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尼莫唑作为乏氧放疗增敏剂的I期临床研究。

A phase I clinical study of Nimorazole as a hypoxic radiosensitizer.

作者信息

Timothy A R, Overgaard J, Overgaard M

出版信息

Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1765-8. doi: 10.1016/0360-3016(84)90545-5.

DOI:10.1016/0360-3016(84)90545-5
PMID:6480460
Abstract

Nimorazole, a 5-Nitromidazole compound has been shown in animal studies to have similar radiosensitizing properties to misonidazole at clinically acceptable dose levels. The drug is well absorbed in humans after oral administration with peak plasma levels occurring around 90 min after ingestion (range 35-135 min) and a plasma half life between 2 and 4.8 hours. Total doses of Nimorazole up to 60 grams given in daily doses with conventional radiation therapy have demonstrated a significant lack of side effects, in particular no demonstrable neurotoxicity.

摘要

尼莫唑,一种5-硝基咪唑化合物,在动物研究中已表明,在临床可接受的剂量水平下,其具有与米索硝唑相似的放射增敏特性。该药物口服后在人体中吸收良好,摄入后约90分钟(范围为35 - 135分钟)达到血浆峰值水平,血浆半衰期在2至4.8小时之间。在常规放射治疗中,每日给予高达60克的尼莫唑总剂量,已证明其副作用显著缺乏,尤其是未发现明显的神经毒性。

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1
A phase I clinical study of Nimorazole as a hypoxic radiosensitizer.尼莫唑作为乏氧放疗增敏剂的I期临床研究。
Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1765-8. doi: 10.1016/0360-3016(84)90545-5.
2
Studies of the pharmacokinetic properties of nimorazole.尼莫唑的药代动力学特性研究。
Br J Cancer. 1983 Jul;48(1):27-34. doi: 10.1038/bjc.1983.153.
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A comparative investigation of nimorazole and misonidazole as hypoxic radiosensitizers in a C3H mammary carcinoma in vivo.硝唑咪和米索硝唑作为体内C3H乳腺癌低氧放射增敏剂的比较研究。
Br J Cancer. 1982 Dec;46(6):904-11. doi: 10.1038/bjc.1982.300.
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A phase I study of the hypoxic cell radiosensitizer Ro-03-8799.乏氧细胞放射增敏剂Ro-03-8799的I期研究。
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The clinical testing of Ro 03-8799--pharmacokinetics, toxicology, tissue and tumor concentrations.Ro 03 - 8799的临床试验——药代动力学、毒理学、组织及肿瘤浓度
Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1759-63. doi: 10.1016/0360-3016(84)90544-3.
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The radiosensitizer Ro 03-8799 and the concentrations which may be achieved in human tumours: a preliminary study.放射增敏剂Ro 03 - 8799及其在人类肿瘤中可能达到的浓度:一项初步研究。
Br J Cancer. 1982 Nov;46(5):706-10. doi: 10.1038/bjc.1982.262.
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Pilot study of nimorazole as a hypoxic-cell sensitizer with the "chart" regimen in head and neck cancer.尼莫唑作为乏氧细胞增敏剂与“图表”方案联合用于头颈癌的初步研究。
Int J Radiat Oncol Biol Phys. 1998 Nov 1;42(4):807-10. doi: 10.1016/s0360-3016(98)00309-5.
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Reevaluation of the radiosensitizing effects of sanazole and nimorazole in vitro and in vivo.体外和体内重新评估沙那唑和尼莫唑的放射增敏作用。
J Radiat Res. 2005 Dec;46(4):453-9. doi: 10.1269/jrr.46.453.
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Initial report of the phase I trial of the hypoxic cell radiosensitizer SR-2508.缺氧细胞放射增敏剂SR - 2508的I期试验初步报告。
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Compliance and toxicity of the hypoxic radiosensitizer nimorazole in the treatment of patients with head and neck squamous cell carcinoma (HNSCC).低氧放射增敏剂尼莫唑在头颈部鳞状细胞癌(HNSCC)患者治疗中的依从性和毒性
Acta Oncol. 2014 May;53(5):654-61. doi: 10.3109/0284186X.2013.864050. Epub 2013 Dec 13.

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