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Review
. 2018;11(3):200-208.
doi: 10.2174/1874471011666180502104524.

An Overview of Targeted Alpha Therapy with 225Actinium and 213Bismuth

Alfred Morgenstern  1 , Christos Apostolidis  1 , Clemens Kratochwil  2 , Mike Sathekge  3 , Leszek Krolicki  4 , Frank Bruchertseifer  1
Affiliations
Review

An Overview of Targeted Alpha Therapy with 225Actinium and 213Bismuth

Alfred Morgenstern et al. Curr Radiopharm. 2018.

Abstract

Background: Recent reports of the remarkable therapeutic efficacy of 225Ac-labeled PSMA- 617 for therapy of metastatic castration-resistant prostate cancer have underlined the clinical potential of targeted alpha therapy.

Objective and conclusion: This review describes methods for the production of 225Ac and its daughter nuclide 213Bi and summarizes the current clinical experience with both alpha emitters with particular focus on recent studies of targeted alpha therapy of bladder cancer, brain tumors, neuroendocrine tumors and prostate cancer.

Keywords: Targeted alpha therapy; actinium-225; alpha emitter; bismuth-213; clinical application; nuclide production..

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Figures

Fig. (1)
Fig. (1)
Decay chain of 233U.
Fig. (2)
Fig. (2)
68Ga-DOTATOC PET/CT image of a patient with recurrent glioblastoma after co-injection of 10 MBq 68Ga-[Thi8,Met(O2)11]-substance P and 1.7 GBq 213Bi-[Thi8,Met(O2)11]-substance P. The image taken at 1 hour post injection shows high retention of the radiolabelled compound in the tumor area, with some residual activity remaining in the catheter system.
Fig. (3)
Fig. (3)
Magnetic resonance images of a patient with grade III glioma showing excellent response to locoregional treatment with 8 cycles of 213Bi-Substance P analogue with a cumulative activity of 14.1 GBq (2 months after first therapy (A); 8 months after 8th therapy (B); 33 months after 8th therapy (C)).
Fig. (4)
Fig. (4)
68Ga-DOTATOC PET/CT images of a patient with a multi-resistant neuroendocrine tumor showing partial response after two treatment cycles with 16 MBq (1st cycle) and 42 MBq (2nd cycle) 225Ac-DOTATOC. (A): before therapy (Oct 2011); (B): 4 months after first therapy with 16 MBq 225Ac-DOTATOC (Feb 2012); (C): 3 months after second therapy with 42 MBq 225Ac-DOTATOC (May 2012).
Fig. (5)
Fig. (5)
Excellent response to therapy after 2 cycles of 225Ac-PSMA-617 demonstrated by 68Ga-PSMA-11 PET/CT images of patient with metastatic castration-resistant prostate cancer before (left panel) and after (right panel), with decrease in serum PSA level from 1,301 to <0.05 ng/mL. The patient was treated at Steve Biko Academic Hospital, Pretoria, with two cycles of 225Ac-PSMA-617 with a cumulative activity of 14 MBq.
See this image and copyright information in PMC

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