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Ro 03-8799对小鼠肿瘤的放射增敏作用:急性和持续给药

Radiosensitization of a mouse tumour by Ro 03-8799: acute and protracted administration.

作者信息

Hill S A, Fowler J F, Minchinton A I, Stratford M R, Denekamp J

出版信息

Int J Radiat Biol Relat Stud Phys Chem Med. 1983 Aug;44(2):143-50. doi: 10.1080/09553008314550941.

Abstract

The nitroimidazole Ro 03-8799 has been tested as a sensitizer of hypoxic tumour cells, using regrowth delay of a mouse mammary carcinoma. This drug has a short biological half-life and has previously proved to be less promising in tumour experiments than was predicted from in vitro studies and from artificially hypoxic skin. The postulate that this might result from the delay in penetrating to poorly vascularized tumour regions has been tested by maintaining constant blood and tumour levels for 2 hours before irradiation, using an infusion pump. For equivalent gross tumour concentrations at the time of irradiation there was no significant difference in the radiosensitization achieved with a single dose or with prolonged administration. This indicates that slow penetration of the drug is not a problem.

摘要

已使用小鼠乳腺癌的再生长延迟,对硝基咪唑Ro 03-8799作为缺氧肿瘤细胞的增敏剂进行了测试。这种药物的生物半衰期很短,先前已证明在肿瘤实验中的效果不如体外研究和人工缺氧皮肤所预测的那样有前景。有人提出,这可能是由于药物渗透到血管化不良的肿瘤区域存在延迟所致,为此通过使用输液泵在照射前2小时维持恒定的血液和肿瘤水平来进行了测试。对于照射时等效的肿瘤总体浓度,单次给药或长时间给药所实现的放射增敏作用没有显著差异。这表明药物的缓慢渗透不是问题。

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