Ginos J Z, Cooper A J, Dhawan V, Lai J C, Strother S C, Alcock N, Rottenberg D A
Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, NY 10021.
J Nucl Med. 1987 Dec;28(12):1844-52.
The biodistribution, blood clearance, and in vivo transformation of cisplatin (cisdiaminedichloroplatinum, DDP) were studied in rats using 13N-labeled and unlabeled DDP. Following the i.v. injection of [13N]DDP, virtually no 13N activity was detected in brain tissue, and no measurable amount of the 13N label was displaced from [13N]DDP. Based on these results, [13N]DDP/positron emission tomographic (PET) scans were performed in two glioblastoma patients undergoing Phase II intra-arterial (i.a.) DDP chemotherapy: [13N]DDP was infused i.v. over 13-15 min, during which time serial PET scans were obtained. One hour later, [13N]DDP mixed with cold DDP (100 mg/m2 therapeutic dose) was infused at the same rate i.a., and a second sequence of PET scans was acquired. The pharmacologic advantage of i.a. administration was calculated as the ratio of integrated tumor/brain count ratios for the i.a. and i.v. studies. Our preliminary results demonstrate the feasibility of quantifying the pharmacologic advantage of i.a. DDP chemotherapy in individual brain tumor patients using [13N]DDP and PET.
使用13N标记和未标记的顺铂（顺二氨二氯铂，DDP）在大鼠中研究了顺铂的生物分布、血液清除率和体内转化。静脉注射[13N]DDP后，在脑组织中几乎未检测到13N活性，并且没有可测量量的13N标记从[13N]DDP中置换出来。基于这些结果，对两名正在接受II期动脉内（i.a.）DDP化疗的胶质母细胞瘤患者进行了[13N]DDP/正电子发射断层扫描（PET）：静脉内输注[13N]DDP持续13 - 15分钟，在此期间获得系列PET扫描。一小时后，以相同速率动脉内输注与冷DDP（100mg/m2治疗剂量）混合的[13N]DDP，并获取第二组PET扫描。动脉内给药的药理学优势计算为动脉内和静脉内研究的肿瘤/脑积分计数比值之比。我们的初步结果证明了使用[13N]DDP和PET对个体脑肿瘤患者动脉内DDP化疗的药理学优势进行定量的可行性。
