Preparation and evaluation of 99mTc(V)-DMSA complex: Studies in medullary carcinoma of thyroid

Ramamoorthy, N.; Shetye, Smita V.; Pandey, Pradeep; Mani, R. S.; Patel, Mohan N.; Patel, Rajesh; Ramanathan, P.; Krishna, B A Rama; Sharma, S. M.

doi:10.1007/bf00284540

Cited by 19 publications

(4 citation statements)

References 2 publications

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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: 91%

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

Guhlke¹,

Scheithauer²,

Oetjen³

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.

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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: 91%

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

Guhlke¹,

Scheithauer²,

Oetjen³

et al. 2004

Radiochimica Acta

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“…[17][18][19][20] Since 1975, there have been also numerous studies on 99m Tc-DMSA complexes and their use in medical imaging especially for cancer detection. [21][22][23][24] Most of the studies on DMSA focus on complexation of heavy metals such as arsenic, mercury and lead. 19,[25][26][27][28] There are several reports on Zn complexes and very few on Cd complexes of DMSA.…”

Section: Introductionmentioning

confidence: 99%

Meso-2,3-dimercaptosuccinic acid: from heavy metal chelation to CdS quantum dots

et al. 2012

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DMSA (meso-2,3-dimercaptosuccinic acid) a prescription drug and a heavy-metal chelating agent, is shown to act both as a sulfur source and a capping agent in the aqueous synthesis of CdS quantum dots under mild conditions. Release of sulfur from DMSA depends on the solution pH and the reaction temperature. Combination of 70 C and pH 7.5 was determined as the best reaction conditions for a well-controlled reaction. Changing the SH/Cd ratio from 2.5 to 7 provides QDs emitting from blue to orange with 6-9% quantum yield with respect to Rhodamine 2B. Viability tests performed with HeLa and MCF-7 cell lines indicate a very low cytotoxicity. Mild reaction conditions and biocompatibility makes these particles valuable candidates for bio applications.

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“…The formation of pentavalent 99m Tc-DMSA complex occurs at elevated pH; therefore, 0.2 ml of a sterile solution of 3.5% sodium bicarbonate is added to the lyophilized DMSA kit before adding 99m Tc-sodium pertechnetate (Ramamoorthy et al 1987). The optimal pH for 99m Tc(V)-DMSA formation is pH 7.5±8.0; the resulting concentration of stannous ion produced a complex with high stability (6 h).…”

Section: Description Of the Kitmentioning

confidence: 99%

“…Pentavalent 99m Tc(V)-DMSA differs structurally and has been evaluated for imaging medullary carcinoma of the thyroid (Ohta et al 1984;Ramamoorthy et al 1987). The sensitivity of lesion detection is 95%; no false positive uptake of 99m Tc(V)-DMSA was seen in nine patients with a histologic diagnosis of medullary carcinoma.…”

Section: Pharmacokinetic Datamentioning

confidence: 99%

Technetium-99m Pharmaceuticals

Zolle¹

2007

103

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Foreword 99m Tc pharmaceuticals mark the beginning of diagnostic nuclear medicine and have contributed to patient care worldwide. Since the short-lived radionuclide was introduced for thyroid imaging in 1964, it has attracted much attention and stimulated clinical research. Little was known about element 43, except that it was an artificial radionuclide obtained by the radioactive decay of molybdenum-99. No wonder specialists from all fields joined medical institutions in the United States to participate in the exploration of its chemistry.This textbook gives an account of the accomplishments related to the development of 99m Tc pharmaceuticals and their application in diagnostic nuclear medicine. Since radioactive drug development is a multidisciplinary task, experts working in nuclear medicine and research institutions have contributed valuable information concerning the preparation with sterile kits, methods of quality control, and the use of 99m Tc pharmaceuticals in patients. In addition, the legal aspects governing production and clinical application are also considered.99m Tc pharmaceuticals in nuclear medicine are presented in two parts. Part 1 includes basic principles and methods used for preparation and analysis, in particular the chemistry of technetium-99m and methods described for the synthesis of complexes and conjugates of technetium-99m, the characteristics and performance of the 99 Mo/ 99m Tc generator system, the importance of kits and formulations for one-step labeling, and safety aspects for labeling blood cells. Special emphasis is given to analytical methods verifying pharmaceutical quality. The quality standards of good manufacturing practice (GMP) for 99m Tc pharmaceuticals and purity standards of the pharmacopeia (European Pharmacopeia and United States Pharmacopeia) have been considered as part of the concept of quality assurance.Part 2 presents 26 monographs of 99m Tc pharmaceuticals, concerning the preparation and safe clinical application. Each monograph provides information on the characteristics of the radiotracer based on chemistry, factors affecting the preparation and in vivo stability, pharmacokinetics and elimination properties, as well as details concerning the clinical application. For each clinical procedure, the effective radiation dose of the patient has been calculated. Methods recommended for quality control and actual results are included.Each radiopharmaceutical is listed under the name used in daily practice. The chemical name, the abbreviated name, and the officinal name in the pharmacopeia are also stated. Listing the trade names may facilitate understanding, especially when relating to products in the literature, which over the years have changed manufacturers.The presentation of 99m Tc pharmaceuticals as monographs serves a practical purpose: it offers relevant information on kit preparation and clinical application at a glance. These monographs provide a wide spectrum of information on 99m Tc pharmaceuticals for daily practice in nuclear medicine, serving as a r...

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Preparation and evaluation of 99mTc(V)-DMSA complex: Studies in medullary carcinoma of thyroid

Cited by 19 publications

References 2 publications

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

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

Meso-2,3-dimercaptosuccinic acid: from heavy metal chelation to CdS quantum dots

Technetium-99m Pharmaceuticals

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Preparation and evaluation of 99mTc(V)-DMSA complex: Studies in medullary carcinoma of thyroid

Cited by 19 publications

References 2 publications

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

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

Meso-2,3-dimercaptosuccinic acid: from heavy metal chelation to CdS quantum dots

Technetium-99m Pharmaceuticals

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

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