☆ 4.7 Review

Targeted Alpha-Particle Therapy: A Review of Current Trials

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Summary: Astatine-211 is a top candidate for targeted alpha therapy (TAT) due to its physical properties. In this article, we summarize the results of completed clinical trials, provide an overview of ongoing trials, and discuss future prospects.

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Phase I dose-escalation results of prostate-specific membrane antigen-targeted radionuclide therapy (PSMA-TRT) with alpha-radiolabeled antibody 225Ac-J591 and beta-radioligand 177Lu-PSMA I&T.

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Article Oncology

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JOURNAL OF NUCLEAR MEDICINE (2023)

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Review Oncology

The Secondary Myelodysplastic Neoplasms (MDS) Jigsaw

Oriol Calvete et al.

Summary: The classification of secondary myelodysplastic neoplasms (MDSs) in patients with a previous primary tumor is still controversial due to the lack of an established consensus risk factor-based classification. Current classifications consider separate etiologies based on exposure to cytotoxic therapy and genetic predisposition, despite the evidence of overlapping risk factors. This review aims to summarize the current knowledge of secondary MDS etiologies and suggests the need for future classifications that take into account all risk factors and their interactions.

CANCERS (2023)

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Article Medicine, General & Internal

Clinical outcomes and treatment patterns in REASSURE : planned interim analysis of a real-world observational study of radium-223 in metastatic castration-resistant prostate cancer

Celestia S. Higano et al.

Summary: This study investigated the use of radium-223 in real-world clinical practice and found that its safety and overall survival were consistent with clinical trial results. It also provided insights into the current application of radium-223 in the treatment of bone-dominant metastatic castration-resistant prostate cancer.

ECLINICALMEDICINE (2023)

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Meeting Abstract Oncology

Phase 1 study of JNJ-69086420, an actinium-225-labeled antibody targeting human kallikrein-2, for advanced prostate cancer.

Michael J. Morris et al.

JOURNAL OF CLINICAL ONCOLOGY (2022)

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Article Radiology, Nuclear Medicine & Medical Imaging

Targeted a-Emitter Therapy with 212Pb-DOTAMTATE for the Treatment of Metastatic SSTR-Expressing Neuroendocrine Tumors: First-in-Humans Dose-Escalation Clinical Trial

Ebrahim S. Delpassand et al.

Summary: The targeted α-therapy with Pb-212-DOTAMTATE showed good tolerability and promising preliminary efficacy in treating patients with somatostatin receptor-positive NETs.

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Review Pharmacology & Pharmacy

212Pb: Production Approaches and Targeted Therapy Applications

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Summary: Targeted alpha therapy has been proven to be highly effective in treating oncological diseases. Lead-212, with its convenient half-life and short-lived daughter alpha-emitter Bi-212, allows for the synthesis and purification of complex radiopharmaceuticals with minimal loss of radioactivity. This review discusses the various methods for isolating Pb-212 and the binding molecules used, as well as presents the results of preclinical studies and recent clinical trials.

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Chung Ying Chan et al.

Summary: In this study, [F-18]rucaparib, a non-invasive PARP-targeting imaging agent, was developed for PET imaging of pancreatic cancer. The results showed its potential application value.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2022)

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Article Medicine, Research & Experimental

Preclinical Investigations to Explore the Difference between the Diastereomers [177Lu]Lu-SibuDAB and [177Lu]Lu-RibuDAB toward Prostate Cancer Therapy

Francesca Borgna et al.

Summary: This study investigated the in vitro and in vivo properties of the new radioligands [Lu-177]Lu-SibuDAB and [Lu-177]Lu-RibuDAB, and found that [Lu-177]Lu-SibuDAB had higher binding affinity and metabolic stability, making it more favorable for tumor targeting. Therapeutic experiments demonstrated the superior efficacy of [Lu-177]Lu-SibuDAB compared to the current gold-standard [Lu-177]Lu-PSMA-617.

MOLECULAR PHARMACEUTICS (2022)

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Article Oncology

[225Ac]Ac-SibuDAB for Targeted Alpha Therapy of Prostate Cancer: Preclinical Evaluation and Comparison with [225Ac]Ac-PSMA-617

Sarah D. Busslinger et al.

Summary: This study compared the therapeutic efficacy of two radioligands for prostate cancer treatment and found that [Ac-225]Ac-SibuDAB was more effective than [Ac-225]Ac-PSMA-617. However, both radioligands had similar undesired side effects, highlighting the need for further clinical studies to determine their safety.

CANCERS (2022)

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[18F]-Labeled PARP-1 PET imaging of PSMA targeted alpha particle radiotherapy response

Hanwen Zhang et al.

Summary: Noninvasive imaging has great potential to guide α-particle therapy. In this study, [F-18]-PARPZ radiotracer was used to delineate castrate resistant prostate cancer xenografts, showing its ability to distinguish treated from control groups and further understand DNA damage response.

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Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects

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FRONTIERS IN CHEMISTRY (2022)

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Meeting Abstract Hematology

Lintuzumab-Ac225 with Combination with Intensive Chemotherapy Yields High Response Rate and MRD Negativity in R/R AML with Adverse Features

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Review Pharmacology & Pharmacy

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Summary: This review discusses the therapeutic advantages of targeted alpha particle therapy, the properties and radiochemistry of common alpha-emitters, production techniques, ongoing and completed clinical trials, and future outlook of TAT.

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Meeting Abstract Oncology

A phase I/II dose-escalation study of fractionated and multiple dose 225Ac-J591 for progressive metastatic castration-resistant prostate cancer (mCRPC).

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JOURNAL OF CLINICAL ONCOLOGY (2021)

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Phase I study of Ac-225-J591 for men with metastatic castration-resistant prostate cancer (mCRPC).

Scott T. Tagawa et al.

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Review Pharmacology & Pharmacy

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Editorial Material Radiology, Nuclear Medicine & Medical Imaging

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CLINICAL NUCLEAR MEDICINE (2020)

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Article Medicine, Research & Experimental

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Whole-body and single-photon emission computed tomography/computed tomography postpeptide receptor alpha radionuclide therapy images of actinium 225-tetraazacyclododecanetetraacetic Acid-Octreotide as a primary modality of treatment in a patient with advanced rectal neuroendocrine tumor with metastases

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INDIAN JOURNAL OF NUCLEAR MEDICINE (2020)

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Article Oncology

Drugs That Modify Cholesterol Metabolism Alter the p38/JNK-Mediated Targeted and Nontargeted Response to Alpha and Auger Radioimmunotherapy

Riad Ladjohounlou et al.

CLINICAL CANCER RESEARCH (2019)

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Meeting Abstract Oncology

A phase I study of [225Ac]-FPI-1434 radioimmunotherapy in patients with IGF-1R expressing solid tumors.

Rosalyn A. Juergens et al.

JOURNAL OF CLINICAL ONCOLOGY (2019)

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Article Radiology, Nuclear Medicine & Medical Imaging

PET Imaging of PARP Expression Using 18F-Olaparib

Thomas C. Wilson et al.

JOURNAL OF NUCLEAR MEDICINE (2019)

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Albumin-Binding PSMA Ligands: Implications for Expanding the Therapeutic Window

James M. Kelly et al.

JOURNAL OF NUCLEAR MEDICINE (2019)

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Clinical evidence of abscopal effect in cutaneous squamous cell carcinoma treated with diffusing alpha emitters radiation therapy: a case report

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Trifunctional PSMA-targeting constructs for prostate cancer with unprecedented localization to LNCaP tumors

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Letter Chemistry, Medicinal

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PMPA for Nephroprotection in PSMA-Targeted Radionuclide Therapy of Prostate Cancer

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JOURNAL OF NUCLEAR MEDICINE (2015)

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Review Medicine, Research & Experimental

Application of Pb-212 for Targeted alpha-particle Therapy (TAT): Pre-clinical and Mechanistic Understanding through to Clinical Translation

Kwon Yong et al.

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Review Chemistry, Medicinal

A Critical Review of Alpha Radionuclide Therapy-How to Deal with Recoiling Daughters?

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NEOPLASIA (2014)

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NEW ENGLAND JOURNAL OF MEDICINE (2013)

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Chen-Yu Huang et al.

MEDICAL PHYSICS (2012)

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