The application of prostate-specific membrane antigen (PSMA)-targeted α-therapy is a promising alternative to β^(-)-particle-based treatments. ^(211)At is among the potential α-emitters that are favorable for this concept. Herein, ^(211)At-based PSMA radiopharmaceuticals were designed, developed, and evaluated. Methods: To identify a ^(211)At-labeled lead, a surrogate strategy was applied. Because astatine does not exist as a stable nuclide, it is commonly replaced with iodine to mimic …