Summary
Chronic myelogenous leukemia (CML) is almost universally associated with a translocation that juxtaposes the Bcr and Abl genes. Because the resulting kinase, p210 Brc/Abl , is found exclusively in malignant hematopoietic cells there has been considerable interest in identifying inhibitors of this enzyme. Adaphostin induces cytotoxicity in human leukemia cells by down-regulating p210 Bcr/Abl , inducing DNA damage and initiating apoptosis. Adaphostin exhibits selectivity for CML myeloid progenitors in vitro and retained its catholicity when cytotoxicity mesylate-resistant K562 cells were examined. Adaphostin may kill a wide range of human leukemia cells and may be effective against other cancer types. The present invention provides pharmaceutical compositions comprising effective amounts of adaphostin.
The compound and composition of the present invention may be used for treating human leukemia and other proliferative diseases.