Applied Radiation and Isotopes

2001

DOI: 10.1016/s0969-8043(00)00278-5

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Uptake of the 188Re(V)-DMSA complex by cervical carcinoma cells in nude mice: pharmacokinetics and dosimetry

L. García-Salinas

¹

,

Guillermina Ferro-Flores

²

,

C Arteaga-Murphy

³

et al.

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Cited by 10 publications

(5 citation statements)

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“…The organ biodistribution results are in accordance with earlier published results obtained with isomeric mixtures of either 188 Re-DMSA in mice [1,2,7] or 99m Tc(V)-DMSA in rats [18].…”

Section: In-vivo Resultssupporting

confidence: 90%

“…therapy of bone pain generated by metastatic prostate cancers [1]. Considerable uptake of 188 Re-DMSA was observed in cervical carcinoma cells in a nude mice model [2]. The Re-labeled DMSA has also been discussed for therapy of medullary thyroid carcinoma [3,4] as well as for head and neck tumors [5]; however its therapeutic use could not be established for this purpose so far.…”

Section: Introductionmentioning

confidence: 99%

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¹⁸⁸Re(V)-DMSA: in-vitro and in-vivo studies on the individual stereo isomers

et al. 2004

Radiochimica Acta

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188 Re(V)-DMSA; Re-188 / Stereo isomers / Radio-therapy Summary. The pentavalent rhenium-188 meso-dimercaptosuccinic acid complex 188 Re(V)-DMSA is a beta-emitting analogue of Tc99 m (V)-DMSA, an established tracer that is taken up in a variety of histological different tumors and especially in bone metastases arising from breast and prostate carcinomas. The similar general biodistribution and tumor avidity of 188 Reand 99m Tc(V)-DMSA therefore suggests the use of the rhenium analog as an agent for therapeutic applications. No-carrier-added 188 Re(V)-DMSA is composed of a mixture of three stereoisomers arising from different orientations of the 4 carboxylate groups of the complex. For therapeutic applications it must be known whether there is a difference in the in-vivo biodistribution and kinetics of the individual stereo isomers. The aim of this study was therefore a) to characterize the chemical stability of each of the 3 stereoisomers with respect to time, temperature and pH and b) to evaluate if there are differences in the in-vivo organ distribution of the pure isomers compared to the isomeric mixture.The in-vitro results revealed for all three individual isomers of 188 Re(V)-DMSA a rather slow (with respect to half-life of Re-188) temperature and pH dependent rate of interconversion which would justify the application of pure isomers. The data obtained from urine samples of rats showed a faster interconversion rate and reached a stable isomer distribution after about six to ten hours, depending on which isomer was injected. However there was no evidence for isomer specific excretion rates. The organ biodistribution patterns of all three isomers were very similar at all times studied (10 min up to 24 hours p.i). The tumor uptake in a rat mammary carcinoma model at 1 hour p.i. did also not show any significant differences.In conclusion the preparation and administration of pure stereoisomers of 188 Re-DMSA is possible, however, in-vivo no significant differences in organ distribution and kinetics were observed which would favour the use of purified stereo isomers over the isomeric mixture of 188 Re(V)-DMSA.

“…The organ biodistribution results are in accordance with earlier published results obtained with isomeric mixtures of either 188 Re-DMSA in mice [1,2,7] or 99m Tc(V)-DMSA in rats [18].…”

Section: In-vivo Resultssupporting

confidence: 90%

“…therapy of bone pain generated by metastatic prostate cancers [1]. Considerable uptake of 188 Re-DMSA was observed in cervical carcinoma cells in a nude mice model [2]. The Re-labeled DMSA has also been discussed for therapy of medullary thyroid carcinoma [3,4] as well as for head and neck tumors [5]; however its therapeutic use could not be established for this purpose so far.…”

Section: Introductionmentioning

confidence: 99%

¹⁸⁸Re(V)-DMSA: in-vitro and in-vivo studies on the individual stereo isomers

et al. 2004

Radiochimica Acta

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188 Re(V)-DMSA; Re-188 / Stereo isomers / Radio-therapy Summary. The pentavalent rhenium-188 meso-dimercaptosuccinic acid complex 188 Re(V)-DMSA is a beta-emitting analogue of Tc99 m (V)-DMSA, an established tracer that is taken up in a variety of histological different tumors and especially in bone metastases arising from breast and prostate carcinomas. The similar general biodistribution and tumor avidity of 188 Reand 99m Tc(V)-DMSA therefore suggests the use of the rhenium analog as an agent for therapeutic applications. No-carrier-added 188 Re(V)-DMSA is composed of a mixture of three stereoisomers arising from different orientations of the 4 carboxylate groups of the complex. For therapeutic applications it must be known whether there is a difference in the in-vivo biodistribution and kinetics of the individual stereo isomers. The aim of this study was therefore a) to characterize the chemical stability of each of the 3 stereoisomers with respect to time, temperature and pH and b) to evaluate if there are differences in the in-vivo organ distribution of the pure isomers compared to the isomeric mixture.The in-vitro results revealed for all three individual isomers of 188 Re(V)-DMSA a rather slow (with respect to half-life of Re-188) temperature and pH dependent rate of interconversion which would justify the application of pure isomers. The data obtained from urine samples of rats showed a faster interconversion rate and reached a stable isomer distribution after about six to ten hours, depending on which isomer was injected. However there was no evidence for isomer specific excretion rates. The organ biodistribution patterns of all three isomers were very similar at all times studied (10 min up to 24 hours p.i). The tumor uptake in a rat mammary carcinoma model at 1 hour p.i. did also not show any significant differences.In conclusion the preparation and administration of pure stereoisomers of 188 Re-DMSA is possible, however, in-vivo no significant differences in organ distribution and kinetics were observed which would favour the use of purified stereo isomers over the isomeric mixture of 188 Re(V)-DMSA.

“…Bolzati et al have proposed a new approach (70) for the synthesis of 188 Re(V)-DMSA, requiring less stringent conditions. The biological properties of 188 Re(V)-DMSA have been studied in animals and humans (71, 72). The results in patients showed a selective attachment to tumor tissues, particularly to metastatic bone cancer originating from prostatic carcinoma, similar to that of the technetium analog (73).…”

Section: Re-labeled Small Moleculesmentioning

confidence: 99%

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

¹

,

²

,

³

et al. 2019

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Rhenium-188 ( 188 Re) is a high energy beta-emitting radioisotope with a short 16.9 h physical half-life, which has been shown to be a very attractive candidate for use in therapeutic nuclear medicine. The high beta emission has an average energy of 784 keV and a maximum energy of 2.12 MeV, sufficient to penetrate and destroy targeted abnormal tissues. In addition, the low-abundant gamma emission of 155 keV (15%) is efficient for imaging and for dosimetric calculations. These key characteristics identify 188 Re as an important therapeutic radioisotope for routine clinical use. Moreover, the highly reproducible on-demand availability of 188 Re from the 188 W/ 188 Re generator system is an important feature and permits installation in hospital-based or central radiopharmacies for cost-effective availability of no-carrier-added (NCA) 188 Re. Rhenium-188 and technetium-99 m exhibit similar chemical properties and represent a “theranostic pair.” Thus, preparation and targeting of 188 Re agents for therapy is similar to imaging agents prepared with 99m Tc, the most commonly used diagnostic radionuclide. Over the last three decades, radiopharmaceuticals based on 188 Re-labeled small molecules, including peptides, antibodies, Lipiodol and particulates have been reported. The successful application of these 188 Re-labeled therapeutic radiopharmaceuticals has been reported in multiple early phase clinical trials for the management of various primary tumors, bone metastasis, rheumatoid arthritis, and endocoronary interventions. This article reviews the use of 188 Re-radiopharmaceuticals which have been investigated in patients for cancer treatment, demonstrating that 188 Re represents a cost effective alternative for routine clinical use in comparison to more expensive and/or less readily available therapeutic radioisotopes.

“…The simple synthesis of the 188 Re complexes and wide interest in these applications led to development of kit-based labelling, [37,38] and preclinical evaluation in normal mice [39,40] and in other tumours (e.g. cervical carcinoma models [41]). Further study showed that the individual isomers showed no significant differences in biodistribution, and underwent interconversion, in rats [42] and (in the case of [ 99m TcO(DMSA) 2 ] -) in humans [43].…”

Section: Rhenium (V) Complexesmentioning

confidence: 99%

Rhenium-188 Radiochemistry: Challenges and Prospects

2017

Int. J. Nucl. Medi. Res.

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After a lull in development of new chemistry for rhenium-188 and technetium-99m since 2000, there has been new investment in production facilities for Mo-99/Tc-99m coupled with increasing interest in rhenium-188 radionuclide therapy, particularly in developing countries. Much of the chemistry developed in the 1990s is not readily amenable to supporting modern radiopharmaceutical development, which places increased emphasis on molecular targeted radiopharmaceuticals. Consequently there is a need for new radiolabelling chemistry to incorporate these radionuclides into biomolecules using simple, kit-based methodology. This review provides an update on progress towards simple rhenium-188 labelling methods since 2000.

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