RRx-001

RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity^[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α^[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity^[3]. In Vitro: RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies^[1].
RRx-001 blocks migration of MM cells and associated angiogenesis^[1].
RRx-001 induces significant G1 phase growth arrest, with a concomitant decrease in the S phase. RRx-001 triggers significant apoptosis in MM cells^[1].
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases^[1].
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages^[2].
In Vivo: RRx-001 (5 mg/kg or 10 mg/kg, I.V., thrice-weekly for 24 days) inhibits tumor growth and prolongs survival in a xenograft mouse model^[1].
RRx-001 (10 mg/kg, IP, twice a week and once a day) exhibits potent anti-cancer activity on the A549 lung cancer model dependent on the presence of tumor-associated macrophages (TAMs) in tumor tissue^[2].