Liposomal encapsulation of chelated actinium-225 and uses...

A - Human Necessities – 61 – K

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A61K 51/00 (2006.01) A61K 9/127 (2006.01) A61K 51/12 (2006.01)

Patent

CA 2411826

Actinium-225 and other alpha particle-emitting radionuclides hold great promise as potential therapeutic agents for cancer treatment. However, use of these radionuclides is limited by systemic toxicity resulting from release of administered radionuclides and radioactive decay products thereof. If the radionuclides are confined to the target cells, efficacy is increased and toxicity is decreased. However, covalent linking of the radionuclides to targeting molecules does not prevent toxicity resulting from the systemic release of alpha-particle emitting daughter radionuclides. The present invention provides targeted delivery of alpha particle-emitting radionuclides and their alpha-emitting progeny using liposomal encapsulating to prevent the loss of progeny radionuclides from the targeting vehicle and, therefore, the tumor site.

L'actinium-225 et d'autres radionucléides à émission de particules alpha sont très prometteurs en tant qu'agents thérapeutiques potentiels dans le traitement du cancer. L'utilisation de ces radionucléides est toutefois limitée par la toxicité systémique causée par la libération de radionucléides administrés et les produits radioactifs de filiation de ces derniers. Si les radionucléides sont confinés aux cellules cibles, l'efficacité s'en trouve augmentée et la toxicité diminuée. La liaison covalente des radionucléides à des molécules de ciblage n'empêche cependant pas la toxicité causée par la libération systémique de radionucléides filles à émission de particules alpha. La présente invention concerne l'administration ciblée de radionucléides à émission de particules alpha et leur descendance à émission de particules alpha, au moyen de l'encapsulation liposomale permettant d'empêcher la perte de radionucléides de descendance du véhicule de ciblage et, à cet effet, du site tumoral.

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