Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy

摘要

The invention relates to novel, water-soluble paclitaxel prodrugs wherein paclitaxel is, through its 2'-hydroxyl functionality, connected to a cleavable spacer group, which is in turn attached to a preferably enzymatically cleavable sugar group. Such prodrugs are relatively non-toxic and can be used in cancer treatment. They can be selectively activated at the tumor site by the action of endogeneous enzymes or targeted enzymes, or via a non-enzymatic process. The enzyme is preferably beta -glucuronidase, beta -glucosidase or beta -galactosidase. The invention also relates to a process for preparing a pharmaceutical composition containing a paclitaxel prodrug as defined herein, which comprises said prodrug with a pharmaceutically acceptable carrier to provide a solid or liquid formulation for administration.