Epigenetic alterations have been strongly associated with tumour formation and resistance to chemotherapeutic drugs, and epigenetic modifications are an attractive target in cancer research. RRx-001 is activated by hypoxia and induces the generation of reactive oxygen and nitrogen species that can epigenetically modulate DNA methylation, histone deacetylation, and lysine demethylation. The aim of this phase 1 study was to assess the safety, tolerability, and pharmacokinetics of RRx-001.
Reid T., Oronsky B., Scicinski J., Scribner C.L., Knox S.J. Ning S., Peehl D.M., Korn R.L., Stirn M., Carter C.A., Oronsky A., Taylor M.J., Fitch W.L., Cabrales P., Kim M.M., Burris H.A. 3rd, Lao C.D., Abrouk N.E., Fanger G.R. and Infante J.R. “Safety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 study.” Lancet Oncol., 16(9):1133-42. doi 10.1016/S1470-2045(15)00089-3. Epub, (2015).