Use of lamellarin-class alkaloids in methods of treatment

Details Use of lamellarin-class alkaloids in methods of treatment Use of lamellarin-class alkaloids in methods of treatment

A - Human Necessities

61

K

A61K 31/475 (2006.01) A61K 31/437 (2006.01) A61K 31/4745 (2006.01) A61K 31/70 (2006.01) A61K 38/08 (2006.01)

Patent

CA 2225807

The lamellarin compounds disclosed herein have been found to be inhibitors of MDR, i.e., acquired multidrug resistance, which has become a major problem in the treatment of various cancers. The lamellarin compounds disclosed herein have also been found to be cytotoxic to MDR cells. MDR is believed to be associated with certain alterations in tumor cells, including an over-expression of a certain high molecular weight membrane glycoprotein and a decrease in the ability of the tumor cell to accumulate and retain chemotherapeutic agents. The present invention is thus directed to methods of treating MDR-type tumors with an effective anti-MDR amount (either inhibitory or cytotoxic) of one or more lamellarin compounds, which compounds have been found to be effective antitumoral agents against MDR cells.

Les composés de lamellarine de la présente invention sont des inhibiteurs de la MDR, c'est-à-dire de la résistance multiple aux anticancéreux, laquelle résistance constitue désormais un problème important pour le traitement de divers cancers. Ces composés de lamellarine sont également des cytotoxiques des cellules MDR. On suppose que la MDR est à relier à certaines modifications internes des cellules tumorales, telles qu'une expression excessive d'un certaine glycoprotéine membranaire de haut poids moléculaire et telles qu'une diminution de l'aptitude de la cellule tumorale à l'accumulation et la rétention des agents chimiothérapiques. L'invention concerne ainsi des traitements des tumeurs de type MDR à base d'une quantité suffisante d'anti-MDR (inhibiteur ou cytotoxique) obtenu à partir d'un ou plusieurs composés de lamellarine, lesquels composés constituent des agents antitumoraux efficaces contre les cellules MDR.

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