scholarly journals Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 906
Author(s):  
Romain Eychenne ◽  
Michel Chérel ◽  
Férid Haddad ◽  
François Guérard ◽  
Jean-François Gestin
Keyword(s):  
Production Process ◽  
Clinical Studies ◽  
Physical Characteristics ◽  
Preclinical Studies ◽  
Chemical Behavior ◽  
Targeted Alpha Therapy ◽  
Therapeutic Applications ◽  
Radium 223 ◽  
Chemical Design ◽  
Alpha Therapy

Among all existing radionuclides, only a few are of interest for therapeutic applications and more specifically for targeted alpha therapy (TAT). From this selection, actinium-225, astatine-211, bismuth-212, bismuth-213, lead-212, radium-223, terbium-149 and thorium-227 are considered as the most suitable. Despite common general features, they all have their own physical characteristics that make them singular and so promising for TAT. These radionuclides were largely studied over the last two decades, leading to a better knowledge of their production process and chemical behavior, allowing for an increasing number of biological evaluations. The aim of this review is to summarize the main properties of these eight chosen radionuclides. An overview from their availability to the resulting clinical studies, by way of chemical design and preclinical studies is discussed.

Targeted alpha therapy using Radium-223: From physics to biological effects

2018 ◽  
Vol 68 ◽  
pp. 47-54 ◽  
Author(s):  
I.A. Marques ◽  
A.R. Neves ◽  
A.M. Abrantes ◽  
A.S. Pires ◽  
E. Tavares-da-Silva ◽  
...  
Keyword(s):  
Biological Effects ◽  
Targeted Alpha Therapy ◽  
Radium 223 ◽  
Alpha Therapy

scholarly journals The Mode-of-Action of Targeted Alpha Therapy Radium-223 as an Enabler for Novel Combinations to Treat Patients with Bone Metastasis

2019 ◽  
Vol 20 (16) ◽  
pp. 3899 ◽  
Author(s):  
Mari I. Suominen ◽  
Timothy Wilson ◽  
Sanna-Maria Käkönen ◽  
Arne Scholz
Keyword(s):  
Prostate Cancer ◽  
Bone Metastasis ◽  
Bone Metastases ◽  
Cancer Cells ◽  
Bone Cells ◽  
Metastatic Cancer ◽  
Signal Molecules ◽  
Targeted Alpha Therapy ◽  
Radium 223 ◽  
Alpha Therapy

Bone metastasis is a common clinical complication in several cancer types, and it causes a severe reduction in quality of life as well as lowering survival time. Bone metastases proceed through a vicious self-reinforcing cycle that can be osteolytic or osteoblastic in nature. The vicious cycle is characterized by cancer cells residing in bone releasing signal molecules that promote the differentiation of osteoclasts and osteoblasts either directly or indirectly. The increased activity of osteoclasts and osteoblasts then increases bone turnover, which releases growth factors that benefit metastatic cancer cells. In order to improve the prognosis of patients with bone metastases this cycle must be broken. Radium-223 dichloride (radium-223), the first targeted alpha therapy (TAT) approved, is an osteomimetic radionuclide that is incorporated into bone metastases where its high-linear energy transfer alpha radiation disrupts both the activity of bone cells and cancer cells. Therefore, radium-223 treatment has been shown preclinically to directly affect cancer cells in both osteolytic breast cancer and osteoblastic prostate cancer bone metastases as well as to inhibit the differentiation of osteoblasts and osteoclasts. Clinical studies have demonstrated an increase in survival in patients with metastatic castration-resistant prostate cancer. Due to the effectiveness and low toxicity of radium-223, several novel combination treatment strategies are currently eliciting considerable research interest.

Facile preparation of radium-doped, functionalized nanoparticles as carriers for targeted alpha therapy

2019 ◽  
Vol 6 (6) ◽  
pp. 1341-1349 ◽  
Author(s):  
Falco Reissig ◽  
René Hübner ◽  
Jörg Steinbach ◽  
Hans-Jürgen Pietzsch ◽  
Constantin Mamat
Keyword(s):  
Functional Groups ◽  
Functionalized Nanoparticles ◽  
Targeted Alpha Therapy ◽  
Therapeutic Applications ◽  
Facile Preparation ◽  
Enhanced Properties ◽  
Co Precipitation ◽  
Alpha Therapy

A facile preparation of nanoparticles with enhanced properties obtained by co-precipitation containing radium-224 and functional groups to connect target (bio)molecules for therapeutic applications in oncology is described.

scholarly journals 212Pb: Production Approaches and Targeted Therapy Applications

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 189
Author(s):  
Konstantin V. Kokov ◽  
Bayirta V. Egorova ◽  
Marina N. German ◽  
Ilya D. Klabukov ◽  
Michael E. Krasheninnikov ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Preclinical Studies ◽  
Clinical Implementation ◽  
Minimum Loss ◽  
Targeted Alpha Therapy ◽  
High Effectiveness ◽  
Alpha Emitter ◽  
Oncological Diseases ◽  
Parent Radionuclide ◽  
Alpha Therapy

Over the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived 212Bi (T1/2 = 1 h), provides the possibility for the synthesis and purification of complex radiopharmaceuticals with minimum loss of radioactivity during preparation. As a benefit for clinical implementation, it can be milked from a radionuclide generator in different ways. The main approaches applied for these purposes are considered and described in this review, including chromatographic, solution, and other techniques to isolate 212Pb from its parent radionuclide. Furthermore, molecules used for lead’s binding and radiochemical features of preparation and stability of compounds labeled with 212Pb are discussed. The results of preclinical studies with an estimation of therapeutic and tolerant doses as well as recently initiated clinical trials of targeted radiopharmaceuticals are presented.

scholarly journals Introduction of the targeted alpha therapy (with Radium-223) into clinical practice in Japan: learnings and implementation

2018 ◽  
Vol 33 (3) ◽  
pp. 211-221 ◽  
Author(s):  
Makoto Hosono ◽  
Hideharu Ikebuchi ◽  
Yoshihide Nakamura ◽  
Sachiko Yanagida ◽  
Seigo Kinuya
Keyword(s):  
Clinical Practice ◽  
Targeted Alpha Therapy ◽  
Radium 223 ◽  
Alpha Therapy

In vitro and preclinical studies of targeted alpha therapy (TAT) for colorectal cancer

2001 ◽  
Vol 3 (5) ◽  
pp. 345-353 ◽  
Author(s):  
S. M. A. Rizvi ◽  
B. J. Allen ◽  
Z. Tian ◽  
G. Goozee ◽  
S. Sarkar
Keyword(s):  
Colorectal Cancer ◽  
Preclinical Studies ◽  
Targeted Alpha Therapy ◽  
Alpha Therapy
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