An Appendix of Radionuclides Used in Targeted Alpha Therapy

Ferrier, Maryline G.; Radchenko, Valery

doi:10.1016/j.jmir.2019.06.051

Cited by 29 publications

(33 citation statements)

References 37 publications

(45 reference statements)

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“…Chelation of 227 Th with two HOPO ligands, 1 and 2, and four pa ligands (3)(4)(5)(6), as well as the stability of the resultant chelates, were investigated. Additionally, limited studies involving chelation of 226 Th using the pa ligand 6 were conducted.…”

Section: Resultsmentioning

confidence: 99%

“…3 This therapeutic approach targets the radiation dose to diseased cells while minimizing damage to surrounding normal tissues, unlike β-emitting radionuclides having longer particle track ranges. [4][5][6] In 2013, the first α-emitting radiopharmaceutical (i.e., [ 223 Ra]RaCl 2 Xofigo™; Bayer Healthcare Pharmaceuticals, Inc.) was approved by the US Food and Drug Administration. The rapid success reignited interest in TAT and the need to find appropriate radionuclides for therapeutic applications.…”

Section: Introductionmentioning

confidence: 99%

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Thorium chelators for targeted alpha therapy: Rapid chelation of thorium‐226

Ferrier

Chyan

et al. 2020

Labelled Comp Radiopharmac

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One of the main challenges in targeted alpha therapy is assuring delivery of the α‐particle dose to the targeted cells. Thus, it is critical to identify ligands for α‐emitting radiometals that will form complexes that are very stable, both in vitro and in vivo. In this investigation, thorium‐227 (t1/2 = 18.70 days) chelation of ligands containing hydroxypyridinonate (HOPO) or picolinic acid (pa) moieties and the stability of the resultant complexes were studied. Chelation reactions were followed by reversed‐phased HPLC and gamma spectroscopy. Studies revealed that high 227Th chelation yields could be obtained within 2.5 h or less with ligands containing four Me‐3,2‐HOPO moieties, 1 (83%) and 2 (65%), and also with ligands containing pa moieties, H4octapa 3 (65%) and H4py4pa 6 (87%). No reaction occurred with H4neunpa‐p‐Bn‐NO2 4, and the chelation reaction with another pa ligand H4pypa 5 gave inconsistent yields with a very broad radio‐HPLC peak. The ligands spermine‐(Me‐3,2‐HOPO)4 1, H4octapa 3, and H4py4pa 6 had high stability (i.e., 87% of 227Th still bound to the ligand) in phosphate‐buffered saline at room temperature over a 6‐day period. Preliminary studies with ligand 6 demonstrated efficient chelation of thorium‐226 (t1/2 = 30.57 min) when heated to 80°C for 5 min.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Thorium chelators for targeted alpha therapy: Rapid chelation of thorium‐226

Ferrier

Chyan

et al. 2020

Labelled Comp Radiopharmac

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“…Therefore, the preferred ionizing radiation types for the treatment of tumor tissue are electrons and alpha particles. Alpha particles have high linear energy (LET) and short-range; beta particles have low linear energy and long-range (17).…”

Section: Physical and Biological Efficacy Of Therapeutic Radionuclidesmentioning

confidence: 99%

“…Apart from this; some beta radionuclides used for therapeutic purposes include 153 Sm, 177 Lu, Y-90, and 131 I, along with the alpha radionuclides 211 As, 212 Bi, 212 Pb, 213 Bi, 225 Ac, 223 Ra, and 227 Th. The physical properties of some therapeutic radionuclides are given in Table 1 (16,17,20).…”

Section: Selection Of Radionuclides For Therapeutic Purposesmentioning

confidence: 99%

Treatment with Radiopharmaceuticals and Radionuclides in Breast Cancer: Current Options

Gulec¹,

Yurt²

2021

EJBH

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The World Health Organization (WHO) reported that 18.1 million people were diagnosed with cancer and 9.6 million people died in the latest data from 2018. With the increase in diagnostic possibilities, more people are diagnosed with cancer and as a public health problem; it has led to more treatment options being investigated in this field. The most common types of cancer in the world are lung, prostate, stomach, and liver in men, while the most common types are breast, lung, cervix, and colon cancer in women. In 2018 WHO report, it was stated that 2.09 million women were diagnosed with breast cancer. Attention is drawn to the importance of new treatment options considering these rates and the fact that it is the most common type of cancer in women (1, 2).The application of radioisotope and radiopharmaceutical therapies in many cancer treatments [thyroid (3), gastrointestinal system (4), prostate (5), gastroenteropancreatic, lung (6), non-Hodgkin lymphoma ( 7), cancers such as prostate bone metastases (8), breast bone metastases (9)] and positive results obtained have directed researchers to preclinical studies about the applicability of these treatment methods to breast cancer.These treatments aim to directly target cancerous cells and protect healthy tissue. Radionuclide therapy (RT) involves sending radioactive elements with different emission properties into cancerous tissue. RT has the advantage of delivering a highly concentrated dose to the targeted tumor tissue while protecting the normal tissues surrounding the tumor tissue. The fact that these treatment practices are minimally invasive and the duration of treatment is shorter than chemotherapy has made them one of the most preferred cancer treatment methods recently (10).Radiopharmaceutical treatments (RPT) are carried out by sending radionuclides conjugated to tumor-targeted pharmaceuticals or bioactive molecules (nanoparticles, antibodies, peptides, small molecules, and various structures of each) that predominantly accumulate in neoplastic cells within tumors into the tumor tissue (11). Recently, RT has attracted attention as a safe and effective method for cancer treatment, and research continues (12).In this review article, the effectiveness of preclinical studies conducted in the last five years with radionuclides and radiopharmaceuticals in breast cancer will be discussed.

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“…Overview of α-emitting radionuclides used in PSMA-TAT[71][72][73][74][75]. Comparisons of prostate-specific membrane antigen (PSMA)-targeting small molecules, antibodies, and their fragments[55,[76][77][78][79][80].…”

mentioning

confidence: 99%

Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer

Juzeniene

Stenberg

Bruland

et al. 2021

Cancers

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Bone, lymph node, and visceral metastases are frequent in castrate-resistant prostate cancer patients. Since such patients have only a few months’ survival benefit from standard therapies, there is an urgent need for new personalized therapies. The prostate-specific membrane antigen (PSMA) is overexpressed in prostate cancer and is a molecular target for imaging diagnostics and targeted radionuclide therapy (theragnostics). PSMA-targeted α therapies (PSMA-TAT) may deliver potent and local radiation more selectively to cancer cells than PSMA-targeted β- therapies. In this review, we summarize both the recent preclinical and clinical advances made in the development of PSMA-TAT, as well as the availability of therapeutic α-emitting radionuclides, the development of small molecules and antibodies targeting PSMA. Lastly, we discuss the potentials, limitations, and future perspectives of PSMA-TAT.

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An Appendix of Radionuclides Used in Targeted Alpha Therapy

Cited by 29 publications

References 37 publications

Thorium chelators for targeted alpha therapy: Rapid chelation of thorium‐226

Thorium chelators for targeted alpha therapy: Rapid chelation of thorium‐226

Treatment with Radiopharmaceuticals and Radionuclides in Breast Cancer: Current Options

Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer

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