RRx-001

RRx-001 is an anticancer agent.¹ It inhibits growth in a panel of 12 cancer cell lines (IC₅₀s =1.8-6 μM), an effect that is enhanced in SCC VII cells under hypoxic conditions. RRx-001 increases intracellular levels of reactive oxygen species (ROS) in HT-29 and SCC VII cells in a concentration- and time-dependent manner and induces apoptosis in SCC VII, HL-60, and Daudi cells when used at concentrations of 5, 5, and 4 μM, respectively. RRx-001 (5 mg/kg per day for five days) reduces tumor growth and enhances radiation-induced tumor growth reduction in an SCC VII murine squamous cell carcinoma model. Pre-incubation of red blood cells and hemolysate with RRx-001 (3 mM) increases nitrite-induced nitric oxide (NO) release under hypoxic conditions.² RRx-001 (10 mg/kg) also decreases parasitemia and increases survival in a mouse model of P. berghei ANKA infection.³

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1. Ning, S., Bednarski, M., Oronsky, B., et al. Dinitroazetidines are a novel class of anticancer agents and hypoxia-activated radiation sensitizers developed from highly energetic materials. Cancer Res. 72(10), 2600-2608 (2012).

2. Fens, M.H., Cabrales, P., Scicinski, J., et al. Targeting tumor hypoxia with the epigenetic anticancer agent, RRx-001: A superagonist of nitric oxide generation. Med. Oncol. 33(8), 85 (2016).

3. Yalcin, O., Oronsky, B., Carvalho, L.J.M., et al. From METS to malaria: RRx-001, a multi-faceted anticancer agent with activity in cerebral malaria. Malar. J. 14, 218 (2015).