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Well-designed bone-seeking radiolabeled compounds for diagnosis and therapy of bone metastases.

Ogawa K, Ishizaki A - Biomed Res Int (2015)

Bottom Line: Furthermore, their effectiveness in the palliation of metastatic bone cancer pain has been demonstrated in the clinical setting.With the aim of developing superior bone-seeking radiopharmaceuticals, many compounds have been designed, prepared, and evaluated.Here, several well-designed bone-seeking compounds used for diagnostic and therapeutic use, having the concept of radiometal complexes conjugated to carrier molecules to bone, are reviewed.

View Article: PubMed Central - PubMed

Affiliation: Division of Pharmaceutical Sciences, Graduate School of Medical Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.

ABSTRACT
Bone-seeking radiopharmaceuticals are frequently used as diagnostic agents in nuclear medicine, because they can detect bone disorders before anatomical changes occur. Furthermore, their effectiveness in the palliation of metastatic bone cancer pain has been demonstrated in the clinical setting. With the aim of developing superior bone-seeking radiopharmaceuticals, many compounds have been designed, prepared, and evaluated. Here, several well-designed bone-seeking compounds used for diagnostic and therapeutic use, having the concept of radiometal complexes conjugated to carrier molecules to bone, are reviewed.

No MeSH data available.


Related in: MedlinePlus

68Ga-BPAMD was injected intravenously into a patient with extensive bone metastases of prostate cancer. 68Ga-BPAMD [maximum intensity projection (MIP) 50 min after injection (p.i.), 462 MBq] revealed intense accumulation in multiple osteoblastic lesions in the central skeleton, ribs, and proximal extremities: (a) = coronal PET, (b) = sagittal PET/CT. For comparison, (c) shows 18F-fluoride PET (sagittal, MIP 90 min p.i., 270 MBq). With kind permission from Springer Science+Business Media: Eur J Nucl Med Mol Imaging, PET/CT imaging of osteoblastic bone metastases with 68Ga-bisphosphonates: first human study, 37, 2010, 834, Fellner et al.
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fig5: 68Ga-BPAMD was injected intravenously into a patient with extensive bone metastases of prostate cancer. 68Ga-BPAMD [maximum intensity projection (MIP) 50 min after injection (p.i.), 462 MBq] revealed intense accumulation in multiple osteoblastic lesions in the central skeleton, ribs, and proximal extremities: (a) = coronal PET, (b) = sagittal PET/CT. For comparison, (c) shows 18F-fluoride PET (sagittal, MIP 90 min p.i., 270 MBq). With kind permission from Springer Science+Business Media: Eur J Nucl Med Mol Imaging, PET/CT imaging of osteoblastic bone metastases with 68Ga-bisphosphonates: first human study, 37, 2010, 834, Fellner et al.

Mentions: In 2010, Fellner et al. reported a human study of 68Ga-DOTA-conjugated bisphosphonate (68Ga-BPAMD, Figure 4(a)), containing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) as a ligand for gallium [31]. 68Ga-BPAMD showed high uptake in osteoblastic metastases lesions in a patient with prostate cancer (Figure 5). The maximal standardized uptake value (SUVmax⁡) was 77.1 and 62.1 in the 10th thoracic and L2 vertebra for 68Ga-BPAMD compared with respective values of 39.1 and 39.2 for 18F-fluoride, which is a typical bone imaging agent for PET (Table 2), respectively. In 2012, Fellner et al. reported the findings of basic experiments on 68Ga-BPAMD using μ-PET with bone metastasis rat model [32]. 68Ga-BPAMD highly accumulated in metastatic bone lesions compared with healthy bone in the same animal (contrast factor = 3.97 ± 1.82). The same research group further reported 68Ga-DOTA-conjugated bisphosphonate derivatives, 68Ga-BPAPD and 68Ga-BPPED (Figures 4(b) and 4(c)) in 2013 [33]. The phosphinate-conjugated bisphosphonate 68Ga-BPPED showed higher accumulation in bone compared with 68Ga-BPAMD and 68Ga-BPAPD, amide-conjugated bisphosphonates. The presence of phosphinate may contribute to an additional binding to HA, leading to higher accumulation in bone.


Well-designed bone-seeking radiolabeled compounds for diagnosis and therapy of bone metastases.

Ogawa K, Ishizaki A - Biomed Res Int (2015)

68Ga-BPAMD was injected intravenously into a patient with extensive bone metastases of prostate cancer. 68Ga-BPAMD [maximum intensity projection (MIP) 50 min after injection (p.i.), 462 MBq] revealed intense accumulation in multiple osteoblastic lesions in the central skeleton, ribs, and proximal extremities: (a) = coronal PET, (b) = sagittal PET/CT. For comparison, (c) shows 18F-fluoride PET (sagittal, MIP 90 min p.i., 270 MBq). With kind permission from Springer Science+Business Media: Eur J Nucl Med Mol Imaging, PET/CT imaging of osteoblastic bone metastases with 68Ga-bisphosphonates: first human study, 37, 2010, 834, Fellner et al.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4446473&req=5

fig5: 68Ga-BPAMD was injected intravenously into a patient with extensive bone metastases of prostate cancer. 68Ga-BPAMD [maximum intensity projection (MIP) 50 min after injection (p.i.), 462 MBq] revealed intense accumulation in multiple osteoblastic lesions in the central skeleton, ribs, and proximal extremities: (a) = coronal PET, (b) = sagittal PET/CT. For comparison, (c) shows 18F-fluoride PET (sagittal, MIP 90 min p.i., 270 MBq). With kind permission from Springer Science+Business Media: Eur J Nucl Med Mol Imaging, PET/CT imaging of osteoblastic bone metastases with 68Ga-bisphosphonates: first human study, 37, 2010, 834, Fellner et al.
Mentions: In 2010, Fellner et al. reported a human study of 68Ga-DOTA-conjugated bisphosphonate (68Ga-BPAMD, Figure 4(a)), containing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) as a ligand for gallium [31]. 68Ga-BPAMD showed high uptake in osteoblastic metastases lesions in a patient with prostate cancer (Figure 5). The maximal standardized uptake value (SUVmax⁡) was 77.1 and 62.1 in the 10th thoracic and L2 vertebra for 68Ga-BPAMD compared with respective values of 39.1 and 39.2 for 18F-fluoride, which is a typical bone imaging agent for PET (Table 2), respectively. In 2012, Fellner et al. reported the findings of basic experiments on 68Ga-BPAMD using μ-PET with bone metastasis rat model [32]. 68Ga-BPAMD highly accumulated in metastatic bone lesions compared with healthy bone in the same animal (contrast factor = 3.97 ± 1.82). The same research group further reported 68Ga-DOTA-conjugated bisphosphonate derivatives, 68Ga-BPAPD and 68Ga-BPPED (Figures 4(b) and 4(c)) in 2013 [33]. The phosphinate-conjugated bisphosphonate 68Ga-BPPED showed higher accumulation in bone compared with 68Ga-BPAMD and 68Ga-BPAPD, amide-conjugated bisphosphonates. The presence of phosphinate may contribute to an additional binding to HA, leading to higher accumulation in bone.

Bottom Line: Furthermore, their effectiveness in the palliation of metastatic bone cancer pain has been demonstrated in the clinical setting.With the aim of developing superior bone-seeking radiopharmaceuticals, many compounds have been designed, prepared, and evaluated.Here, several well-designed bone-seeking compounds used for diagnostic and therapeutic use, having the concept of radiometal complexes conjugated to carrier molecules to bone, are reviewed.

View Article: PubMed Central - PubMed

Affiliation: Division of Pharmaceutical Sciences, Graduate School of Medical Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.

ABSTRACT
Bone-seeking radiopharmaceuticals are frequently used as diagnostic agents in nuclear medicine, because they can detect bone disorders before anatomical changes occur. Furthermore, their effectiveness in the palliation of metastatic bone cancer pain has been demonstrated in the clinical setting. With the aim of developing superior bone-seeking radiopharmaceuticals, many compounds have been designed, prepared, and evaluated. Here, several well-designed bone-seeking compounds used for diagnostic and therapeutic use, having the concept of radiometal complexes conjugated to carrier molecules to bone, are reviewed.

No MeSH data available.


Related in: MedlinePlus