Journal Article

FZJ-2026-02484

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Reconsidering astatine-211 analytics: Retention effects in reversed-phase HPLC

Humpert, S.FZJ* ; Mues, L.FZJ* ; Pedersen, N. B. ; Neumaier, F.FZJ* ; Herth, M. M. ; Neumaier, B. (Corresponding author)FZJ*

2026
Science Direct New York, NY [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.jpba.2026.117547

Abstract: Astatine-211 is a short-lived alpha-emitting radionuclide with high potential for cancer treatment by targeted alpha therapy (TAT). Reversed-phase high-performance liquid chromatography (RP-HPLC) is central to the development and quality control of 211At-labeled radiopharmaceuticals. However, accurate analysis remains challenging due to the ultra-trace levels of astatine and its complex, unpredictable chemical behaviour. In this study, we systematically evaluated the recovery of representative inorganic astatine formulations under different redox conditions using various chromatographic conditions, which is a prerequisite for reliable quantification. Examination of four different columns with distinct stationary phase chemistry demonstrated that significant discrepancies can arise when radiochemical conversion is assessed solely based on eluted activity, as is common standard for RP-HPLC analysis. Among the chromatographic conditions examined, the highest and most consistent astatine recoveries (88−98%) were achieved using a basic mobile phase containing 0.4% triethylamine in combination with a base-tolerant stationary phase, likely due to a shift in astatine speciation under alkaline conditions, reduced secondary interactions with the stationary phase, and/or potentially beneficial ion pairing effects. In contrast, widely used standard solvent systems based on acetonitrile/water with or without 0.1% trifluoroacetic acid resulted in unsatisfactory and highly variable recoveries (7−71% or 30−79%, respectively) across all columns investigated. These findings highlight the necessity of optimized chromatographic conditions and suggest that inadequate recovery of free astatine could lead to substantial misestimation of the radiochemical conversion and purity of radiopharmaceutical formulations if not explicitly accounted for by auxiliary quantification strategies.

Note: This project was supported by the Innovative Health Initiative Joint Undertaking (IHI JU) under grant agreement No 101173001 — Accelerate.EU. The JU receives support from the European Union’s Horizon Europe research and innovation programme and COCIR, EFPIA, Europa Bío, MedTech Europe, Vaccines Europe, IBA, Tetrakit, and LabLogic.

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 5253 - Neuroimaging (POF4-525) (POF4-525)

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Database coverage:
; BIOSIS Previews ; Biological Abstracts ; Clarivate Analytics Master Journal List ; Current Contents - Life Sciences ; Ebsco Academic Search ; Essential Science Indicators ; IF < 5 ; JCR ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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