A High Relaxivity Magnetic Resonance Imaging Contrast Agent Targeted to Serum Albumin

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Contents Vol 61(9)

doi:10.1071/CH08164

A High Relaxivity Magnetic Resonance Imaging Contrast Agent Targeted to Serum Albumin

Stéphane Dumas ^A, Jeffrey S. Troughton ^A, Normand J. Cloutier ^A, Jaclyn M. Chasse ^A, Thomas J. McMurry ^A, Peter Caravan ^B ^C

^A EPIX Pharmaceuticals Inc., 4 Maguire Road, Lexington, MA 02421, USA.
^B Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, 149 Thirteenth Street, Suite 2301, Charlestown, MA 02129, USA.
^C Corresponding author. Email: caravan@nmr.mgh.harvard.edu





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Australian Journal of Chemistry 61(9) 682–686 http://dx.doi.org/10.1071/CH08164
Submitted: 18 April 2008 Accepted: 5 June 2008 Published online: 5 September 2008

Abstract

EP-647 is a serum albumin-targeted magnetic resonance imaging contrast agent comprising a GdDTPA (DTPA, diethylenetriaminepentaacetate) chelate for magnetic resonance signal generation linked via a phosphodiester to a substituted biphenyl for albumin targeting. Albumin binding and relaxivity are higher than the benchmark magnetic resonance angiographic agent MS-325. EP-647 binds primarily to a unique site on serum albumin that is different from the MS-325 site and the binding sites of other drugs.