Water soluble paclitaxel prodrugs

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01) A61F 2/04 (2006.01) A61F 2/06 (2006.01) A61K 31/335 (2006.01) A61K 31/337 (2006.01) A61K 49/00 (2006.01) A61K 51/04 (2006.01) A61L 31/10 (2006.01) A61L 31/16 (2006.01) A61M 5/00 (2006.01) A61M 31/00 (2006.01)

Patent

CA 2250295

Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble chelator, polyethylene glycol or polymer such as poly (1-glutamic acid) or poly (1-aspartic acid). Also disclosed are methods of using the compositions for treatment of tumors, autoimmune disorders such as rheumatoid arthritis and for prediction of paclitaxel uptake by tumors and radiolabeled DTPA-paclitaxel tumor imaging. Other embodiments include the coating of implantable stents for prevention of restenosis.

Compositions hydrosolubles de paclitaxel et de docetaxel formés par la conjugaison de paclitaxel avec un chélateur hydrosoluble, un polyéthylène glycol ou un polymère tel que poly(acide L-glutamique) ou poly(acide L-aspartique). Sont également décrites des méthodes d'utilisation de ces compositions pour le traitement des tumeurs, de maladies auto-immunes telles que l'arthrite rhumatoïde et pour l'estimation de la fixation de paclitaxel par les tumeurs et l'imagerie des tumeurs par DTPA-paclitaxel radiomarqués. Parmi d'autres utilisations figure l'enrobage d'extenseurs implantables pour la prévention de la resténose.

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