Solid-Phase Conversion of Tc-99m Pertechnetate to a Reactive N-Hydroxysuccinimide Ester (BIDMC 947)

Category:    Medical Imaging

KeyWords:  Molecular Imaging;  Cancer;  Method;  

BIDMC ID:    947

Abstract:

Single-photon emission computed tomography (SPECT) imaging is used routinely in the care of patients with cancer and heart disease. However, the number of molecular-targeted SPECT contrast agents is few, mainly because of the difficulty of radioactive technetium (Tc-99m) chemistry. Traditional labeling approaches utilize large amounts of soluble carboxylic acid carrier, and require HPLC purification of intermediates. We have invented chemical methods for converting Tc-99m into a reactive N-hydroxysuccinimide (NHS) ester using solid-phase reagents. Our technology permits inexpensive and readily available pertechnetate to be converted at high specific activity into a MAG3 or MAS3 reactive intermediate. Since it is based on solid-phase chemistry and requires no extraneous carrier, the entire process can be automated. The Tc-99m-NHS molecule can be used to label virtually any small molecule, peptide, or protein to high specific activity, and is expected to greatly accelerate the development of SPECT contrast agents.

Inventor:   John Frangioni, MD, PhD Preeti Misra, PhD

Commercial Opportunity:

Commercial applications include the manufacturer of “boxes” to perform the conversion at the reactor-scale, “kits” to permit individual investigators to prepare contrast agents, and as a crucial step in the manufacture of clinical radioactive SPECT contrast agents.

Competitive Advantages:

Related Publications:

Misra et al. J Nucl Med 2007; 48:1379–1389

State of Development:

Related Technology URL:

Patent Status:

PCT Pending and Published as WO 2008/027995 A2

TVO Contact Info:
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