TAT-10: Exploration of the Chemistry of Astatine; From Basic Research Towards Applied Questions

Kanazawa, Japan (UroToday.com) Conventional As211 labeling protocols are based on astatine as an iodine analog. These are lacking since astatbenzoate-labeled compounds are unstable when metabolized, contrary to the iodine analog. We have developed a number of both calculational and experimental tools to understand the basic chemistry of astatine.

TAT-10: Progress in the [At211]-Astatination of Antibodies by Nuclephilic Approaches Using Aryliodonium Salts Precursors

Kanazawa, Japan (UroToday.com) In this study, we develop a method for At211 radio-labeling based on aryliodonium salts and compare with the more conventional approach using arylstannane chemistry. We find improved yields of 43 +/- 2 % for aryliodonium compared with 20 +/- 5% for arylstannane.

TAT-10: Quality Assurance and Labeling Chemistry Qualification for cGMP Production of Astatine-211-labeled anti-CD45 Antibodies

Kanazawa, Japan (UroToday.com) For a drug to be used on humans the US Food and Drug Administration requires current Good Manufacturing Practice (cGMP), a set of regulations that assure proper design, monitoring,  and control of manufacturing, process, and facilities. The objective of research reported here is to set up procedures to translate the production of At211-labeled anti-CD45 antibodies from benchtop to cGMP-compliant results. This requires demonstration of purity, safety, and sterility of compound produced under cGMP conditions.

TAT-10: Development of Effective Chelators for Th227 to be Used in Targeted Thorium Conjugates

Kanazawa, Japan (UroToday.com) Ra223 represents a breakthrough in alpha therapy after FDA approval in May 2013 of Ra223 – dichloride (XOFIGO) for the treatment of metastatic castration-resistant prostate cancer. As a calcium analog, Ra223 is well-suited for treatment of bone metastases but the absence of efficient chelators limit its use in other types of radiotherapy. The same generators used for Ra223 production can be also be used for highly purified Th-227. This study aims to produce efficient chelators for Th227.

TAT-10: Spectroscopic and Computational Studies of Actinium Coordination Chemistry

Kanazawa, Japan (UroToday.com) Ac225 is a very promising isotope for targeted alpha therapy. Production of efficient, pure conjugates would benefit from a better understanding of the basic actinium chemistry. In contrast to the tracer-level quantities of Ac225, Ac227 (half-life 22y) is available in microgram quantities which enables traditional chemical techniques. Using our stock of 150 mg (10 mCi) of Ac227, we have developed multiple spectroscopic and theoretical approaches to understand Ac coordination chemistry.

TAT-10: A Novel Micro-Actinium225-Bismuth212 Biomedical Generator System

Kanazawa, Japan (UroToday.com) A micro-fluidic “lab-on-a-chip” was described for the separation of Bi213. Miniturization has certain advantage such as efficient use of reagents and minimizing radioactivity exposure to workers even while producing enough Bi213 for individual patient injection or lab studies.

TAT-10: US DOE Tri-Lab Research Effort to Provide Accelerator produced Ac225 for radiotherapy: 2017 Update

Kanazawa, Japan (UroToday.com) The US DOE’s isotope program at three of its national labs (LANL, Oak Ridge, and BNL) is an on-going program to produce Ac225 isotopes for research and patient treatment. The BNL Brookhaven Linear Isotope Producer (BLIP) uses excess pulses diverted from the primary proton linac serving the BNL accelerator complex.
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