Sealy R, Korrubel J, Cridland S, Blekkenhorst G
Cancer. 1984 Oct 15;54(8):1535-40. doi: 10.1002/1097-0142(19841015)54:8<1535::aid-cncr2820540811>3.0.co;2-f.
The actions of misonidazole as a radiation sensitizer, hypoxic cytotoxic, and metabolic inhibitor are all concentration-dependent, and the commonly prescribed oral dose (12 g/m2) appears to be inadequate. The drug has, therefore, been given interstitially in solid form, when local tissue doses of the order of tens of millimolar are attained, to four patients, all with advanced disease. In the three cases (two squamous carcinomas and a malignant melanoma) in whom the drug concentration was considered to be adequate, a beneficial effect was obtained, which, in two instances, was associated with doses of radiation of 6 and 8 Gy, respectively. This approach has a wide potential application in cancer therapy.
米索硝唑作为一种辐射增敏剂、低氧细胞毒素和代谢抑制剂，其作用均呈浓度依赖性，常用的口服剂量（12 g/m²）似乎并不足够。因此，已将该药物以固体形式间质内给药，使局部组织剂量达到数十毫摩尔，用于4例均患有晚期疾病的患者。在3例（2例鳞状细胞癌和1例恶性黑色素瘤）被认为药物浓度足够的病例中，获得了有益效果，其中2例分别与6 Gy和8 Gy的辐射剂量相关。这种方法在癌症治疗中具有广泛的潜在应用。
