Dady P J, Taylor G A, Muindi J F, Calvert A H, Smith I E, Smyth J F, Harrap K R
Cancer Treat Rep. 1981;65 Suppl 1:37-43.
A phase I clinical study of a combination of thymidine (TdR), inosine (IR), and allopurinol used as rescue from 24-hour infusions of methotrexate (MTX) was undertaken following animal studies that had shown a better preservation of antitumor activity with this system than with folinic acid. TdR and IR were given in the dose ratio 5:1 by weight throughout. Rescue from MTX, 400 mg/m2, could be achieved with a TdR dose in the combination of 1 g/m2/24 hours. This same rescue was also effective when the MTX dose was increased to 800 mg/m2, but only partly effective at an MTX dose of 1.5 g/m2. It was not necessary to raise the levels of circulating nucleosides significantly above normal to achieve rescue. MTX-related skin lesions occurred more frequently than might be expected with the MTX dose used.
在动物研究表明该系统比甲酰四氢叶酸能更好地保留抗肿瘤活性之后，开展了一项关于使用胸苷（TdR）、肌苷（IR）和别嘌呤醇联合作为24小时甲氨蝶呤（MTX）输注解救剂的I期临床研究。整个过程中，TdR和IR按重量比5:1给药。对于400mg/m²的MTX，联合使用1g/m²/24小时的TdR剂量可实现解救。当MTX剂量增加到800mg/m²时，同样的解救方法也有效，但在MTX剂量为1.5g/m²时仅部分有效。无需将循环核苷水平显著提高到正常水平以上即可实现解救。与MTX相关的皮肤病变出现的频率高于所用MTX剂量可能预期的频率。
