Summary
The in vivo distribution of the antileukemic agent busulfan labeled with the positron-emitting radionuclide carbon 11 was investigated in cynomolgus monkeys and in a human patient using positron emission tomography. After i.v. injection of the radiotracer, its regional uptake was monitored for about 1 h in the monkey's body and in a separate experiment, in the monkey's brain. The concentration of radioactivity in the liver, which showed the highest levels of all the organs scanned, increased throughout the experiment and was 9-fold that in the brain at the end of the experiment. [11C]-Busulfan rapidly crossed the blood-brain barrier. The radioactivity peaked in both the cortex and the white matter showing a ratio of 1.25, at 3 min but declined quickly to yield a ratio of approximately 1 after 30 min. In the human brain, radioactivity in the cerebellum, cortex, and white matter reached a maximum within 5 min showing a cortex:white matter ratio of 1.6. The activity in the cortex declined to yield a ratio of 1 within 30 min. Of the delivered dose, 20% penetrated into the brain.
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Abbreviations
- CSF:
-
cerebrospinal fluid
- AML:
-
acute myelocytic leukemia
- BMT:
-
bone marrow transplantation
- PET:
-
positron emission tomography
- BBB:
-
blood-brain barrier
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This work was supported by grants from the Swedish Cancer Society (2805-B90-01X) and the Swedish Medical Research Council (B9012X0827603A and B9012P0843102B)
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Hassan, M., öberg, G., Ericson, K. et al. In vivo distribution of [11C]-busulfan incynomolgus monkey and in the brain of a human patient. Cancer Chemother. Pharmacol. 30, 81–85 (1992). https://doi.org/10.1007/BF00686397
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DOI: https://doi.org/10.1007/BF00686397