Fig. 5.

In vitro and in vivo therapeutic efficacy of PSMA-targeted radioligands. a In vitro cell kill effect of ¹⁷⁷Lu-PSMA-617, ¹⁷⁷Lu-PSMA I&T, ¹⁷⁷Lu-L1 and ¹⁷⁷Lu-L3 after 48 h incubation in PSMA(+) PC3 PIP and PSMA(−) flu cells (data mean ± SD, n = 3) at37 °C. b Effect of ¹⁷⁷Lu-PSMA-617 (n = 9), ¹⁷⁷Lu-L1,¹⁷⁷Lu-L3 and ¹⁷⁷Lu-L5 (n = 10) on the PSMA(+) PC3 PIP tumor growth (data mean ± SD) after administration of 111 MBq via tail-vein injection. c Kaplan−Meier plot of survival for the group treated with ¹⁷⁷Lu-PSMA-617 (n = 9) and ¹⁷⁷Lu-L1 (n = 10), censored event (dot), three mice were removed from each group at 8 weeks for evaluating acute toxicity. d Hemoglobin and blood counts (white blood cells, neutrophil and platelets) level after 8-week. Data are mean ± SD (n = 3). e and f Acute toxicity evaluation by H&E staining of lacrimal glands and testes. Extraorbital lacrimal glands control untreated (left); ¹⁷⁷Lu-PSMA-617(middle and right), adjacent parotid gland (arrowhead) is spared (middle); higher magnification, showing acinar loss, with chronic and active inflammation (right). Testis control untreated, active spermatogenesis, near the rete testis 2 tubules (arrowhead) contain only Sertoli cells (left), ¹⁷⁷Lu-PSMA-617 (right). Diffuse and near complete loss of seminiferous epithelium, with prominent interstitial cells