Beckley S, Wajsman L Z, Slack N H, Murphy G P
Urology. 1981 May;17(5):446-8. doi: 10.1016/0090-4295(81)90186-2.
Chlorambucil plus prednisolone were administered to 11 patients with metastasis hormone refractory prostatic cancer, and the results were contrasted with a previously reported series of 23 similar patients treated with the chemical conjugate of these two agents, known as prednimustine or Leo 1031. The conjugated form of treatment (Leo 1031) had a limited therapeutic advantage, in that 3 patients experienced shrinkage of an enlarged prostate, 2 of whom also had elevated acid phosphatase levels return to normal and 5 others experienced only subjective improvement. There were, however, more adverse side effects in this group than those noted in patients treated with the combination of agents. Patients treated with the combination of drugs experienced no appreciable tumor shrinkage and none had acid phosphatase return to normal, although some reduction was noted in 8 of 11 patients who had elevated levels initially. Two of the 11 patients were considered stable for twelve months and one other remained ambulatory with mild pain for six months. Thus, to the degree that these studies permit, it is judged that the conjugated agent may have some limited therapeutic advantage not observed when the unconjugated agents were used.
对11例转移性激素难治性前列腺癌患者给予苯丁酸氮芥加泼尼松龙治疗,并将结果与先前报道的23例接受这两种药物化学偶联物(称为泼尼莫司汀或Leo 1031)治疗的类似患者进行对比。联合治疗形式(Leo 1031)具有有限的治疗优势,即3例患者前列腺肿大缩小,其中2例患者升高的酸性磷酸酶水平也恢复正常,另外5例仅主观症状改善。然而,该组患者的不良反应比联合用药治疗的患者更多。联合用药治疗的患者未出现明显的肿瘤缩小,且无一例酸性磷酸酶恢复正常,尽管最初酸性磷酸酶水平升高的11例患者中有8例有所降低。11例患者中有2例被认为病情稳定达12个月,另1例在轻度疼痛的情况下仍能行走6个月。因此,就这些研究而言,判断该偶联剂可能具有一些未观察到的有限治疗优势,而使用未偶联药物时则无此优势。