Efaproxiral - CAS 131179-95-8
Catalog number:
Not Intended for Therapeutic Use. For research use only.
synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. One use for efaproxiral is to increase the efficacy of certain chemotherapy drugs which have reduced efficacy against hypoxic tumours, and can thus be made more effective by increased offloading of oxygen into the tumour tissues. However, no benefit was seen for efaproxiral in phase III clinical trials.
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RSR13,Efaproxyn; NSC722758
Current Developer:
Allos Therapeutics
1.The role of emerging and investigational therapies for metastatic brain tumors: a systematic review and evidence-based clinical practice guideline of selected topics.
Olson JJ1, Paleologos NA, Gaspar LE, Robinson PD, Morris RE, Ammirati M, Andrews DW, Asher AL, Burri SH, Cobbs CS, Kondziolka D, Linskey ME, Loeffler JS, McDermott M, Mehta MP, Mikkelsen T, Patchell RA, Ryken TC, Kalkanis SN. J Neurooncol. 2010 Jan;96(1):115-42. doi: 10.1007/s11060-009-0058-3. Epub 2009 Dec 3.
QUESTION: What evidence is available regarding the emerging and investigational therapies for the treatment of metastatic brain tumors?
2.Non-cytotoxic radiosensitizers in brain radiotherapy: journey till the first decade of this millennium.
Mohindra P1, Sinha RN, Andrews RJ, Khuntia D. Curr Cancer Drug Targets. 2012 Mar;12(3):260-78.
Brain tumors, primary and metastatic, are a cause of significant mortality and morbidity. Radiotherapy (RT) forms an integral part of the treatment of brain tumors. Intrinsic relative tumor radio-resistance, normal tissue tolerance and impact on neurocognitive function, all limit the efficacy of RT. Radiosensitizers can potentially increase efficacy on tumors while maintaining normal tissue toxicity, with or without inherent cytotoxicity. This article reviews the evolution of evidence with use of non-cytotoxic radiosensitizers in brain radiotherapy and their status at the end of the first decade of this millennium. Considering, the era of development and mechanism of action, these agents are classified as first, second and third-generation non-cytotoxic radiosensitizers. The last millennium involved elaboration of first-generation compounds including halogenated pyrimidines, hypoxic cell sensitizers (e.g. imidazoles) and glycolytic inhibitors (e.
3.Improved survival, quality of life, and quality-adjusted survival in breast cancer patients treated with efaproxiral (Efaproxyn) plus whole-brain radiation therapy for brain metastases.
Scott C1, Suh J, Stea B, Nabid A, Hackman J. Am J Clin Oncol. 2007 Dec;30(6):580-7.
OBJECTIVE: To determine whether efaproxiral, an allosteric modifier of hemoglobin, improves quality of life and quality of survival in patients with primary breast cancer and brain metastases when used as an adjunct to whole-brain radiation therapy (WBRT).
4.Reduction in hemoglobin-oxygen affinity results in the improvement of exercise capacity in mice with chronic heart failure.
Watanabe T1, Takeda T, Omiya S, Hikoso S, Yamaguchi O, Nakano Y, Higuchi Y, Nakai A, Abe Y, Aki-Jin Y, Taniike M, Mizote I, Matsumura Y, Shimizu T, Nishida K, Imai K, Hori M, Shirasawa T, Otsu K. J Am Coll Cardiol. 2008 Aug 26;52(9):779-86. doi: 10.1016/j.jacc.2008.06.003.
OBJECTIVES: This study examined whether a reduction in hemoglobin-oxygen affinity improves exercise capacity in mice with heart failure.
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CAS 131179-95-8 Efaproxiral

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