Yamasaki T, Nagao S, Kagawa T, Konishi S, Akiyama Y, Fukuda M, Kimura Y, Moritake K
Department of Neurosurgery, Shimane Medical University.
No Shinkei Geka. 1995 Nov;23(11):963-9.
This clinical study was undertaken to examine intratumoral (i.t.) pharmacokinetics after intraarterial (i.a.) administration of MCNU (80mg/m2) in 5 patients with glioblastoma (GB) and 2 with anaplastic astrocytoma (AA). After resection or stereotactic biopsy of the cystic lesion, an Ommaya reservoir was placed into the tumor cavity in all patients. The distribution of MCNU in blood was compatible with a two-compartment model, and the half life of the alpha-phase and beta-phase was 4.1 minutes and 160.4 minutes, respectively. MCNU was detected in the i.t. fluid in 5 cases, 4 of GB and 1 of AA. The concentration of i.t. MCNU gradually increased during the 5 to 30 minutes after i.a. injection to a level about 20.0% of its blood concentration. However, no MCNU was detected in patients showing partial response (3 of GB and 1 of AA) or no change (1 of GB) after the i.a. infusion of MCNU during maintenance chemotherapy. These results suggests that MCNU may transfer into the tumor tissues. Further investigation is warranted.
本临床研究旨在检测5例胶质母细胞瘤（GB）患者和2例间变性星形细胞瘤（AA）患者经动脉内（i.a.）给予甲环亚硝脲（MCNU，80mg/m²）后的瘤内（i.t.）药代动力学。在对囊性病变进行切除或立体定向活检后，所有患者均在肿瘤腔内放置了Ommaya储液器。MCNU在血液中的分布符合二室模型，α相和β相的半衰期分别为4.1分钟和160.4分钟。在5例患者的瘤内液体中检测到了MCNU，其中4例为GB患者，1例为AA患者。瘤内MCNU的浓度在动脉内注射后5至30分钟内逐渐升高，达到其血液浓度的约20.0%。然而，在维持化疗期间动脉内输注MCNU后显示部分缓解（3例GB患者和1例AA患者）或无变化（1例GB患者）的患者中未检测到MCNU。这些结果表明MCNU可能会转移至肿瘤组织中。有必要进行进一步研究。
