Abstract: The present invention is described as a lipid-complexed topoisomerase I inhibitor (TII), for example camptothecin (CPT) preparation that allows for intravenous administration in vivo in clinically relevant lipid:drug ratios. The lipid formulation has in vitro antitumor activity similar to that of the base compound and displays similar cytotoxicity against both MDR-1 negative and positive tumor cells.
Type:
Grant
Filed:
May 3, 1995
Date of Patent:
November 10, 1998
Assignees:
Roman Perez-Soler, Steven M. Sugarman, Kenneth R. Poirot
Inventors:
Roman Perez-Soler, Steven M. Sugarman, Kenneth R. Poirot
Abstract: The present disclosure details novel modified anthracyclines, the synthesis thereof, and their use in treating patients with tumors. Preferred aspects of the disclosure involve modified anthracyclines which have an O-substituted aromatic ring on their sugar moiety. Other preferred aspects of the disclosure involve synthesis steps wherein a hydroxyl group on a sugar moiety to be added is blocked with a halo-substituted alkyl group during the process of adding it to an anthracycline ring compound.
Type:
Grant
Filed:
February 27, 1995
Date of Patent:
April 29, 1997
Assignees:
Waldemar Priebe, Piotr Skibicki, Roman Perez-Soler
Inventors:
Waldemar Priebe, Piotr Skibicki, Roman Perez-Soler