The development and characterisation of novel bifunctional variants of the dicarboxylate analogue, HBED-CC, has been growing over the past decade since Eder and co-workers’ reported the conjugation of the PSMA-targeting motif, Glu-urea-Lys, to HBED-CC for the imaging of prostate cancer ([68Ga]Ga-HBED-CC-PSMA) in 2012 [31,77]. The gene discussed is FOLH1; the disease is prostate carcinoma.