Enzyme-activated cytostatic conjugates with integrin ligands

摘要

The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to alpha v beta 3 integrin antagonists via preferred linking units which can be selevtively cleaved by elastase, i.e. by an enzyme which can especially be found in tumor tissue. The preferred linking units provide sufficient stability of the conjugateof cytostatic and alpha v beta 3 integrin antagonist in biological fluids and, at the same time, the desired intracellular action within tumour cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.