MPC-2130
MPC-2130 is an investigational new cancer drug being developed by Myriad Pharmaceuticals for the treatment of advanced metastatic tumors or blood cancers as well as refractory cancers that have progressed despite previous chemotherapy.
About MPC-2130
MPC-2130 is a broad-acting inducer of apoptosis in cancer cells. MPC-2130 promotes programmed cell death in tumor cells at a later point in the apoptotic pathway. This leads us to believe that MPC-2130 may have additive or synergistic activity with other cancer compounds which work at earlier stages of the apoptotic pathway. In preclinical studies MPC-2130 demonstrated significant killing activity in ovarian cancer cells and prostate cancer cells as well as two lymphoma cell lines, Burkitt's lymphoma and T-cell lymphoma. MPC-2130 also caused a significant tumor size reduction in mice implanted with human ovarian and prostate cancers. Unlike most chemotherapeutic drugs, MPC-2130 did not cause neutropenia or gastrointestinal toxicity in animal studies. These results suggest that MPC-2130 will have a low side effect profile in humans. In addition, in vitro studies showed that MPC-2130 was not a substrate for MDR pumps and has significant brain penetration.
Back to top About Multiple Drug Resistance (MDR)
Importantly, MPC-2130 was highly active in cancer cell lines
that are resistant to multiple drugs. Cancer cells may become resistant to
chemotherapy through a cellular function that actively purges drug from the
cell. The function is carried out by MDR pumps and is the primary cause of
cancer' resistance to many marketed drugs such as paclitaxel and vinblastine. When MPC-2130 was tested to determine its susceptibility to MDR pumps, its anti-cancer activity in the MDR cell lines was similar to its activity in non-resistant cell lines. This indicated MPC-2130 is not a substrate for MDR pumps.
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Clinical Trial
MPC-2130 is currently being studied in a phase 1 clinical trial for the treatment of blood cancers.
MPC-2130 is listed on clinicaltrials.gov at:
http://www.clinicaltrials.gov/ct/show/NCT00387153
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Reference
- Antitumor Activity of MPC-2130 in Human Hematopoietic Cell Lines and Ovarian and Prostate Tumor Xenografts in Athymic Nude Mice. [Poster PDF]
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