Comparison of the Biodistribution of <sup>225</sup>Ac and Radio-Lanthanides as Citrate Complexes

Beyer, G.J.; Bergmann, Ralf; Schomäcker, K.; Rösch, Frank; Schäfer, Gerhard; Kulikov, Evgeny Vladimirovich; Novgorodov, A.F.

doi:10.1080/10256019008624245

Cited by 25 publications

(25 citation statements)

References 4 publications

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“…The biodistribution of a mixed 225 Ac, 169 Yb and 148 Pm sodium citrate solution (pH 6.5) was examined in normal rats and mice bearing adenocarcinoma tumor implants [28]. The rats were injected i.v.…”

Section: Biological Studies In Animal Modelsmentioning

confidence: 99%

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

Scheinberg

McDevitt²

2011

CRP

146

114

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Alpha particle-emitting isotopes are being investigated in radioimmunotherapeutic applications because of their unparalleled cytotoxicity when targeted to cancer and their relative lack of toxicity towards untargeted normal tissue. Actinium-225 has been developed into potent targeting drug constructs and is in clinical use against acute myelogenous leukemia. The key properties of the alpha particles generated by 225Ac are the following: i) limited range in tissue of a few cell diameters; ii) high linear energy transfer leading to dense radiation damage along each alpha track; iii) a 10 day half-life; and iv) four net alpha particles emitted per decay. Targeting 225Ac-drug constructs have potential in the treatment of cancer.

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Section: Biological Studies In Animal Modelsmentioning

confidence: 99%

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

Scheinberg

McDevitt²

2011

CRP

146

114

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“…[11,12,32] As expected, the biodistribution profile of uncomplexed 225 Ac-(NO 3 ) 3 (Figure 3a)r eveals slow blood clearance and excretion, coupled to large accumulation in the liver and spleen. Inadequate stability of an 225 Ac complex leading to the loss of ar adioisotope in vivo is manifested by the accumulation of 225 Ac in the liver,s pleen, and bone of mice.…”

mentioning

confidence: 99%

An Eighteen‐Membered Macrocyclic Ligand for Actinium‐225 Targeted Alpha Therapy

et al. 2017

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The 18-membered macrocycle H macropa was investigated for Ac chelation in targeted alpha therapy (TAT). Radiolabeling studies showed that macropa, at submicromolar concentration, complexed all Ac (26 kBq) in 5 min at RT. [ Ac(macropa)] remained intact over 7 to 8 days when challenged with either excess La ions or human serum, and did not accumulate in any organ after 5 h in healthy mice. A bifunctional analogue, macropa-NCS, was conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. Both constructs rapidly radiolabeled Ac in just minutes at RT, and macropa-Tmab retained>99 % of its Ac in human serum after 7 days. In LNCaP xenograft mice, Ac-macropa-RPS-070 was selectively targeted to tumors and did not release free Ac over 96 h. These findings establish macropa to be a highly promising ligand for Ac chelation that will facilitate the clinical development of Ac TAT for the treatment of soft-tissue metastases.

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“…225 Ac can be produced by spallation of uranium targets via the reaction nat U( p , x ) 225 Ac by high‐energy (0.6‐2 GeV) protons . Several suitable high‐energy proton facilities exist worldwide and could be exploited for this production path.…”

Section: Production Of 225acmentioning

confidence: 99%

“…3.3 | High-energy proton irradiation of uranium and thorium spallation targets 225 Ac can be produced by spallation of uranium targets via the reaction nat U(p,x) 225 Ac by high-energy (0.6-2 GeV) protons. 39,40 Several suitable high-energy proton facilities exist worldwide and could be exploited for this production path. After irradiation, the target is dissolved and the numerous spallation products are radiochemically separated.…”

Section: Medium-energy Proton Irradiation Of 226 Ramentioning

confidence: 99%

Targeted alpha therapy with bismuth‐213 and actinium‐225: Meeting future demand

Bruchertseifer

Kellerbauer

Malmbeck

et al. 2019

Labelled Comp Radiopharmac

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Targeted alpha therapy (TAT) is a promising approach for the treatment of cancer. The use of alpha emitters for cancer therapy has two distinct advantages over conventional therapies. The short range of alpha radiation in human tissue (less than 0.1 mm), corresponding to only a few cell diameters, allows selective killing of targeted cancer cells while sparing surrounding healthy tissue. At the same time, the high energy (several MeV) of alpha radiation and its associated high linear energy transfer leads to highly effective cell kill. Consequently, alpha radiation can destroy cells which otherwise exhibit resistance to treatment with beta or gamma irradiation or chemotherapeutic drugs, and can thus offer a therapeutic option for tumors resistant to conventional therapies. Recent results demonstrating the remarkable therapeutic efficacy of alpha emitters to treat various cancers have underlined the clinical potential of TAT. This paper describes the recent clinical experience with 213Bi and 225Ac. In view of the enormous benefit of targeted cancer treatment with alpha emitters, their production will have to be considerably increased beyond current supply capabilities. Alternative production methods based on the irradiation of uranium, thorium, or radium targets at reactors or accelerator facilities have the potential to meet future demand.

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Comparison of the Biodistribution of ²²⁵Ac and Radio-Lanthanides as Citrate Complexes

Cited by 25 publications

References 4 publications

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

An Eighteen‐Membered Macrocyclic Ligand for Actinium‐225 Targeted Alpha Therapy

Targeted alpha therapy with bismuth‐213 and actinium‐225: Meeting future demand

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Comparison of the Biodistribution of 225Ac and Radio-Lanthanides as Citrate Complexes

Cited by 25 publications

References 4 publications

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

Actinium-225 in Targeted Alpha-Particle Therapeutic Applications

An Eighteen‐Membered Macrocyclic Ligand for Actinium‐225 Targeted Alpha Therapy

Targeted alpha therapy with bismuth‐213 and actinium‐225: Meeting future demand

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Comparison of the Biodistribution of ²²⁵Ac and Radio-Lanthanides as Citrate Complexes