"目录号: HY-13619
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Efaproxiral是一种血红蛋白 (Hb) 合成变构调节剂, 降低血红蛋白氧 (O2) 的结合亲和力。
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生物活性
Description
Efaproxiral is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.in vitro: 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. Efaproxiral can enhance the oxygenation of hypoxic tumours and function as a radiation sensitiser, increasing the effectiveness of RT.
Clinical Trial
NCT00083304
Spectrum Pharmaceuticals, Inc
Breast Cancer-Metastases
February 2004
Phase 3
NCT00005887
Spectrum Pharmaceuticals, Inc
Metastatic Cancer
February 2000
Phase 3
NCT00005855
New Approaches to Brain Tumor Therapy Consortium-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
July 2000
Phase 1-Phase 2
NCT00055887
Spectrum Pharmaceuticals, Inc
Lung Cancer
November 2002
Phase 3
NCT00004202
Spectrum Pharmaceuticals, Inc
Lung Cancer
October 1998
Phase 2
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References
[1].Stea B, et al. Efaproxiral red blood cell concentration predicts efficacy in patients with brain metastases. Br J Cancer. 2006 Jun 19;94(12):1777-1784.