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Targeting the prostate-specific membrane antigen (PSMA) using lutetium-177-labeled PSMA-specific tracers has become a very promising novel therapy option for prostate cancer (PCa). The efficacy of this therapy might be further improved by replacing the β-emitting lutetium-177 with the α-emitting actinium-225. Actinium-225 is thought to have a higher therapeutic efficacy due to the high linear energy transfer (LET) of the emitted α-particles, which can increase the amount and complexity of the therapy induced DNA double strand breaks (DSBs). Here we evaluated the relative biological effectiveness of [ 225 Ac]Ac-PSMA-I&amp;T and [ 177 Lu]Lu-PSMA-I&amp;T by assessing in vitro binding characteristics, dosimetry, and therapeutic efficacy.

In vitro dose effect relationships of actinium-225- and lutetium-177-labeled PSMA-I&T