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Comparative Study
. 1999 Jul;26(5):581-9.
doi: 10.1016/s0969-8051(99)00024-4.

Comparison of 225actinium chelates: tissue distribution and radiotoxicity

I A Davis  1 , K A Glowienka, R A Boll, K A Deal, M W Brechbiel, M Stabin, P N Bochsler, S Mirzadeh, S J Kennel
Affiliations
Comparative Study

Comparison of 225actinium chelates: tissue distribution and radiotoxicity

I A Davis et al. Nucl Med Biol. 1999 Jul.

Abstract

The biodistribution and tissue toxicity of intravenously administered 225-actinium (225Ac) complexed with acetate, ethylene diamine tetraacetic acid (EDTA), 1, 4, 7, 10, 13-pentaazacyclopentadecane-N, N', N", N"', N""-pentaacetic acid (PEPA), or the "a" isomer of cyclohexyl diethylenetriamine pentaacetic acid (CHX-DTPA), were examined. The percent of injected dose per organ and per gram of tissue for each chelate complex was determined. 225Ac-CHX-DTPA was evaluated further for radiotoxic effects. Mice receiving > or =185 kBq 225Ac-CHX-DTPA suffered 100% morbidity by 5 days and 100% mortality by 8 days postinjection, and all animals evaluated had significant organ damage. The in vivo instability of the 225Ac-CHX-DTPA complex likely allowed accumulation of free 225Ac in organs, which resulted in tissue pathology.

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