Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations

Makvandi, Mehran; Dupis, Edouard; Engle, Jonathan W.; Nortier, F. Meiring; Fassbender, Michael E.; Simon, Sam; Birnbaum, Eva R.; Atcher, Robert W.; John, Kevin D.; Rixe, Olivier; Norenberg, Jeffrey P.

doi:10.1007/s11523-018-0550-9

Title: Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations

Abstract

Alpha-emitters are radionuclides that decay through the emission of high linear energy transfer α-particles and possess favorable pharmacologic profiles for cancer treatment. When coupled with monoclonal antibodies, peptides, small molecules, or nanoparticles, the excellent cytotoxic capability of α-particle emissions has generated a strong interest in exploring targeted α-therapy in the pre-clinical setting and more recently in clinical trials in oncology. Multiple obstacles have been overcome by researchers and clinicians to accelerate the development of targeted α-therapies, especially with the recent improvement in isotope production and purification, but also with the development of innovative strategies for optimized targeting. Numerous studies have demonstrated the in vitro and in vivo efficacy of the targeted α-therapy. Radium-223 (²²³Ra) dichloride (Xofigo®) is the first α-emitter to have received FDA approval for the treatment of prostate cancer with metastatic bone lesions. There is a significant increase in the number of clinical trials in oncology using several radionuclides such as Actinium-225 (²²⁵Ac), Bismuth-213 (²¹³Bi), Lead-212 (²¹²Pb), Astatine (²¹¹At) or Radium-223 (²²³Ra) assessing their safety and preliminary activity. Finally, this review will cover their therapeutic application as well as summarize the investigations that provide the foundation for further clinical development.

Authors:

Makvandi, Mehran ^[1]; Dupis, Edouard ^[2]; Engle, Jonathan W. ^[3]; Nortier, F. Meiring ^[3]; Fassbender, Michael E. ^[3]; Simon, Sam ^[1]; Birnbaum, Eva R. ^[3]; Atcher, Robert W. ^[4]; John, Kevin D. ^[3]; Rixe, Olivier ^[2]; Norenberg, Jeffrey P. ^[1]

Univ. of New Mexico, Albuquerque, NM (United States). Radiopharmaceutical Sciences Program. College of Pharmacy. Health Sciences Center
Univ. of New Mexico Comprehensive Cancer Center, Albuquerque, NM (United States). Experimental Therapeutics Unit
Los Alamos National Lab. (LANL), Los Alamos, NM (United States)
Univ. of New Mexico, Albuquerque, NM (United States). Radiopharmaceutical Sciences Program. College of Pharmacy. Health Sciences Center; Los Alamos National Lab. (LANL), Los Alamos, NM (United States)

Publication Date:: Thu Feb 08 00:00:00 EST 2018

Research Org.:: Los Alamos National Laboratory (LANL), Los Alamos, NM (United States); Univ. of New Mexico, Albuquerque, NM (United States)

Sponsoring Org.:: USDOE

OSTI Identifier:: 1459839

Report Number(s):: LA-UR-16-27976
Journal ID: ISSN 1776-2596

Grant/Contract Number:: AC52-06NA25396

Resource Type:: Accepted Manuscript

Journal Name:: Targeted Oncology

Additional Journal Information:: Journal Volume: 13; Journal Issue: 2; Journal ID: ISSN 1776-2596

Publisher:: Springer

Country of Publication:: United States

Language:: English

Subject:: 62 RADIOLOGY AND NUCLEAR MEDICINE

Citation Formats


                    Makvandi, Mehran, Dupis, Edouard, Engle, Jonathan W., Nortier, F. Meiring, Fassbender, Michael E., Simon, Sam, Birnbaum, Eva R., Atcher, Robert W., John, Kevin D., Rixe, Olivier, and Norenberg, Jeffrey P. Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations.  United States: N. p., 2018. 
Web.  doi:10.1007/s11523-018-0550-9.

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                    Makvandi, Mehran, Dupis, Edouard, Engle, Jonathan W., Nortier, F. Meiring, Fassbender, Michael E., Simon, Sam, Birnbaum, Eva R., Atcher, Robert W., John, Kevin D., Rixe, Olivier, & Norenberg, Jeffrey P. Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations.  United States.  https://doi.org/10.1007/s11523-018-0550-9

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                    Makvandi, Mehran, Dupis, Edouard, Engle, Jonathan W., Nortier, F. Meiring, Fassbender, Michael E., Simon, Sam, Birnbaum, Eva R., Atcher, Robert W., John, Kevin D., Rixe, Olivier, and Norenberg, Jeffrey P. Thu .  
"Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations".  United States.  https://doi.org/10.1007/s11523-018-0550-9.  https://www.osti.gov/servlets/purl/1459839.

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@article{osti_1459839,

  title        = {Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations},

  author       = {Makvandi, Mehran and Dupis, Edouard and Engle, Jonathan W. and Nortier, F. Meiring and Fassbender, Michael E. and Simon, Sam and Birnbaum, Eva R. and Atcher, Robert W. and John, Kevin D. and Rixe, Olivier and Norenberg, Jeffrey P.},

  abstractNote = {Alpha-emitters are radionuclides that decay through the emission of high linear energy transfer α-particles and possess favorable pharmacologic profiles for cancer treatment. When coupled with monoclonal antibodies, peptides, small molecules, or nanoparticles, the excellent cytotoxic capability of α-particle emissions has generated a strong interest in exploring targeted α-therapy in the pre-clinical setting and more recently in clinical trials in oncology. Multiple obstacles have been overcome by researchers and clinicians to accelerate the development of targeted α-therapies, especially with the recent improvement in isotope production and purification, but also with the development of innovative strategies for optimized targeting. Numerous studies have demonstrated the in vitro and in vivo efficacy of the targeted α-therapy. Radium-223 (223Ra) dichloride (Xofigo®) is the first α-emitter to have received FDA approval for the treatment of prostate cancer with metastatic bone lesions. There is a significant increase in the number of clinical trials in oncology using several radionuclides such as Actinium-225 (225Ac), Bismuth-213 (213Bi), Lead-212 (212Pb), Astatine (211At) or Radium-223 (223Ra) assessing their safety and preliminary activity. Finally, this review will cover their therapeutic application as well as summarize the investigations that provide the foundation for further clinical development.},

  doi          = {10.1007/s11523-018-0550-9},

  journal      = {Targeted Oncology},

  number       = 2,

  volume       = 13,

  place        = {United States},

  year         = {Thu Feb 08 00:00:00 EST 2018},

  month        = {Thu Feb 08 00:00:00 EST 2018}

}

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Fig. 1 : Path length and ionization density of $α$-particles versus $β$-particles

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journal, July 2005

Prise, Kevin M.; Schettino, Giuseppe; Folkard, Melvyn
The Lancet Oncology, Vol. 6, Issue 7
DOI: 10.1016/S1470-2045(05)70246-1

Astatine-211: Production and Availability
journal, July 2011

R. Zalutsky, Michael; Pruszynski, Marek
Current Radiopharmaceuticalse, Vol. 4, Issue 3
DOI: 10.2174/1874471011104030177

Remodeling the Vascular Microenvironment of Glioblastoma with -Particles
journal, June 2016

Behling, K.; Maguire, W. F.; Di Gialleonardo, V.
Journal of Nuclear Medicine, Vol. 57, Issue 11
DOI: 10.2967/jnumed.116.173559

213Bi-[DOTA0, Tyr3]Octreotide Peptide Receptor Radionuclide Therapy of Pancreatic Tumors in a Preclinical Animal Model
journal, February 2006

Norenberg, J. P.
Clinical Cancer Research, Vol. 12, Issue 3
DOI: 10.1158/1078-0432.CCR-05-1264

Efforts to Control the Errant Products of a Targeted In vivo Generator
journal, June 2005

Singh Jaggi, Jaspreet; Kappel, Barry J.; McDevitt, Michael R.
Cancer Research, Vol. 65, Issue 11
DOI: 10.1158/0008-5472.CAN-04-3096

Long-Term Toxicity of 213Bi-Labelled BSA in Mice
journal, March 2016

Dorso, Laëtitia; Bigot-Corbel, Edith; Abadie, Jérôme
PLOS ONE, Vol. 11, Issue 3
DOI: 10.1371/journal.pone.0151330

Cytotoxicity of 213Bi- and 225Ac-immunoconjugates
journal, January 1995

Kaspersen, F. M.; Bos, E.; Doornmalen, A. V.
Nuclear Medicine Communications, Vol. 16, Issue 6
DOI: 10.1097/00006231-199506000-00009

Bismuth-213 and Actinium-225 – Generator Performance and Evolving Therapeutic Applications of Two Generator-Derived Alpha-Emitting Radioisotopes
journal, June 2012

Morgenstern, Alfred; Bruchertseifer, Frank; Apostolidis, Christos
Current Radiopharmaceuticals, Vol. 5, Issue 3
DOI: 10.2174/1874471011205030221

Phase I trial of α-particle therapy with actinium-225 ( ²²⁵ Ac)-lintuzumab (anti-CD33) and low-dose cytarabine (LDAC) in older patients with untreated acute myeloid leukemia (AML.
journal, May 2015

Jurcic, Joseph G.; Ravandi, Farhad; Pagel, John M.
Journal of Clinical Oncology, Vol. 33, Issue 15_suppl
DOI: 10.1200/jco.2015.33.15_suppl.7050

Targeted α particle immunotherapy for myeloid leukemia
journal, August 2002

Jurcic, Joseph G.; Larson, Steven M.; Sgouros, George
Blood, Vol. 100, Issue 4
DOI: 10.1182/blood.V100.4.1233.h81602001233_1233_1239

Works referencing / citing this record:

Production of 149Tb, 152Tb, 155Tb and 161Tb from gadolinium using different light-particle beams
journal, December 2019

Rahman, A. K. M. Rezaur; Awal, Abdul
Journal of Radioanalytical and Nuclear Chemistry, Vol. 323, Issue 2
DOI: 10.1007/s10967-019-06973-0

Targeting the Tetraspanins with Monoclonal Antibodies in Oncology: Focus on Tspan8/Co-029
journal, February 2019

Bonnet, Mathilde; Maisonial-Besset, Aurélie; Zhu, Yingying
Cancers, Vol. 11, Issue 2
DOI: 10.3390/cancers11020179

Towards elucidating the radiochemistry of astatine – Behavior in chloroform
journal, November 2019

Aneheim, Emma; Palm, Stig; Jensen, Holger
Scientific Reports, Vol. 9, Issue 1
DOI: 10.1038/s41598-019-52365-5

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives
journal, June 2019

Lepareur, Nicolas; Lacœuille, Franck; Bouvry, Christelle
Frontiers in Medicine, Vol. 6
DOI: 10.3389/fmed.2019.00132

Ion acceleration by an ultrashort laser pulse interacting with a near-critical-density gas jet
preprint, January 2020

Ehret, M.; Salgado-Lopez, C.; Ospina-Bohorquez, V.
arXiv
DOI: 10.48550/arxiv.2012.09455

Measurement of Ac227 Impurity in Ac225 using Decay Energy Spectroscopy
preprint, January 2021

Tollefson, Aidan D.; Smith, Chandler M.; Carpenter, Matthew H.
arXiv
DOI: 10.48550/arxiv.2102.02813

Figures / Tables found in this record:

Table 4: Part 1 (p. 9)

Table 4: Part 2 (p. 10)

Figures/Tables have been extracted from DOE-funded journal article accepted manuscripts.

Similar Records in DOE PAGES and OSTI.GOV collections:

Commercial Availability of Alpha-Emitting Radionuclides for Medicine

Journal Article Fisher, Darrell R - Current Radiopharmaceuticals, 1(3):127-134

Alpha-emitting radionuclides provide effective cell-killing properties and have been shown to be effective in cancer treatment. The number of different alpha emitters having suitable physical and chemical characteristics for applications in medicine is relatively few. Development and testing of new radiopharmaceuticals requires a reliable supply of alpha-emitters in high quality, with timely delivery, but at reasonable cost. Applications and commercial availability of the follow alpha emitters are reviewed: Actinium-225, bismuth-213, astatine-211, radium-223, bismuth-212, radium-224, radium-226, terbium-149, and thorium-227. Recommendations for improving the supply of these alpha emitters include an increased federal commitment (through funding and joint-agency cooperation), establishing new productionmore »« less
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Radiation-induced cancer of bone, liver and lung has been a prominent harmful side-effect of medical applications of alpha emitters. In recent years, however, the potential use of antibodies labeled with alpha emitting radionuclides against cancer has seemed promising because alpha particles are highly effective in cell killing. High dose rates at high LET, effectiveness under hypoxic conditions, and minimal expectancy of repair are additional advantages of alpha emitters over antibodies labeled with beta emitting radionuclides for cancer therapy. Cyclotron-produced astatine-211 ({sup 211}At) and natural bismuth-212 ({sup 212}Bi) have been proposed and are under extensive study in the United States andmore »« less
Full Text Available
Radium-223 in the Treatment of Osteoblastic Metastases: A Critical Clinical Review

Journal Article Humm, John L. ; Sartor, Oliver ; Parker, Chris ; ... - International Journal of Radiation Oncology, Biology and Physics

The element radium (Ra) was discovered by the Curies in 1898 and within a decade was in broad scientific testing for the management of several forms of cancer. The compound was known to give rise to a series of both high-energy particulate and penetrating γ-emissions. The latter found an important role in early 20th century brachytherapy applications, but the short-range α-particles seemed much less useful. Although highly cytotoxic when released within a few cell diameters of critical cell nuclei, the dense double-strand break damage was poorly repaired, and concerns regarding treatment-related toxicities and secondary malignancies halted clinical development. Moreover, themore »« less
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The science of cancer research is currently expanding its use of alpha particle emitting radioisotopes. Coupled with the discovery and proliferation of molecular species that seek out and attach to tumors, new therapy and diagnostics are being developed to enhance the treatment of cancer and other diseases. This latest technology is commonly referred to as Alpha Immunotherapy (AIT). Actinium-225/Bismuth-213 is a parent/daughter alpha-emitting radioisotope pair that is highly sought after because of the potential for treating numerous diseases and its ability to be chemically compatible with many known and widely used carrier molecules (such as monoclonal antibodies and proteins/peptides). Unfortunately,more »« less
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Purpose: Alpha-emitting radionuclides exhibit a potential advantage for cancer treatments because they release large amounts of ionizing energy over a few cell diameters (50–80 μm), causing localized, irreparable double-strand DNA breaks that lead to cell death. Radioimmunotherapy (RIT) approaches using monoclonal antibodies labeled with α emitters may thus inactivate targeted cells with minimal radiation damage to surrounding tissues. Tools are needed to visualize and quantify the radioactivity distribution and absorbed doses to targeted and nontargeted cells for accurate dosimetry of all treatment regimens utilizing α particles, including RIT and others (e.g., Ra-223), especially for organs and tumors with heterogeneous radionuclidemore »« less
https://doi.org/10.1118/1.4921997

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Title: Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations

Abstract

Citation Formats

Figures / Tables:

First Clinical Experience with -Emitting Radium-223 in the Treatment of Skeletal Metastases journal, June 2005

Improved safety and efficacy of 213Bi-DOTATATE-targeted alpha therapy of somatostatin receptor-expressing neuroendocrine tumors in mice pre-treated with l-lysine journal, November 2016

Gold Coated Lanthanide Phosphate Nanoparticles for Targeted Alpha Generator Radiotherapy journal, January 2013

Preclinical Evaluation of the α-Particle Generator Nuclide 225Ac for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors journal, June 2008

Targeted Alpha-Particle Immunotherapy for Acute Myeloid Leukemia journal, May 2014

Treatment of Peritoneal Carcinomatosis by Targeted Delivery of the Radio-Labeled Tumor Homing Peptide 213Bi-DTPA-[F3]2 into the Nucleus of Tumor Cells journal, May 2009

Design and evaluation of an external high-current target for production of 211 At journal, October 2012

Selective Alpha-Particle Mediated Depletion of Tumor Vasculature with Vascular Normalization journal, March 2007

Preliminary Production of 211At at the Texas A&M University Cyclotron Institute journal, January 2014

225Ac-PSMA-617 for PSMA-Targeted -Radiation Therapy of Metastatic Castration-Resistant Prostate Cancer journal, July 2016

Production of α-particle emitting 211 At using 45 MeV α-beam journal, May 2014

Astatine-211 conjugated to an anti-CD20 monoclonal antibody eradicates disseminated B-cell lymphoma in a mouse model journal, March 2015

Analysis of patient survival in a Phase I trial of systemic targeted α-therapy for metastatic melanoma journal, September 2011

Enhanced Loading Efficiency and Retention of 225 Ac in Rigid Liposomes for Potential Targeted Therapy of Micrometastases journal, June 2008

Tumor Targeting with Antibody-Functionalized, Radiolabeled Carbon Nanotubes journal, July 2007

Clinical Experience with -Particle Emitting 211At: Treatment of Recurrent Brain Tumor Patients with 211At-Labeled Chimeric Antitenascin Monoclonal Antibody 81C6 journal, December 2007

Patient-reported quality-of-life analysis of radium-223 dichloride from the phase III ALSYMPCA study journal, February 2016

An overview of targeted alpha therapy journal, December 2011

Dry-distillation of astatine-211 from irradiated bismuth targets: a time-saving procedure with high recovery yields journal, August 2001

(2S)-2-(3-(1-Carboxy-5-(4-211At-Astatobenzamido)Pentyl)Ureido)-Pentanedioic Acid for PSMA-Targeted -Particle Radiopharmaceutical Therapy journal, May 2016

Evaluation of an internal cyclotron target for the production of 211At via the 209Bi (α,2n)211At reaction journal, February 1996

α-Particle Radioimmunotherapy of Disseminated Peritoneal Disease Using a 212 Pb-Labeled Radioimmunoconjugate Targeting HER2 journal, October 2005

Targeted α-particle radiotherapy with 211At-labeled monoclonal antibodies journal, October 2007

What is the Role of the Bystander Response in Radionuclide Therapies? journal, January 2013

A schema for estimating absorbed dose to organs following the administration of radionuclides with multiple unstable daughters: A matrix approach journal, December 1999

Targeted deletion of T-cell clones using alpha-emitting suicide MHC tetramers journal, October 2004

Radioimmunotherapy with alpha-emitting nuclides journal, September 1998

Modification of Radiation Damage by Fractionation of the Dose, Anoxia, and Chemical Protectors in Relation to let journal, March 1964

LaPO 4 Nanoparticles Doped with Actinium-225 that Partially Sequester Daughter Radionuclides journal, April 2011

The pre-clinical characterization of an alpha-emitting sigma-2 receptor targeted radiotherapeutic journal, January 2016

Safety and Outcome Measures of First-in-Human Intraperitoneal α Radioimmunotherapy With 212Pb-TCMC-Trastuzumab journal, January 2018

Proton-induced cross sections relevant to production of 225Ac and 223Ra in natural thorium targets below 200MeV journal, November 2012

Enhanced Retention of the α-Particle-Emitting Daughters of Actinium-225 by Liposome Carriers journal, November 2007

Bystander effects and radiotherapy journal, January 2015

Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for alpha radionuclide therapy journal, November 2015

Targeting of Radio-Isotopes for Cancer Therapy journal, April 2004

Targeted alpha-radionuclide therapy of functionally critically located gliomas with 213Bi-DOTA-[Thi8,Met(O2)11]-substance P: a pilot trial journal, February 2010

Treatment of Metastatic Bone Disease and the Emerging Role of Radium-223 journal, March 2016

Significant systemic therapeutic effects of high-LET immunoradiation by 212Pb-trastuzumab against prostatic tumors of androgen-independent human prostate cancer in mice journal, February 2012

Targeted Alpha Therapy with 213Bi journal, October 2011

Pharmacokinetics and Imaging of 212 Pb-TCMC-Trastuzumab After Intraperitoneal Administration in Ovarian Cancer Patients journal, February 2014

The Metabolism of Actinium in the Rat journal, January 1970

213Bi-PSMA-617 targeted alpha-radionuclide therapy in metastatic castration-resistant prostate cancer journal, March 2017

Absorbed Doses and Risk Estimates of 211At-MX35 F(ab')2 in Intraperitoneal Therapy of Ovarian Cancer Patients journal, November 2015

A new internal target system for production of 211At on the cyclotron U-120M journal, July 2005

B7-H3-targeted 212Pb radioimmunotherapy of ovarian cancer in preclinical models journal, April 2017

Production of 211 At by a vertical beam irradiation method journal, December 2014

Radioimmunotherapy with Bismuth-213 as Conditioning for Nonmyeloablative Allogeneic Hematopoietic Cell Transplantation in Dogs: A Dose Deescalation Study journal, January 2004

A randomized, dose–response, multicenter phase II study of radium-223 chloride for the palliation of painful bone metastases in patients with castration-resistant prostate cancer journal, March 2012

Different ways to improve the clinical effectiveness of radioimmunotherapy in solid tumors journal, January 2009

213Bi-DOTATOC receptor-targeted alpha-radionuclide therapy induces remission in neuroendocrine tumours refractory to beta radiation: a first-in-human experience journal, July 2014

Renal Tubulointerstitial Changes after Internal Irradiation with α-Particle–Emitting Actinium Daughters journal, June 2005

Metabolic Characteristics Within a Chemical Family journal, January 1959

Intraperitoneal -Particle Radioimmunotherapy of Ovarian Cancer Patients: Pharmacokinetics and Dosimetry of 211At-MX35 F(ab')2--A Phase I Study journal, June 2009

A kit method for the high level synthesis of [211At]MABG journal, May 2007

MIRD Pamphlet No. 22 (Abridged): Radiobiology and Dosimetry of -Particle Emitters for Targeted Radionuclide Therapy journal, January 2010

Intralesional targeted alpha therapy for metastatic melanoma journal, December 2005

Improved efficacy of α-particle-targeted radiation therapy: Dual targeting of human epidermal growth factor receptor-2 and tumor-associated glycoprotein 72 journal, February 2010

Selective Killing of Tumor Neovasculature Paradoxically Improves Chemotherapy Delivery to Tumors journal, November 2010

Sequential Cytarabine and α-Particle Immunotherapy with Bismuth-213–Lintuzumab (HuM195) for Acute Myeloid Leukemia journal, September 2010

Mitigation of radiation nephropathy after internal α-particle irradiation of kidneys journal, April 2006

Theoretical estimation of absorbed dose to organs in radioimmunotherapy using radionuclides with multiple unstable daughters journal, September 2001

Improved tumor imaging and therapy via i.v. IgG–mediated time-sequential modulation of neonatal Fc receptor journal, September 2007

Melanoma Therapy via Peptide-Targeted -Radiation journal, August 2005

Large scale accelerator production of 225Ac: Effective cross sections for 78–192 MeV protons incident on 232Th targets journal, December 2016

Radioimmunotherapy of Breast Cancer Metastases with -Particle Emitter 225Ac: Comparing Efficacy with 213Bi and 90Y journal, November 2009

The Relative Radiosensitivity of the Nucleus and Cytoplasm of Chinese Hamster Fibroblasts journal, June 1970

Effective treatment of ductal carcinoma in situ with a HER-2- targeted alpha-particle emitting radionuclide in a preclinical model of human breast cancer journal, April 2016

Breaking Chemoresistance and Radioresistance with [ 213 Bi]anti-CD45 Antibodies in Leukemia Cells journal, March 2007

Interim analysis of toxicity and response in phase 1 trial of systemic targeted alpha therapy for metastatic melanoma journal, June 2007

An 225Ac/213Bi generator system for therapeutic clinical applications: construction and operation journal, May 1999

Evaluation of 225 Ac for Vascular Targeted Radioimmunotherapy of Lung Tumors journal, June 2000

Pharmacokinetics and toxicity of 213Bi-labeled PAI2 in preclinical targeted alpha therapy for cancer journal, June 2007

New insights on cell death from radiation exposure journal, July 2005

Astatine-211: Production and Availability journal, July 2011

Remodeling the Vascular Microenvironment of Glioblastoma with -Particles journal, June 2016

First Clinical Experience with -Emitting Radium-223 in the Treatment of Skeletal Metastases
journal, June 2005

Improved safety and efficacy of 213Bi-DOTATATE-targeted alpha therapy of somatostatin receptor-expressing neuroendocrine tumors in mice pre-treated with l-lysine
journal, November 2016

Gold Coated Lanthanide Phosphate Nanoparticles for Targeted Alpha Generator Radiotherapy
journal, January 2013

Preclinical Evaluation of the α-Particle Generator Nuclide ²²⁵Ac for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors
journal, June 2008

Targeted Alpha-Particle Immunotherapy for Acute Myeloid Leukemia
journal, May 2014

Treatment of Peritoneal Carcinomatosis by Targeted Delivery of the Radio-Labeled Tumor Homing Peptide 213Bi-DTPA-[F3]2 into the Nucleus of Tumor Cells
journal, May 2009

Design and evaluation of an external high-current target for production of ²¹¹ At
journal, October 2012

Selective Alpha-Particle Mediated Depletion of Tumor Vasculature with Vascular Normalization
journal, March 2007

Preliminary Production of 211At at the Texas A&M University Cyclotron Institute
journal, January 2014

225Ac-PSMA-617 for PSMA-Targeted -Radiation Therapy of Metastatic Castration-Resistant Prostate Cancer
journal, July 2016

Production of α-particle emitting ²¹¹ At using 45 MeV α-beam
journal, May 2014

Astatine-211 conjugated to an anti-CD20 monoclonal antibody eradicates disseminated B-cell lymphoma in a mouse model
journal, March 2015

Analysis of patient survival in a Phase I trial of systemic targeted α-therapy for metastatic melanoma
journal, September 2011

Enhanced Loading Efficiency and Retention of ²²⁵ Ac in Rigid Liposomes for Potential Targeted Therapy of Micrometastases
journal, June 2008

Tumor Targeting with Antibody-Functionalized, Radiolabeled Carbon Nanotubes
journal, July 2007

Clinical Experience with -Particle Emitting 211At: Treatment of Recurrent Brain Tumor Patients with 211At-Labeled Chimeric Antitenascin Monoclonal Antibody 81C6
journal, December 2007

Patient-reported quality-of-life analysis of radium-223 dichloride from the phase III ALSYMPCA study
journal, February 2016

An overview of targeted alpha therapy
journal, December 2011

Dry-distillation of astatine-211 from irradiated bismuth targets: a time-saving procedure with high recovery yields
journal, August 2001

(2S)-2-(3-(1-Carboxy-5-(4-211At-Astatobenzamido)Pentyl)Ureido)-Pentanedioic Acid for PSMA-Targeted -Particle Radiopharmaceutical Therapy
journal, May 2016

Evaluation of an internal cyclotron target for the production of 211At via the 209Bi (α,2n)211At reaction
journal, February 1996

α-Particle Radioimmunotherapy of Disseminated Peritoneal Disease Using a ²¹² Pb-Labeled Radioimmunoconjugate Targeting HER2
journal, October 2005

Targeted α-particle radiotherapy with ²¹¹At-labeled monoclonal antibodies
journal, October 2007

What is the Role of the Bystander Response in Radionuclide Therapies?
journal, January 2013

A schema for estimating absorbed dose to organs following the administration of radionuclides with multiple unstable daughters: A matrix approach
journal, December 1999

Targeted deletion of T-cell clones using alpha-emitting suicide MHC tetramers
journal, October 2004

Radioimmunotherapy with alpha-emitting nuclides
journal, September 1998

Modification of Radiation Damage by Fractionation of the Dose, Anoxia, and Chemical Protectors in Relation to let
journal, March 1964

LaPO ₄ Nanoparticles Doped with Actinium-225 that Partially Sequester Daughter Radionuclides
journal, April 2011

The pre-clinical characterization of an alpha-emitting sigma-2 receptor targeted radiotherapeutic
journal, January 2016

Safety and Outcome Measures of First-in-Human Intraperitoneal α Radioimmunotherapy With 212Pb-TCMC-Trastuzumab
journal, January 2018

Proton-induced cross sections relevant to production of 225Ac and 223Ra in natural thorium targets below 200MeV
journal, November 2012

Enhanced Retention of the α-Particle-Emitting Daughters of Actinium-225 by Liposome Carriers
journal, November 2007

Bystander effects and radiotherapy
journal, January 2015

Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for alpha radionuclide therapy
journal, November 2015

Targeting of Radio-Isotopes for Cancer Therapy
journal, April 2004

Targeted alpha-radionuclide therapy of functionally critically located gliomas with 213Bi-DOTA-[Thi8,Met(O2)11]-substance P: a pilot trial
journal, February 2010

Treatment of Metastatic Bone Disease and the Emerging Role of Radium-223
journal, March 2016

Significant systemic therapeutic effects of high-LET immunoradiation by 212Pb-trastuzumab against prostatic tumors of androgen-independent human prostate cancer in mice
journal, February 2012

Targeted Alpha Therapy with 213Bi
journal, October 2011

Pharmacokinetics and Imaging of ²¹² Pb-TCMC-Trastuzumab After Intraperitoneal Administration in Ovarian Cancer Patients
journal, February 2014

The Metabolism of Actinium in the Rat
journal, January 1970

213Bi-PSMA-617 targeted alpha-radionuclide therapy in metastatic castration-resistant prostate cancer
journal, March 2017

Absorbed Doses and Risk Estimates of 211At-MX35 F(ab')2 in Intraperitoneal Therapy of Ovarian Cancer Patients
journal, November 2015

A new internal target system for production of 211At on the cyclotron U-120M
journal, July 2005

B7-H3-targeted 212Pb radioimmunotherapy of ovarian cancer in preclinical models
journal, April 2017

Production of 211 At by a vertical beam irradiation method
journal, December 2014

Radioimmunotherapy with Bismuth-213 as Conditioning for Nonmyeloablative Allogeneic Hematopoietic Cell Transplantation in Dogs: A Dose Deescalation Study
journal, January 2004

A randomized, dose–response, multicenter phase II study of radium-223 chloride for the palliation of painful bone metastases in patients with castration-resistant prostate cancer
journal, March 2012

Different ways to improve the clinical effectiveness of radioimmunotherapy in solid tumors
journal, January 2009

213Bi-DOTATOC receptor-targeted alpha-radionuclide therapy induces remission in neuroendocrine tumours refractory to beta radiation: a first-in-human experience
journal, July 2014

Renal Tubulointerstitial Changes after Internal Irradiation with α-Particle–Emitting Actinium Daughters
journal, June 2005

Metabolic Characteristics Within a Chemical Family
journal, January 1959

Intraperitoneal -Particle Radioimmunotherapy of Ovarian Cancer Patients: Pharmacokinetics and Dosimetry of 211At-MX35 F(ab')2--A Phase I Study
journal, June 2009

A kit method for the high level synthesis of [211At]MABG
journal, May 2007

MIRD Pamphlet No. 22 (Abridged): Radiobiology and Dosimetry of -Particle Emitters for Targeted Radionuclide Therapy
journal, January 2010

Intralesional targeted alpha therapy for metastatic melanoma
journal, December 2005

Improved efficacy of α-particle-targeted radiation therapy: Dual targeting of human epidermal growth factor receptor-2 and tumor-associated glycoprotein 72
journal, February 2010

Selective Killing of Tumor Neovasculature Paradoxically Improves Chemotherapy Delivery to Tumors
journal, November 2010

Sequential Cytarabine and α-Particle Immunotherapy with Bismuth-213–Lintuzumab (HuM195) for Acute Myeloid Leukemia
journal, September 2010

Mitigation of radiation nephropathy after internal α-particle irradiation of kidneys
journal, April 2006

Theoretical estimation of absorbed dose to organs in radioimmunotherapy using radionuclides with multiple unstable daughters
journal, September 2001

Improved tumor imaging and therapy via i.v. IgG–mediated time-sequential modulation of neonatal Fc receptor
journal, September 2007

Melanoma Therapy via Peptide-Targeted -Radiation
journal, August 2005

Large scale accelerator production of 225Ac: Effective cross sections for 78–192 MeV protons incident on 232Th targets
journal, December 2016

Radioimmunotherapy of Breast Cancer Metastases with -Particle Emitter 225Ac: Comparing Efficacy with 213Bi and 90Y
journal, November 2009

The Relative Radiosensitivity of the Nucleus and Cytoplasm of Chinese Hamster Fibroblasts
journal, June 1970

Effective treatment of ductal carcinoma in situ with a HER-2- targeted alpha-particle emitting radionuclide in a preclinical model of human breast cancer
journal, April 2016

Breaking Chemoresistance and Radioresistance with [ ²¹³ Bi]anti-CD45 Antibodies in Leukemia Cells
journal, March 2007

Interim analysis of toxicity and response in phase 1 trial of systemic targeted alpha therapy for metastatic melanoma
journal, June 2007

An²²⁵Ac/²¹³Bi generator system for therapeutic clinical applications: construction and operation
journal, May 1999

Evaluation of ²²⁵ Ac for Vascular Targeted Radioimmunotherapy of Lung Tumors
journal, June 2000

Pharmacokinetics and toxicity of 213Bi-labeled PAI2 in preclinical targeted alpha therapy for cancer
journal, June 2007

New insights on cell death from radiation exposure
journal, July 2005

Astatine-211: Production and Availability
journal, July 2011

Remodeling the Vascular Microenvironment of Glioblastoma with -Particles
journal, June 2016

213Bi-[DOTA0, Tyr3]Octreotide Peptide Receptor Radionuclide Therapy of Pancreatic Tumors in a Preclinical Animal Model
journal, February 2006

Efforts to Control the Errant Products of a Targeted In vivo Generator
journal, June 2005

Long-Term Toxicity of 213Bi-Labelled BSA in Mice
journal, March 2016

Cytotoxicity of 213Bi- and 225Ac-immunoconjugates
journal, January 1995