A radiolabelled ligand for selectively introducing an auger...

A - Human Necessities – 61 – K

Patent

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A61K 51/08 (2006.01)

Patent

CA 2273946

The invention is a radiolabelled ligand for introducing an Auger electron emitting radionuclide into the nucleus of a cancer cell. The ligand binds selectively to a cell surface receptor that is unique to a cancer cell or which is overexpressed on a cancer cell. An Auger electron emitting radionuclide is bonded to the ligand either directly or by means of a chelator. The radiolabelled ligand is internalized by the cell upon binding to the receptor, and a sufficient portion of the ligands so internalized are transported to the nucleus to provide a lethal dose of radiation to it.

Cette invention se rapporte à un ligand radiomarqué qui permet d'introduire un radionucléide émetteur d'électrons Auger dans le noyau d'une cellule cancéreuse. Ce ligand se lie spécifiquement à un récepteur de surface cellulaire qui est unique à une cellule cancéreuse ou qui est surexprimé sur une cellule cancéreuse. Un radionucléide émetteur d'électrons Auger se lie au ligand soit directement soit par l'intermédiaire d'un chélateur. Le ligand radiomarqué est internalisé par la cellule lors de la liaison au récepteur, et une partie suffisante des ligands ainsi internalisés est transportée jusqu'au noyau, afin d'appliquer sur celui-ci une dose de rayonnement l'étale.

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