactive polypeptide probe structurally comprises a PD-L1 targeted polypeptide ligand, a targeted / metabolic functional regulating group, a
radionuclide chelating group and a
radionuclide (such as 68Ga). According to the radioactive polypeptide probe provided by the invention, on the basis of a PD-L1 targeted polypeptide motif, a chelating group is introduced to
label radionuclide, and the radioactive polypeptide probe is mainly used for diagnostic imaging. And a functional regulating group, namely a 5-(
trifluoromethyl)
pyridine-3-
carboxylic acid group, is inserted for improving targeting and
in vivo metabolism. The radioactive polypeptide probe has excellent
tumor targeting property and remarkable tumor
retention capacity, shows good in-vivo stability and pharmacokinetic characteristics, and is easy to synthesize. The method can help to screen potential benefited patients of the PD-1 / PD-L1
immunotherapy, and can quickly and accurately monitor real-time and dynamic changes of PD-L1 in the tumor
immunotherapy process so as to predict and evaluate the effect of the PD-1 / PD-L1
immunotherapy.