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Pharmacokinetics of Superselective Intra-Arterial and Intravenous [¹¹C]BCNU Evaluated by PET

Brain Imaging Center, Montreal Neurological Institute and Hospital, and the Department of Neurology and Neurosurgery of McGill University

Correspondence: For reprints contact: Jane L. Tyler, MD, Brain Imaging Center, Montreal Neurology Institute and Hospital, 3801 University, Montreal, Quebec, Canada H3A 2B4.

ABSTRACT

The pharmacokinetics of i.v. and superselective intra-arterial carbon-11 1,3-bis-(2-chloroethyl)-1-nitrosourea ([¹¹C]BCNU) were directly compared for the first time in ten patients with recurrent gliomas using positron emission tomography (PET). Intra-arterial administration of [¹¹C]BCNU achieved concentrations of the drug in the tumor that averaged 50 times higher than with a comparable i.v. dose. These preliminary results suggest that the degree of early metabolic trapping of BCNU in tumor correlates with the clinical response to this chemotherapy.

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