MNPR-201 (GPX-150; 5-imino-13-deoxydoxorubicin) is a proprietary doxorubicin analog that is selective for topoisomerase-IIα. Doxorubicin is used to treat adult and pediatric solid and blood (hematologic) cancers including breast, gastric, ovarian and bladder cancer, soft tissue sarcomas, leukemias and lymphomas. A number of clinical studies have demonstrated the anti-cancer benefit of higher doses of doxorubicin administered for longer periods of time. The optimal clinical efficacy of doxorubicin, however, has been limited historically by the risk of patients developing irreversible, potentially life-threatening cardiotoxicity. MNPR-201 has been engineered specifically to retain the anticancer activity of doxorubicin while minimizing the toxic effects on the heart. Monopar believes the results of these studies, along with the potential to combine a less or non-cardiotoxic analog of doxorubicin with other anticancer agents, emphasizes that there is a large market opportunity for MNPR-201 in a broad spectrum of cancer types.
The antitumor effects of MNPR-201 are mediated through the stabilization of the topoisomerase II complex after a DNA strand break and DNA intercalation leading to apoptosis (cell death) through a mechanism similar to doxorubicin and other anthracycline drugs. Inhibiting the topoisomerase IIα isoform is desired for the anti-cancer effect, while inhibiting the topoisomerase IIβ isoform has been demonstrated to mediate, at least in part, the cardiotoxicity associated with all anthracycline drugs currently used in the clinic. MNPR-201 is substantially more selective than doxorubicin for inhibiting topoisomerase IIα versus topoisomerase IIβ. This selectivity may at least partly explain the minimal cardiotoxicity that MNPR-201 has demonstrated in clinical studies to date.
Learn more about the clinical studies that support the safety and efficacy of MNPR-201.