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68 Ga-Labeled (4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetic acid (BPAMD)

68 Ga-Labeled (4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetic acid (BPAMD)

Arvind Chopra

PMID: 23193622

Abstract:

Bisphosphonates (BPs; also known as diphosphonates), such as methylene diphosphonate (MDP) and zoledronic acid, can be labeled with technetium-99m ([99mTc]-BPs) for bone scintigraphy (gamma planar imaging or single-photon emission computed tomography (SPECT)) to detect osteoporosis and other skeletal-related events (SREs), including bone metastases (1). These chemicals are known to promote osteoclast apoptosis and have a strong affinity for hydroxyapatite, a component of the bone matrix. The exact mechanism of action of these bone-seeking compounds is described in detail elsewhere (2-4). Although the 99mTc-labeled compounds have high sensitivity, selectivity, and accuracy for the detection of SREs, they are known to generate some false positive and false negative results in the clinic (5). [18F]-Fluoride is another nuclide that is commonly used for bone imaging with positron emission tomography (PET) and is believed to be superior to [99mTc]-BPs for the diagnosis of SREs (6). However, the main limitations of using 18F are the requirement of a cyclotron to produce it and the high costs that are associated with the production of this radionuclide (5). In an effort to develop an imaging compound that does not have the limitations of tracers that are currently used to detect SREs with scintigraphy or PET, a bisphosphonate labeled with 68Ga was developed and shown to be potentially useful for imaging the mouse skeletal system with PET (5).
The main advantage of using 68Ga (half-life = 68 min; β+ = 89%; E+βmax = 1.9 MeV) for bone imaging over either 99mTc (half-life = 6 h; γ+ = 100%; E+γmax = 140 keV) or 18F (half-life = ~110 min; β+ = 97%; E+βmax = 0.635 MeV) as a radiolabel is that 68Ga can be produced economically on-site with a 68Ge/68Ga generator (5, 7). In addition, images obtained with PET have a higher spatial resolution compared with those obtained with SPECT (7). In an ongoing effort to develop a compound that could be used for the targeted imaging of bone metastases, a novel 1,4,7,10-tetraazacyclododecane-N,N',N,N'-tetraacetic acid (DOTA) derivative that contained a bisphosphonate within its structure ((4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetic acid (BPAMD)) was developed (8, 9), labeled with 68Ga ([68Ga]BPAMD), and shown to be suitable for the imaging of bone metastases in mice (7) and humans (10).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP22884102	Zoledronic acid Related Compound A		22884-10-2	Price

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