INOR 298 |
| Michael F. Tweedle, Bracco Research USA Inc, Bracco Research USA Inc, Bracco Group, 305 College Rd. East, Princeton, NJ 08540 |
| Contrast agents with biochemical targets have thus far been largely restricted to the field of nuclear medicine by the sensitivity requirements for imaging scarce receptors. MRI has definable, if evolving limits on the sensitivity with which it can detect its contrast agents. Biochemical imaging agents are natural partners with targeted therapeutics. 177Lu-Amba (177Lu-DOTA-Gly-4-aminobenzoyl-Glu-Trp-Ala-Val-Gly-His-Leu-Met-NH2) contains a tetraazadodecane macrocyclic chelating agent similar to one used clinically with Gd(III) as an MRI contrast agent. The DOTA chelating agent is linked to a nonapeptide derived from Bombesin (BBN7-14) that is an agonist of GRP-r (gastrin releasing peptide receptor). GRP-r is overexpressed in a variety of cancers including prostate, breast, small cell lung cancer and glioblastoma. While Gd(III), 111In(III) and 177Lu(III) could use the DOTA chelate, 177Lu contains an imageable gamma as well as the cell-killing beta emission. Preclinical results with 177Lu-Amba will be presented along with the rationale for choosing a particular imaging modality to match the biochemical target. |
|
The Chemistry of Biological Molecular Imaging
8:30 AM-12:00 PM, Monday, August 23, 2004 Pennsylvania Convention Center -- 108B, Oral
Division of Inorganic Chemistry |