| Abstract: |
The biodistribution, blood clearance, and in vivo transformation of cisplatin (cis-diaminedichloroplatinum, 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. |
| Keywords: |
cancer chemotherapy; unclassified drug; cisplatin; nonhuman; comparative study; positron emission tomography; brain tumor; brain neoplasms; animal; animal experiment; diagnostic agent; rat; computer assisted emission tomography; scintiscanning; intraarterial drug administration; rats; radioisotope; nitrogen; intravenous drug administration; injections, intravenous; pharmacokinetics; tomography, emission-computed; injections, intra-arterial; nitrogen 13; nitrogen radioisotopes; human; male; article; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; cisplatin n 13
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