RRx-001, A novel dinitroazetidine radiosensitizer
نویسندگان
چکیده
منابع مشابه
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
RRx-001 has shown promise as a novel cancer therapeutic agent. The disposition of RRx-001 was evaluated in vitro and after intravenous administration to rats. At both 24 and 168 h after a single intravenous administration of ¹⁴C-RRx-001 (10 mg/kg), the majority of radiolabel was in the blood. The recovery of label in excreta was quite low, but the major route of radiolabel excretion was via the...
متن کاملMagnetic resonance imaging of RRx-001 pharmacodynamics in preclinical tumors
RRx-001 is an anticancer agent that subjects cancer cells to reactive oxygen/nitrogen species (ROS/RNS) and acts as an epigenetic modifier. We have used a thiol-bearing MRI contrast agent, Gd-LC7-SH, to investigate the pharmacodynamics of RRx-001 in CHP-100 Ewing's Sarcoma, HT-29 colorectal carcinoma, and PANC-1 pancreatic carcinoma xenografts in SCID mice. Binding of Gd-LC7-SH to the Cys34 res...
متن کاملNrf2 activity as a potential biomarker for the pan-epigenetic anticancer agent, RRx-001
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a master regulatory transcription factor that plays an important role in the antioxidant response pathway against anticancer drug-induced cytotoxic effects. RRx-001 is a new anticancer agent that generates reactive oxygen and nitrogen species, and leads to epigenetic alterations in cancer cells. Here we report the RRx-001 mediated nuclear tr...
متن کاملEpigenetic effects of RRx-001: a possible unifying mechanism of anticancer activity
RRx-001 is a novel aerospace-derived compound currently under investigation in several ongoing Phase II studies. In a Phase I trial, it demonstrated anti-cancer activity and evidence of resensitization to formerly effective therapies in heavily pre-treated patients with relapsed/refractory solid tumors. RRx-001 generates reactive oxygen and nitrogen species (ROS and RNS) and nitric oxide (NO), ...
متن کاملA Recurrent Platinum Refractory Ovarian Cancer Patient With a Partial Response After RRx-001 Resensitization to Platinum Doublet
This case report describes the clinical course of a heavily pretreated patient enrolled on the Phase II QUADRUPLE THREAT clinical trial (NCT02489903) with recurrent metastatic epithelial ovarian cancer that was previously treated with a platinum doublet and that benefited from another reintroduction of a platinum doublet after a brief priming period with RRx-001. Platinum-taxane combination is ...
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ژورنال
عنوان ژورنال: Investigational New Drugs
سال: 2016
ISSN: 0167-6997,1573-0646
DOI: 10.1007/s10637-016-0326-y