2. Academic Validation
  3. Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development

Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development

  • J Med Chem. 2021 Jun 10;64(11):7261-7271. doi: 10.1021/acs.jmedchem.1c00599.
Bryan Oronsky 1,  XiaoNing Guo 2,  XiaoHui Wang 2,  Pedro Cabrales 3,  David Sher 4,  Lou Cannizzo 5,  Bob Wardle 5,  Nacer Abrouk 1,  Michelle Lybeck 1,  Scott Caroen 1,  Arnold Oronsky 6,  Tony R Reid 1
Affiliations

Affiliations

  • 1 EpicentRx Inc., 11099 North Torrey Pines Road, Suite 160, La Jolla, California 92037, United States.
  • 2 SciClone Pharmaceuticals Co., Ltd., 22 Floor, Shanghai Central Plaza, No. 381 Middle Huaihai Road, Huangpu, Shanghai 200020, China.
  • 3 Department of Bioengineering, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States.
  • 4 Department of Radiation Oncology, UT Southwestern Medical Center, 2280 Inwood Road, Dallas, Texas 75390, United States.
  • 5 Department of Space Systems, Northrop Grumman Corporation, 2980 Fairview Park Drive, Falls Church, Virginia 22042, United States.
  • 6 InterWest Partners, 467 First Street, Suite 201, Los Altos, California 94022, United States.
PMID: 34043360 DOI: 10.1021/acs.jmedchem.1c00599
Abstract

After extensive screening of aerospace compounds in an effort to source a novel Anticancer agent, RRx-001, a first-in-class dinitroazetidine small molecule, was selected for advancement into preclinical and clinical development. RRx-001 is a minimally toxic small molecule with a distinct chemical structure and mechanism of action. The paradox of RRx-001 is that it mediates both antitumor cytotoxicity and normal tissue protection. The question of exactly how RRx-001 does this, and by means of what mechanism(s), depending on the route of delivery, intravenous or intratumoral, are explored. RRx-001 is currently in phase 2 and 3 clinical trials for the treatment of multiple solid tumor malignancies and as a supportive care drug.

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