新型辐射增敏药RRx-001

A novel radiosensitizer RRx-001

辐射增敏药可提高射线对肿瘤细胞,尤其是乏氧细胞的杀伤率,增强放疗效果,且其对有氧正常组织危害小,使用方便,因而有望成为放疗中的重要辅助药物.新型二硝基氮杂环丁烷辐射增敏药RRx-001源自航空产业.作为一氧化氮的供体分子,RRx-001可透过红细胞膜,与血红蛋白的β半胱氨酸93结合,并在乏氧环境中大量释放一氧化氮,从而提高乏氧细胞对照射的敏感度.临床实验显示RRx-001具有良好的安全性和耐受性.目前其对胆管癌、结直肠癌等肿瘤的治疗正在进行临床Ⅱ期实验.

The effect of radiotherapy can be enhanced by radiosensitizers because these compounds can improve the killing rate of radiation on tumor cells,especially on hypoxic cells.Moreover,radiosensitizers show little damage to the aerobic normal tissue and are easy to use.For these reasons,radiosensitizers are expected to become the important treatment in radiotherapy.RRx-001,a novel dinitroazetidine radiosensitizer,is an aerospace industry-derived anti-cancer agent.As an NO-donating compound,RRx-001 can pass through erythrocyte membrane,selectively bind to hemoglobin at the betacysteine 93 residue,and release large amounts of NO under hypoxic conditions,so as to improve radiosensitivity of hypoxic cells.RRx-001 shows good safety and tolerability in clinical studies and now is undergoing phase Ⅱ clinical trials in cholangiocarcinoma,colorectal neoplasms,ect.