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EPISENSITIZATION AND RRx-001

 

EpicentRx’s lead compound is called RRx-001, a structurally unique pharmacophore that inhibits multiple epi-enzymes and independently affects the apoptosis pathway and reactive oxygen and nitrogen species (RONS) production. RRx-001 is not cross-resistant with approved therapies and selectively targets and resensitizes hypoxic tumor cells to immunotherapy, chemotherapy and radiotherapy.

RRx-001 has successfully completed a Phase 1 “all comers” dose escalation study in 25 patients with advanced, refractory cancer in which safety and activity were demonstrated in all six cohorts tested and in a variety of tumor types. Results from the Phase I trial are available in Lancet Oncology, August 2015. To read the press release visit this link.

The success of the Phase 1 study was the springboard for further clinical development in multi-site biomarker-driven Phase 2 trials, as single agent and in combination with other anti-cancer drugs and with radiotherapy.

Preclinical data has demonstrated a synergistic combination of RRx-001 and radiotherapy that EpicentRx plans to explore fully in the clinical setting.

The ROS-mediated epigenetic mechanism of action elicited by RRx-001 lead to a suite of antitumor responses including immune upregulation, reinduction of p53, anti-energetic glycolytic inhibition, and G6PD inhibition ultimately culminating in ‘episensitization’ which experimentally enhances drug combinatorial effects and resensitizes chemoresistant and immunoresistant tumors to previously failed therapies.

Since RRx-001 increases the responsiveness of tumor cells to chemotherapy at least in part through reactions, which locally increase oxidative and nitrosative stress, it literally represents a radical approach to cancer treatment.

During 2014-2015 EpicentRx has launched Phase 2 trials in brain, colorectal, non-small cell lung, small cell lung and cholangiocarcinoma both alone and in combination.

 

 

If you would like to request further information about any of our technologies, please contact us at info@epicentrx.com or by telephone at (858) 812-2069.