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放射增敏剂Ro-07-0582的临床试验。I. 剂量耐受性、血清和肿瘤浓度。

Clinical testing of the radiosensitiser Ro-07-0582. I. Dose tolerance, serum and tumour concentrations.

作者信息

Gray A J, Dische S, Adams G E, Flockhart I R, Foster J L

出版信息

Clin Radiol. 1976 Apr;27(2):151-7. doi: 10.1016/s0009-9260(76)80137-7.

DOI:10.1016/s0009-9260(76)80137-7
PMID:776493
Abstract

Patients have been given single oral doses of the radiosensitiser Ro-07-0582 and serum concentrations have been attained in the range expected to be of value in radiosensitisation. Immediate gastrointestinal side effects appear to limit the dose to below 140 mg/kg but radiosensitising serum levels of approximately 200 mug/ml can be attained. Tolerance may be improved by giving anti-emetics and a more palatable preparation. Estimates of the concentration of Ro-07-0582 in tumour have ranged from 12 to 92% of the serum concentration at the time of determination.

摘要

已给患者单次口服放射增敏剂Ro-07-0582,并已达到预期对放射增敏有价值的血清浓度范围。即刻出现的胃肠道副作用似乎将剂量限制在140mg/kg以下,但可达到约200μg/ml的放射增敏血清水平。给予止吐药和更可口的制剂可能会提高耐受性。在测定时,肿瘤中Ro-07-0582的浓度估计为血清浓度的12%至92%。

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