Bone lesion detection with carrier-added 99mTc-EDTMP in comparison with 99mTc-DPD

Fueger, Barbara J.; Mitterhauser, Markus; Wadsak, Wolfgang; Ofluoglu, Sedat; Traub, Tatjana; Karanikas, Georgios; Dudczak, Robert; Pirich, Christian

doi:10.1097/00006231-200404000-00008

Cited by 20 publications

(11 citation statements)

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“…Again, the order of uptake is in close agreement with our in vitro model. (Füger et al, 2004;Mitterhauser et al, 2001). We found uptake in the order: n.c.a.…”

Section: Discussionmentioning

confidence: 99%

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

Mitterhauser

Toegel²

2008

ALTEX

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The absence of secured knowledge regarding the binding interaction between bone seeking pharmaceuticals and bone, rules out the possibility of modern rational drug design of novel bone seekers. Hence, the first step in the preclinical evaluation of any new bone seeker involves biodistribution and efficacy studies in laboratory animals. Here we report the development of a simple in vitro model for the comparative evaluation of new bone seekers. Additionally, we compared the binding characteristics found in our model with results obtained from animal experiments and evaluated the feasibility of our model to reduce or replace animal experiments in future. Correlations between our in vitro model and data from in vivo, ex vivo and cell culture studies support its applicability. On the basis of our findings we feel confident that this model could serve as a convenient alternative to animal experiments for the comparative evaluation of bone seekers. It could even be a basis for the development of a future pharmacopoeia-listed method allowing both the officinal quality control of bone seekers and a more respectful approach to animals.

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“…Again, the order of uptake is in close agreement with our in vitro model. (Füger et al, 2004;Mitterhauser et al, 2001). We found uptake in the order: n.c.a.…”

Section: Discussionmentioning

confidence: 99%

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

Mitterhauser

Toegel²

2008

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“…This can be achieved by the synthesis of new organic ligands with higher affinity for bone . Many new studies were oriented to synthesized new 99m Tc‐ligands with high affinity to bone . The present study aimed to synthesize a new organic ligand (1‐thioethylidene‐l,l‐disodiumphosphonate [TEDP]; Figure ), of expected high affinity for the bone, to label this new ligand with technetium‐99m, to study the factors affecting the labeling yield in details, and to evaluate its utility as a novel bone scintigraphy radiopharmaceutical, 99m Tc‐TEDP complex, able to detect all bone abnormalities in its early stages.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and preclinical pharmacological evaluation of ^99mTc‐TEDP as a novel bone imaging agent

Motaleb

Sakr

2011

Labelled Comp Radiopharmac

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The detection of bone metastasis in early stages requires the development of high-affinity bone imaging radiopharmaceuticals for the improvement of the diagnostic accuracy of routine bone scanning and effective management of these medical cases. This study aimed to provide a convenient synthesis of 1-thioethylidene-l,l-disodiumphosphonate (TEDP) and an improved preparation of its 99m Tc-TEDP complex. The results showed that the radiochemical purity of 99m Tc-TEDP was found to be 95 ± 2% and that its stability was up to 6 h. Biodistribution study showed high and long uptake of 99m Tc-TEDP in bone starting from 15 min (39 ± 4 ID/g) to 3 h (53 ± 2.4 ID/g) showing high affinity of 99m Tc-TEDP complex to bones. This research could introduce a novel radiopharmaceutical that could be used in scanning body bones starting from 15 min between injection of 99m Tc-TEDP and bone imaging, minimizing the burden on patients in terms of the total length of the examination and the dose of radiation absorbed and showing high specificity and efficacy in bone scintigraphy.

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“…Analysis of published data indicates that 99m Tc-EDTMP has tropism for bony tissue, though systematic studies in this area remain to be performed [12,13].…”

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The Pharmacokinetics of Technetium-99m-Labeled N,N,N′,N′-Ethylenediaminetetra-Kis-(Methylenephosphonic Acid) in Intact Rats

et al. 2015

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Pharmacokinetic studies of technetium-99m-labeled N,N,N¢,N¢-ethylenediaminetetra-kis-(methylenephosphonic acid) ( 99m Tc-EDTMP) showed that this radiopharmaceutical (RP) has high in vivo stability. Studies of the biodistribution of 99m Tc-EDTMP were performed in healthy rats. Labeled agent was found to accumulate mainly in bone tissue. The greatest activity in the skeleton, (1.93 ± 0.12)%/g, was seen 1 h after i.v. administration. Accumulation of 99m Tc-EDTMP content in the skeleton was 4.7 -24.3 times greater than that of sodium pertechnetate (Na 99m TcO 4 ) (p < 0.001). Numerical values for differential accumulation coefficients (DAC) for activity in bones and internal organs and tissues were found to increase gradually to maximum values 3 h after i.v. administration. RP was eliminated mainly via the urinary tract. Study agent was rapidly cleared from the blood and only minor quantities accumulated in the internal organs. Contents were lower than those of Na 99m TcO 4 in in virtually all organs and tissues. These results indicate that 99m Tc-EDTMP can be regarded as a potential RP for diagnostic investigations of bone tissues.The main method for diagnosis of metastatic lesions in bone tissue is bone scintigraphy using 99m Tc-labeled phosphonic acids. 99m Tc has an optimum decay halflife (6 h) and gamma quantum energy (140 keV). These agents have affinity for hydroxyapatite in the bone matrix and show selective accumulation in zones with increased mineralization requirements, predominantly metastatic and inflammatory-destructive foci [1 -11]. At the same time, the need for osteoscintigraphy with maximal sensitivity and specificity is driving an intense search for new radiopharmaceuticals (RP) based on phosphonic acids.Among the polyaminophosphonic acids, there is great interest in N,N,N¢,N¢-ethylenediaminetetra-kis-(methylenephosphonic acid) (EDTMP). This is used as the basis of the agent 153 Sn-EDTMP (Lexidronam), which has undergone clinical trials and is used in clinical practice.Analysis of published data indicates that 99m Tc-EDTMP has tropism for bony tissue, though systematic studies in this area remain to be performed [12,13].We have therefore conducted detailed studies of the pharmacokinetic properties of 99m Tc-EDTMP in intact laboratory animals.

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Bone lesion detection with carrier-added 99mTc-EDTMP in comparison with 99mTc-DPD

Cited by 20 publications

References 5 publications

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

Synthesis and preclinical pharmacological evaluation of ^99mTc‐TEDP as a novel bone imaging agent

The Pharmacokinetics of Technetium-99m-Labeled N,N,N′,N′-Ethylenediaminetetra-Kis-(Methylenephosphonic Acid) in Intact Rats

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Bone lesion detection with carrier-added 99mTc-EDTMP in comparison with 99mTc-DPD

Cited by 20 publications

References 5 publications

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

An in vitro model for the comparative evaluation of bone seeking pharmaceuticals

Synthesis and preclinical pharmacological evaluation of 99mTc‐TEDP as a novel bone imaging agent

The Pharmacokinetics of Technetium-99m-Labeled N,N,N′,N′-Ethylenediaminetetra-Kis-(Methylenephosphonic Acid) in Intact Rats

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Synthesis and preclinical pharmacological evaluation of ^99mTc‐TEDP as a novel bone imaging agent