Table 2.

Isotopes and relevant characteristics for PSMA-targeted radionuclides.

Isotopes	Agents	Imaging/therapeutic properties	Half-lives	Stage	Strengths	Limitations
Commonly used
111In	111In-PSMA-I&T; 111In-PSMA-617	Imaging-PSMA-RGS	2.83 d	Clinical trial	Earliest used agents	Suboptimal nuclear properties, high cost, and limited availability of 111InCl3
99mTc	111In-PSMA-I&S	Imaging-PSMA-RGS	6.02 h	Clinical trial	Optimal nuclear properties, lower cost, and easily available	Inferior ability in pre-operative imaging, compared with PET/CT
177Lu	177Lu-PSMA-617; 177Lu-PSMA-I&T	Beta-therapy	6.65 d	Clinical trial	Most widely used agents for therapy of CRPC	Heterogeneous PSMA expression after ADT
225Ac	225Ac-PSMA-617	Alpha-therapy	10.00 d	Clinical trial	Higher level of radiobiologic effectiveness when compared with Beta-therapy	Heterogeneous PSMA expression after ADT
18F	18F-DCFPyL	PET/CT	110 min	FDA approved 2021	High resolution	Relatively limited availability
68Ga	68Ga-PSMA-I&T; 68Ga-PSMA-11	PET/CT	6.7 h	FDA approved 2020 (PSMA-11)	High resolution	Relatively limited availability
Uncommonly used
44Sc	44Sc-PSMA-617	PET/CT	3.93 h	Clinical trial	More appropriate for delayed imaging	——
64Cu	64Cu-CA003; 64Cu-CA003	PET/CT	12.7 h	Preclinical	——	Instability of 64Cu complexes in vivo
89Zr	89Zr-PSMA-DFO	PET/CT	78.4 h	Clinical trial	Localize lesions with weak PSMA expression	——
131I	131I-MIP-1095	Beta-therapy	8.02 d	Clinical trial	A potential alternative to 177Lu-PSMA	——
161Tb	161Tb-PSMA-617	Alpha-therapy	7.90 d	Preclinical	A potential alternative to 177Lu-PSMA	——
165Er	165Er-PSMA-617	Alpha-therapy	10.40 h	——	——	——
212Pb	212Pb-CA012	Alpha-therapy	10.64 h	Preclinical	A potential alternative to 225Ac-PSMA	——
213Bi	213Bi-PSMA-617; 213Bi-PSMA I&T; 213Bi-JVZ-008	Alpha-therapy	45.59 min	Clinical trial	A potential alternative to 225Ac-PSMA	——
227Th	227Th-PSMA-TTC (BAY 2315497)	Alpha-therapy	18.70 d	Preclinical	Synergistic antitumor efficacy in combination with darolutamide	——