Jentzsch K, Kärcher K H, Kogelnik H D, Maida E, Mamoli B, Wessely P, Zaunbauer F, Nitsche V
Strahlentherapie. 1977 Dec;153(12):825-31.
The 2-nitroimidazole derivate Ro 07-0582 is known from experimental studies to be a very efficient radiosensitizer of hypoxic cells. Experiences with its clinical use are very limited so far. This study reports the side effects observed in the use of this drug in 12 patients. Nine of these patients were suffering from brain tumors, 3 from extracerebral tumors. In 8 of our 12 patients a sensoric polyneuropathy occurred which was strongly related to the total dose of the drug administered. Polyneuropathy was observed on the average after a total dose of 26 grams, but was already noticed at doses as low as 22 grams. It showed a good tendency for remission after termination of the drug treatment and was reversible in all patients within 4 weeks. In one patient with a brain tumor a severe organic psychosyndrome occurred which is possibly related to the drug. This side effect was also reversible. In this small group of patients the critical dose limit seems to be 29 grams. This dose can be divided into 6 fractions of 60-80 mg/kg. Up to the present knowledge this single dose is likely to give an enhancement ratio of 1,5, which would be extremly valuable for the treatment of hypoxic tumor cells.
2-硝基咪唑衍生物Ro 07-0582在实验研究中被认为是一种非常有效的低氧细胞放射增敏剂。到目前为止，其临床应用经验非常有限。本研究报告了在12例患者中使用该药物时观察到的副作用。其中9例患者患有脑肿瘤，3例患有脑外肿瘤。在我们的12例患者中有8例出现了感觉性多发性神经病，这与所给药的总剂量密切相关。平均在总剂量达到26克后观察到多发性神经病，但在低至22克的剂量时就已被注意到。在药物治疗终止后，它显示出良好的缓解趋势，并且在所有患者中4周内均可逆转。在1例脑肿瘤患者中出现了严重的器质性精神综合征，这可能与药物有关。这种副作用也是可逆的。在这一小群患者中，临界剂量限值似乎为29克。该剂量可分为6个60 - 80毫克/千克的分次剂量。就目前所知，这一单剂量可能会产生1.5的增强比，这对于治疗低氧肿瘤细胞将极其有价值。
