Chemistry of Antimony in Radiopharmaceutical Development: Unlocking the Theranostic Potential of Sb Isotopes

Overview

Journal Chempluschem

Specialty Chemistry

Date 2024 Jul 24

PMID 39048512

Authors

Aivija Grundmane

Valery Radchenko

Caterina F Ramogida

Affiliations

Soon will be listed here.

Abstract

Antimony-119 (Sb) holds promise for radiopharmaceutical therapy (RPT), emitting short-range Auger and conversion electrons that can deliver cytotoxic radiation on a cellular level. While it has high promise theoretically, experimental validation is necessary for Sb in vivo applications. Current Sb production and separation methods face robustness and compatibility challenges in radiopharmaceutical synthesis. Limited progress in chelator development hampers targeted experiments with Sb. This review compiles literature on the toxicological, biodistribution and redox properties of Sb, along with existing Sb complexes, evaluating their suitability for radiopharmaceuticals. Sb(III) is suggested as the preferred oxidation state for radiopharmaceutical elaboration due to its stability in vivo and lack of skeletal uptake. While Sb complexes with both hard and soft donor atoms can be achieved, Sb thiol complexes offer enhanced stability and compatibility with the desired Sb(III) oxidation state. For Sb to find application in RPT, scientists need to make discoveries and advancements in the areas of isotope production, and radiometal chelation. This review aims to guide future research towards harnessing the therapeutic potential of Sb in RPT.

Citing Articles

Sustainable production of radionuclidically pure antimony-119.

Olson A, Verich F, Ellison P, Aluicio-Sarduy E, Nickles R, Mixdorf J EJNMMI Radiopharm Chem. 2024; 9(1):72.

PMID: 39438347 PMC: 11496484. DOI: 10.1186/s41181-024-00303-w.

Chemistry of Antimony in Radiopharmaceutical Development: Unlocking the Theranostic Potential of Sb Isotopes.

Grundmane A, Radchenko V, Ramogida C Chempluschem. 2024; 89(12):e202400250.

PMID: 39048512 PMC: 11639648. DOI: 10.1002/cplu.202400250.

References

Grundmane A, Radchenko V, Ramogida C . Chemistry of Antimony in Radiopharmaceutical Development: Unlocking the Theranostic Potential of Sb Isotopes. Chempluschem. 2024; 89(12):e202400250. PMC: 11639648. DOI: 10.1002/cplu.202400250. View

dos Santos Ferreira C, Martins P, Demicheli C, Brochu C, Ouellette M, Frezard F . Thiol-induced reduction of antimony(V) into antimony(III): a comparative study with trypanothione, cysteinyl-glycine, cysteine and glutathione. Biometals. 2003; 16(3):441-6. DOI: 10.1023/a:1022823605068. View

Wilson T, Jannetti S, Guru N, Pillarsetty N, Reiner T, Pirovano G . Improved radiosynthesis of I-MAPi, an auger theranostic agent. Int J Radiat Biol. 2020; 99(1):70-76. PMC: 7775866. DOI: 10.1080/09553002.2020.1781283. View

Litau S, Seibold U, Wangler B, Schirrmacher R, Wangler C . iEDDA Conjugation Reaction in Radiometal Labeling of Peptides with Ga and Cu: Unexpected Findings. ACS Omega. 2018; 3(10):14039-14053. PMC: 6217686. DOI: 10.1021/acsomega.8b01926. View

Capaldo L, Ertl M, Fagnoni M, Knor G, Ravelli D . Antimony-Oxo Porphyrins as Photocatalysts for Redox-Neutral C-H to C-C Bond Conversion. ACS Catal. 2021; 10(16):9057-9064. PMC: 8009479. DOI: 10.1021/acscatal.0c02250. View

King M, Keyes M, Frank S, Crook J, Butler W, Rossi P . Low dose rate brachytherapy for primary treatment of localized prostate cancer: A systemic review and executive summary of an evidence-based consensus statement. Brachytherapy. 2021; 20(6):1114-1129. DOI: 10.1016/j.brachy.2021.07.006. View

Thisgaard H, Jensen M . Production of the Auger emitter 119Sb for targeted radionuclide therapy using a small PET-cyclotron. Appl Radiat Isot. 2008; 67(1):34-8. DOI: 10.1016/j.apradiso.2008.09.003. View

Pirovano G, Wilson T, Reiner T . Auger: The future of precision medicine. Nucl Med Biol. 2021; 96-97:50-53. PMC: 8164972. DOI: 10.1016/j.nucmedbio.2021.03.002. View

Parker C, Nilsson S, Heinrich D, Helle S, OSullivan J, Fossa S . Alpha emitter radium-223 and survival in metastatic prostate cancer. N Engl J Med. 2013; 369(3):213-23. DOI: 10.1056/NEJMoa1213755. View

10.

Liu F, Le X, McKnight-Whitford A, Xia Y, Wu F, Elswick E . Antimony speciation and contamination of waters in the Xikuangshan antimony mining and smelting area, China. Environ Geochem Health. 2010; 32(5):401-13. DOI: 10.1007/s10653-010-9284-z. View

11.

Olson A, Ma L, Feng Y, Najafi Khosroshahi F, Kelley S, Aluicio-Sarduy E . A Third Generation Potentially Bifunctional Trithiol Chelate, Its Sb(III) Complex, and Selective Chelation of Radioantimony (Sb) from Its Sn Target. Inorg Chem. 2021; 60(20):15223-15232. PMC: 8800004. DOI: 10.1021/acs.inorgchem.1c01690. View

12.

Lukaszczyk L, Zyrnicki W . Speciation analysis of Sb(III) and Sb(V) in antileishmaniotic drug using Dowex 1 x 4 resin from hydrochloric acid solution. J Pharm Biomed Anal. 2010; 52(5):747-51. DOI: 10.1016/j.jpba.2010.02.009. View

13.

Handula M, Chen K, Seimbille Y . IEDDA: An Attractive Bioorthogonal Reaction for Biomedical Applications. Molecules. 2021; 26(15). PMC: 8347371. DOI: 10.3390/molecules26154640. View

14.

Besold J, Kumar N, Scheinost A, Pacheco J, Fendorf S, Planer-Friedrich B . Antimonite Complexation with Thiol and Carboxyl/Phenol Groups of Peat Organic Matter. Environ Sci Technol. 2019; 53(9):5005-5015. DOI: 10.1021/acs.est.9b00495. View

15.

Yeong C, Cheng M, Ng K . Therapeutic radionuclides in nuclear medicine: current and future prospects. J Zhejiang Univ Sci B. 2014; 15(10):845-63. PMC: 4201313. DOI: 10.1631/jzus.B1400131. View

16.

Li D, Zhong G . Synthesis and Crystal Structure of the Bioinorganic Complex [Sb(Hedta)]·2H2O. Bioinorg Chem Appl. 2014; 2014:461605. PMC: 3943296. DOI: 10.1155/2014/461605. View

17.

Li Y, Li H, Zhang R, Bing X . Toxicity of antimony to Daphnia magna: Influence of environmental factors, development of biotic ligand approach and biochemical response at environmental relevant concentrations. J Hazard Mater. 2023; 462:132738. DOI: 10.1016/j.jhazmat.2023.132738. View

18.

Xue L, Butler N, Makrigiorgos G, Adelstein S, Kassis A . Bystander effect produced by radiolabeled tumor cells in vivo. Proc Natl Acad Sci U S A. 2002; 99(21):13765-70. PMC: 129772. DOI: 10.1073/pnas.182209699. View

19.

Poddelsky A, Smolyaninov I, Shataeva A, Baranov E, Fukin G . Binuclear Triphenylantimony(V) Catecholates through N-Donor Linkers: Structural Features and Redox Properties. Molecules. 2022; 27(19). PMC: 9573088. DOI: 10.3390/molecules27196484. View

20.

Khangarot B, Ray P . Investigation of correlation between physiochemical properties of metals and their toxicity to the water flea Daphnia magna Straus. Ecotoxicol Environ Saf. 1989; 18(2):109-20. DOI: 10.1016/0147-6513(89)90071-7. View