CPI-0004Na, a new doxorubicin prodrug, reduces growth of 3LL-H61 carcinoma lung metastases in C57BI/6 mice.

The ETAP concept (Extracellularly Tumor-Activated Prodrug) is a new approach developed to overcome the lack of selectivity and the side effects responsible for the limited efficacy of chemotherapeutic agents. CPI-0004Na, a doxorubicin (Dox) prototype prodrug of this type, is less toxic than free Dox and showed increased efficacy against subcutaneous human tumor xenografts. The aim of this study was to assess the efficacy of the prodrug vs Dox (given ip) at their maximal tolerated dose (MTD) for this administration schedule (129.

CPI-0004Na, a new extracellularly tumor-activated prodrug of doxorubicin: in vivo toxicity, activity, and tissue distribution confirm tumor cell selectivity.

The search for cancer therapies that are more selective for tumor cells and spare normal sensitive cells has been very active for at least 20 years. The extracellularly tumor-activated peptidic prodrug of doxorubicin (Dox) CPI-0004Na (N-succinyl-beta-alanyl-L-leucyl-L-alanyl-L-leucyl-Dox) is potentially such a treatment. Here, we report the results of lethality studies performed with this compound in the mouse, showing that it is up to 4.