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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use
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Azetidines / chemistry*
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Azetidines / pharmacology
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Azetidines / therapeutic use
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CD47 Antigen / genetics
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CD47 Antigen / metabolism*
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Down-Regulation / drug effects
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Half-Life
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Humans
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Immunogenic Cell Death / drug effects
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Male
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Mice
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Mice, Inbred C3H
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Neoplasms / diagnostic imaging
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Neoplasms / drug therapy
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Nitro Compounds / chemistry*
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Nitro Compounds / pharmacology
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Nitro Compounds / therapeutic use
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Positron-Emission Tomography
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Proto-Oncogene Proteins c-myc / genetics
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Proto-Oncogene Proteins c-myc / metabolism*
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Structure-Activity Relationship
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Transplantation, Heterologous
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Tumor-Associated Macrophages / cytology
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Tumor-Associated Macrophages / drug effects
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Tumor-Associated Macrophages / metabolism
Substances
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Antineoplastic Agents
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Azetidines
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CD47 Antigen
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CD47 protein, human
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Nitro Compounds
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Proto-Oncogene Proteins c-myc
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RRx-001