Thorium and Actinium Polyphosphonate Compounds As Bone-seeking Alpha Particle-emitting Agents
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The present study explores the use of alpha-particle-emitting, bone-seeking agents as candidates for targeted radiotherapy. Actinium and thorium 1,4,7,10 tetraazacyclododecane N,N',N'',N''' 1,4,7,10-tetra(methylene) phosphonic acid (DOTMP) and thorium-diethylene triamine N,N',N'' penta(methylene) phosphonic acid (DTMP) were prepared and their biodistribution evaluated in conventional Balb/C mice at four hours after injection. All three bone-seeking agents showed a high uptake in bone and a low uptake in soft tissues. Among the soft tissue organs, only kidney had a relatively high uptake. The femur/kidney ratios for 227Th-DTMP, 228-Ac-DOTMP and 227Th-DOTMP were 14.2, 7.6 and 6.0, respectively. A higher liver uptake of 228Ac-DOTMP was seen than for 227Th-DTMP and 227Th-DOTMP. This suggests that some demetallation of the 228Ac-DOTMP complex had occurred. The results indicate that 225Ac-DOTMP, 227Th-DOTMP and 227Th-DTMP have promising properties as potential therapeutic bone-seeking agents.
Rubira L, Deshayes E, Santoro L, Kotzki P, Fersing C Pharmaceutics. 2023; 15(4).
PMID: 37111537 PMC: 10146019. DOI: 10.3390/pharmaceutics15041051.
Juzeniene A, Stenberg V, Bruland O, Revheim M, Larsen R Front Med (Lausanne). 2023; 9:1051825.
PMID: 36733936 PMC: 9887039. DOI: 10.3389/fmed.2022.1051825.
Harnessing -Emitting Radionuclides for Therapy: Radiolabeling Method Review.
Yang H, Wilson J, Orvig C, Li Y, Wilbur D, Ramogida C J Nucl Med. 2021; 63(1):5-13.
PMID: 34503958 PMC: 8717181. DOI: 10.2967/jnumed.121.262687.
Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The "Hopeful Eight".
Eychenne R, Cherel M, Haddad F, Guerard F, Gestin J Pharmaceutics. 2021; 13(6).
PMID: 34207408 PMC: 8234975. DOI: 10.3390/pharmaceutics13060906.
Theoretical Study of Actinide(III)-DOTA Complexes.
Kovacs A ACS Omega. 2021; 6(20):13321-13330.
PMID: 34056480 PMC: 8158830. DOI: 10.1021/acsomega.1c01292.