Liposomal formulation of bortezomib (ps-341)

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 47/10 (2006.01) A61K 47/26 (2006.01)

Patent

CA 2586348

A liposome composition comprised of liposomes having the peptide boronic acid proteasome inhibitor compound bortezomib entrapped in the liposomes is described. The boronic acid compound is entrapped in the liposomes in the form of a boronate ester, subsequent to interaction with a liposome-entrapped polyol. In one embodiment, the liposomes have an outer coating of hydrophilic polymer chains and are used to treat a solid tumor in a subject.

La présente invention concerne une composition de liposome constituée de liposomes possédant un bortezomib composé inhibiteur de protéase acide borique peptidique piégé dans les liposomes. Ce composé acide borique est piégé dans les liposomes sous la forme d'un ester de borate, suite à l'interaction avec un polyol piégé par liposome. Dans un mode de réalisation de l'invention, les liposomes possèdent un revêtement extérieur de chaînes polymères hydrophiles et sont utilisés pour traiter une tumeur solide chez un sujet.

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