Despite the success of the theranostic pair of [68Ga]Ga-PSMA-11 and [177Lu]Lu-PSMA-617 in clinical trials and practice, further chemical modifications are required to alleviate side effects while improving the treatment efficacy because (1) the performance of [68Ga]Ga-PSMA-11 in prostate cancer local recurrence is suboptimal due to its rapid in vivo kinetics and high renal uptake, and (2) [177Lu]Lu-PSMA-617 is more tuned for radionuclide therapy with slower in vivo kinetics to enhance tumor uptake and lower renal accumulation to reduce the kidney toxicity [65,66]. Here, FOLH1 is linked to prostate carcinoma.