TY - JOUR
T1 - Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development
AU - Oronsky, Bryan
AU - Guo, Xiaoning
AU - Wang, Xiaohui
AU - Cabrales, Pedro
AU - Sher, David
AU - Cannizzo, Lou
AU - Wardle, Bob
AU - Abrouk, Nacer
AU - Lybeck, Michelle
AU - Caroen, Scott
AU - Oronsky, Arnold
AU - Reid, Tony R.
N1 - Publisher Copyright:
© 2021 The Authors. Published by American Chemical Society.
PY - 2021/6/10
Y1 - 2021/6/10
N2 - 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.
AB - 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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U2 - 10.1021/acs.jmedchem.1c00599
DO - 10.1021/acs.jmedchem.1c00599
M3 - Article
C2 - 34043360
AN - SCOPUS:85108020327
SN - 0022-2623
VL - 64
SP - 7261
EP - 7271
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 11
ER -