Page last updated: 2024-11-12

rrx-001

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

RRx-001: has antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15950826
CHEMBL ID3526802
SCHEMBL ID2249018
MeSH IDM0580411

Synonyms (33)

Synonym
S8405
rrx 001 [who-dd]
radiosensitizer rrx-001
abdnaz
n-(bromoacetyl)-3,3-dinitroazetidine
2-bromo-1-(3,3-dinitroazetidin-1-yl)ethan-1-one
rrx-001
unii-7rpw6su9sc
925206-65-1
2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone
7rpw6su9sc ,
ethanone, 2-bromo-1-(3,3-dinitro-1-azetidinyl)-
HY-16438
CS-5286
SCHEMBL2249018
AC-32908
CHEMBL3526802
rrx 001
1-bromoacetyl-3,3-dinitroazetidine
P15978
AS-53015
DB12060
rrx001
BCP19228
mfcd25976849
CCG-267126
EX-A2006
Q27268765
AKOS037644389
2-bromo-1-(3,3-dinitro-1-azetidinyl)ethanone
SY100127
BR164811
c5h6brn3o5

Research Excerpts

Toxicity

The primary objective was to assess safety, tolerability, and dose-limiting toxic effects of RRx-001. The goal was to determine single-dose pharmacokinetics, and to identify a recommended dose for phase 2 trials.

ExcerptReferenceRelevance
" The primary objective was to assess safety, tolerability, and dose-limiting toxic effects of RRx-001, to determine single-dose pharmacokinetics, and to identify a recommended dose for phase 2 trials."( Safety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 study.
Abrouk, NED; Burris, HA; Cabrales, P; Carter, CA; Fanger, GR; Fitch, WL; Infante, JR; Kim, MM; Knox, SJ; Korn, R; Lao, CD; Ning, S; Oronsky, A; Oronsky, B; Peehl, DM; Reid, T; Scicinski, J; Scribner, CL; Stirn, M; Taylor, MJ, 2015
)
0.95
" Pain at the injection site, mostly grade 1 and grade 2, was the most common adverse event related to treatment, experienced by 21 (84%) patients."( Safety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 study.
Abrouk, NED; Burris, HA; Cabrales, P; Carter, CA; Fanger, GR; Fitch, WL; Infante, JR; Kim, MM; Knox, SJ; Korn, R; Lao, CD; Ning, S; Oronsky, A; Oronsky, B; Peehl, DM; Reid, T; Scicinski, J; Scribner, CL; Stirn, M; Taylor, MJ, 2015
)
0.73
"RRx-001 is a well-tolerated novel compound without clinically significant toxic effects at the tested doses."( Safety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 study.
Abrouk, NED; Burris, HA; Cabrales, P; Carter, CA; Fanger, GR; Fitch, WL; Infante, JR; Kim, MM; Knox, SJ; Korn, R; Lao, CD; Ning, S; Oronsky, A; Oronsky, B; Peehl, DM; Reid, T; Scicinski, J; Scribner, CL; Stirn, M; Taylor, MJ, 2015
)
2.17
" RRx-001 is a minimally toxic small molecule with a distinct chemical structure and mechanism of action."( Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
Abrouk, N; Cabrales, P; Cannizzo, L; Caroen, S; Guo, X; Lybeck, M; Oronsky, A; Oronsky, B; Reid, TR; Sher, D; Wang, X; Wardle, B, 2021
)
1.9
" There were no severe adverse events attributed to the study drug."( PREVLAR: Phase 2a Randomized Trial to Assess the Safety and Efficacy of RRx-001 in the Attenuation of Oral Mucositis in Patients Receiving Head and Neck Chemoradiotherapy.
Abrouk, N; Bar-Ad, V; Biagioli, M; Blakaj, DM; Bonomi, M; Caroen, S; Colvett, K; Goyal, S; Kabarriti, R; Muzyka, B; Niermann, K; Oronsky, B; Reid, T; Sher, DJ; Sonis, S; Takiar, V, 2023
)
1.14

Dosage Studied

ExcerptRelevanceReference
" U87 tumors showed an absence of blood flow over large areas of treated tumors after dosing with RRx-001."( RRx-001, an epigenetic-based radio- and chemosensitizer, has vascular normalizing effects on SCCVII and U87 tumors.
Cabrales, P; Minchinton, A; Oronsky, B; Scicinski, J, 2016
)
2.09
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (80)

Assay IDTitleYearJournalArticle
AID1220447Binding affinity to monkey hemoglobin assessed as protein bound compound level at 20 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220450Drug metabolism assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-(hydroxyimino)azetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation after 1 hr in presence of excess reduced GSH at pH 7.8 by LC-MS/MS meth2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220395Drug metabolism in human whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220431Drug excretion in Wistar Hanover rat urine at 10 mg/kg, iv administered as single dose after 0 to 8 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220400Drug metabolism in rat whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-nitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220404Drug metabolism in rat whole blood assessed as [(R)-2-(2-amino-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)propanamido)acetic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814607Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220419Binding affinity to dog hemoglobin assessed as protein bound compound level at 20 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220435Drug level in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose after 168 hrs relative to total radioactivity2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220433Ratio of drug level in blood to plasma in Wistar Hanover rat at 10 mg/kg, iv administered as single dose after 0.083 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220392Retention time in rat whole blood in presence of 0.1% formic acid in water at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220390Retention time in human whole blood at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220401Drug metabolism in human whole blood assessed as [(R)-2-amino-3-((2-(3-nitroazetidin-1-yl)-2-oxoethyl)thio)propanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220448Binding affinity to human hemoglobin assessed as protein bound compound level at 20 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220430Drug excretion in Wistar Hanover rat urine at 10 mg/kg, iv administered as single dose after 168 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220449Retention time in rat whole blood at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220420Ratio of drug level in dog blood to dog plasma at 20 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814599Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220391Retention time in human whole blood in presence of 0.1% formic acid in water at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220437Drug level in Wistar Hanover rat stomach at 10 mg/kg, iv administered as single dose after 24 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220399Drug metabolism in human whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-nitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220425AUC (0 to t) in Wistar Hanover rat plasma at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220427Volume of distribution in Wistar Hanover rat plasma at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220406Drug metabolism in rat whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-1-oxo-3-((2-oxo-2-(3-oxoazetidin-1-yl)ethyl)thio)propan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220414Binding affinity to rat hemoglobin assessed as protein bound compound level at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220412Ratio of drug level in monkey blood to monkey plasma at 20 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1882259Cytotoxicity against human multiple myeloma cells by WST-1 assay2022European journal of medicinal chemistry, Feb-05, Volume: 229A review on the treatment of multiple myeloma with small molecular agents in the past five years.
AID1220440Stability in water2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814595Antitumor activity against mouse SCC-7 cells implanted in C3H mouse assessed as tumor growth time at 12 mg/kg, ip treated every other day 3 times in total (Rvb = 2.8 +/- 0.6 day)2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220429Drug excretion in Wistar Hanover rat feces at 10 mg/kg, iv administered as single dose measured on day 12012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220421Half life in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220451Drug metabolism assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-1-oxo-3-((2-oxo-2-(3-oxoazetidin-1-yl)ethyl)thio)propan-2-yl)amino)-5-oxopentanoic acid] formation after 1 hr in presence of excess reduced GSH at pH 7.8 by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220403Drug metabolism in human whole blood assessed as [(R)-2-(2-amino-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)propanamido)acetic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220405Drug metabolism in human whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-1-oxo-3-((2-oxo-2-(3-oxoazetidin-1-yl)ethyl)thio)propan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814597Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220434Drug excretion in Wistar Hanover rat feces at 10 mg/kg, iv administered as single dose measured on day 72012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814603Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220424Volume of distribution in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814602Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220416Binding affinity to monkey hemoglobin assessed as protein bound compound level at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220452Ratio of drug level in rat blood to rat plasma at 1 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220418Binding affinity to rat hemoglobin assessed as protein bound compound level at 20 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220417Binding affinity to human hemoglobin assessed as protein bound compound level at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220453Ratio of drug level in dog blood to dog plasma at 1 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220397Drug metabolism in human whole blood assessed as (R)-2-amino-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)propanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814604Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220442Drug metabolism assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation after 1 hr in presence of reduced GSH at pH 7.8 by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220394Retention time in rat whole blood in presence of 0.1% formic acid in acetonitrile at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220438Drug level in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose after 24 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814605Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220441Stability in pH 7.0 buffer2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814601Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220398Drug metabolism in rat whole blood assessed as (R)-2-amino-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)propanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220393Retention time in human whole blood in presence of 0.1% formic acid in acetonitrile at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220407Drug metabolism in human whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-(hydroxyimino)azetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220415Binding affinity to dog hemoglobin assessed as protein bound compound level at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220411Binding affinity to human hemoglobin assessed as alkylation on Hb beta chain Cys-93 locus at 0.53 to 5.5 mM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220413Ratio of drug level in human blood to human plasma at 20 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220439Drug level in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose after 168 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814600Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1814598Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1814608Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220422AUC (0 to t) in Wistar Hanover rat blood at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220408Drug metabolism in rat whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-(hydroxyimino)azetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220402Drug metabolism in rat whole blood assessed as [(R)-2-amino-3-((2-(3-nitroazetidin-1-yl)-2-oxoethyl)thio)propanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220456Ratio of drug level in rat blood to rat plasma at 20 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220428Drug excretion in Wistar Hanover rat feces at 10 mg/kg, iv administered as single dose measured on day 22012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220454Ratio of drug level in monkey blood to monkey plasma at 1 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220432Ratio of drug level in blood to plasma in Wistar Hanover rat at 10 mg/kg, iv administered as single dose after 168 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814596Antitumor activity against mouse SCC-7 cells implanted in C3H mouse assessed as tumor growth time delay at 12 mg/kg, ip treated every other day 3 times in total2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220396Drug metabolism in rat whole blood assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation at 20 uM by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814606Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220455Ratio of drug level in human blood to human plasma at 1 uM after 30 mins2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1814609Terminal half life in human plasma2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Discovery of RRx-001, a Myc and CD47 Downregulating Small Molecule with Tumor Targeted Cytotoxicity and Healthy Tissue Cytoprotective Properties in Clinical Development.
AID1220426AUC (0 to infinity) in Wistar Hanover rat plasma at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220436Drug level in Wistar Hanover rat bile at 10 mg/kg, iv administered as single dose after 24 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220445Drug metabolism assessed as [(S)-2-amino-5-(((R)-1-((carboxymethyl)amino)-3-((2-(3-nitroazetidin-1-yl)-2-oxoethyl)thio)-1-oxopropan-2-yl)amino)-5-oxopentanoic acid] formation after 1 hr in presence of excess reduced GSH at pH 7.8 by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220423Half life in Wistar Hanover rat plasma at 10 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1220444Drug metabolism assessed as (R)-2-amino-3-((2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl)thio)propanoic acid] formation after 1 hr in presence of cysteine at pH 7.8 by LC-MS/MS method2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (45)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's31 (68.89)24.3611
2020's14 (31.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.85

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.85 (24.57)
Research Supply Index3.93 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index43.69 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (11.11%)5.53%
Reviews9 (20.00%)6.00%
Case Studies3 (6.67%)4.05%
Observational0 (0.00%)0.25%
Other28 (62.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]