99mTc-hydroxymethane diphosphonate: a new bone imaging agent with a low tin content.

Domstad, Peggy A.; Coupal, John J.; Kim, E E; Blake, J.; DeLand, Frank H.

doi:10.1148/radiology.136.1.6446106

Cited by 33 publications

(16 citation statements)

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“…DOTA-Bn-SCN-HBP (3) as a precursor was synthesized by a Ogawa et al 13/35 coupling reaction between p-SCN-Bn-DOTA (1) and alendronate (2) according to Scheme 1. 67 Ga labeling was performed by complexation between DOTA-Bn-SCN-HBP or DOTA and 67 Ga.…”

Section: Preparation Of 67 Ga-labeled Compoundsmentioning

confidence: 99%

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Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Ogawa

Takai

Kanbara

et al. 2011

Nuclear Medicine and Biology

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Introduction:68 Ga is a radionuclide of great interest as a positron emitter for PET. To develop a new bone-imaging agent with radiogallium, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was chosen as a chelating site and Ga-DOTA complex-conjugated bisphosphonate, which has a high affinity for bone, was prepared and evaluated. Although we are interested in developing 68 Ga labeled bone imaging agents for PET, in these initial studies 67 Ga was used because of its longer half-life. Methods:DOTA-conjugated bisphosphonate (DOTA-Bn-SCN-HBP) was synthesized by conjugation of 2-(4-isothiocyanatebenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraac etic acid (p-SCN-Bn-DOTA) to 4-amino-1-hydroxybutylidene-1,1-bisphosphonate (alendronate).67 Ga-DOTA-Bn-SCN-HBP was prepared by coordination with 67 Ga, and its in vitro and in vivo evaluations were performed. Ogawa et al. 4/35 Results:67 Ga-DOTA-Bn-SCN-HBP was prepared with a radiochemical purity of over 95% without purification. 67 Ga-DOTA-Bn-SCN-HBP had great affinity for hydroxyapatite in binding assay. In biodistribution experiments, 67 Ga-DOTA-Bn-SCN-HBP accumulated in bone rapidly but was hardly observed in tissues other than bone. Pretreatment of an excess amount of alendronate inhibited the bone accumulation of 67 Ga-DOTA-Bn-SCN-HBP. Conclusions:67 Ga-DOTA-Bn-SCN-HBP showed ideal biodistribution characteristics as a bone-imaging agent. These findings should provide useful information on the drug design of bone-imaging agents for PET with 68 Ga. Ogawa et al. 5/35

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Section: Preparation Of 67 Ga-labeled Compoundsmentioning

confidence: 99%

“…Over the last thirty years, complexes of 99m Tc with bisphosphonate, such as methylene diphosphonate ( 99m Tc-MDP) and hydroxymethylene diphosphonate ( 99m Tc-HMDP), have been widely used as radiopharmaceuticals for the imaging of bone disorders such as metastatic bone disease, Paget's disease, osteoporotic fractures, etc [1][2][3][4].…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Ogawa

Takai

Kanbara

et al. 2011

Nuclear Medicine and Biology

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“…After introduction of 99m Tc-methylene diphosphonate (MDP, Figure 1(c)) by Subramanian et al [11] in 1975 and 99m Tc-hydroxymethylene diphosphonate (HMDP, Figure 1(d)) by Bevan et al [12] in 1980, 99m Tc-MDP, and 99m Tc-HMDP, which showed superior biodistribution compared to 99m Tc-HEDP, have been used as radiopharmaceuticals for bone scintigraphy for over thirty years [13–15]. 99m Tc-MDP is postulated to form a bidentate-bidentate bridge with hydroxyapatite while the presence of the hydroxyl group in 99m Tc-HMDP would convert the ligand to form a bidentate-tridentate bridge and is expected to enhance the hydroxyapatite affinity of the 99m Tc complex [12, 16].…”

Section: 99mtc-bisphosphonate Complexesmentioning

confidence: 99%

Advances in Drug Design of Radiometal-Based Imaging Agents for Bone Disorders

Ogawa

Saji

2011

International Journal of Molecular Imaging

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Nuclear medicine bone imaging has been the optimum diagnosis for the detection of bone disorders because the lesion could be detectable before the appearance of symptomatic and radiographic changes. Over the past three decades, 99mTc-MDP and 99mTc-HMDP have been used as bone scintigraphic agents because of their superior biodistribution characteristics, although they are far from optimal from a chemical and pharmaceutical point of view. Recently, a more logical drug design has been proposed as a concept of bifunctional radiopharmaceuticals in which the carrier molecules (bisphosphonates) and radiometal chelating groups are separated within a molecule, specifically, 99mTc-mononuclear complex-conjugated bisphosphonate. Some of the 99mTc-mononuclear complex-conjugated bisphosphonate compounds showed superior biodistribution in preclinical studies. Moreover, the drug design concept could be applied to 68Ga PET bone imaging agents. These studies would provide useful information for the development of radiometal-based imaging and therapeutic agents for bone disorders such as bone metastases.

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“…A variety of 99m Tc-based radiopharmaceuticals have been developed and approved by the Federal Drug Administration (FDA) for determining organ function or assessing disease status by imaging methods [5][6][7]. Bone imaging agents are among the first developed 99m Tc-based radiopharmaceuticals and among the most widely used radiopharmaceuticals in the diagnostic nuclear medicine [7], which involve the coordination of 99m Tc to diphosphonates such as methylenediphosphonate (MDP) [8] and hydroxymethylenediphosphonate (HMDP) [9]. They have been widely used as radiopharmaceuticals for bone scintigraphy in cases of metastatic bone disease, Paget's disease, osteoporosis, etc.…”

Section: Introductionmentioning

confidence: 99%

“…They have been widely used as radiopharmaceuticals for bone scintigraphy in cases of metastatic bone disease, Paget's disease, osteoporosis, etc. [8][9][10][11][12]. With these 99m Tc-labeled diphosphonates (DPs), however, an interval of 2-6 h is needed *Author for correspondence (E-mail: jglin@yahoo.cn).…”

Section: Introductionmentioning

confidence: 99%

A novel ^99mTc-labeled dimethyl-substituted zoledronic acid (DMIDP) with improved bone imaging efficiency

Qiu¹,

Lin²,

Luo³

et al. 2012

Radiochimica Acta

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99m Tc-DMIDP / Bone imaging / Biodistribution / Blood clearance Summary. A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2,4-dimethyl-1H-imidazol-1-yl)-ethane-1,1-diyldiphosphonic acid (DMIDP, dimezoledronate), was successfully prepared and labeled with 99m Tc in a high labeling yield. The biodistribution in mice shows that 99m Tc-DMIDP has significant advantage regarding bone resorption and clearance from soft tissues compared with 99m Tc-ZL and the clinically widelyused bone-imaging agent 99m Tc-MDP (methylenediphosphonic acid). Kinetics of blood clearance displayed that distribution half-life (T 1/2α ) and elimination half-life (T 1/2β ) of 99m Tc-DMIDP were 2.53 min and 23.53 min, while those of 99m Tc-ZL were 2.28 and 52.63 min, respectively. Excellent images of the rabbit skeleton can be quickly obtained from 99m Tc-DMIDP, which was faster than 99m Tc-ZL and 99m Tc-MDP. The present findings indicate that 99m Tc-DMIDP possesses excellent potential for application as a novel bone scanning agent.

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99mTc-hydroxymethane diphosphonate: a new bone imaging agent with a low tin content.

Cited by 33 publications

References 0 publications

Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Advances in Drug Design of Radiometal-Based Imaging Agents for Bone Disorders

A novel ^99mTc-labeled dimethyl-substituted zoledronic acid (DMIDP) with improved bone imaging efficiency

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99mTc-hydroxymethane diphosphonate: a new bone imaging agent with a low tin content.

Cited by 33 publications

References 0 publications

Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Advances in Drug Design of Radiometal-Based Imaging Agents for Bone Disorders

A novel 99mTc-labeled dimethyl-substituted zoledronic acid (DMIDP) with improved bone imaging efficiency

Contact Info

Product

Resources

About

A novel ^99mTc-labeled dimethyl-substituted zoledronic acid (DMIDP) with improved bone imaging efficiency