Pharmacokinetics of intracarotid artery 14C-BCNU in the squirrel monkey

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Abstract
A comparison of i.v. to intracarotid artery (ICA) administration of 14C-BCNU (1,3-bis(2-chloroethyl)-1-nitrosourea) [anti-cancer agent] was made in squirrel monkeys. Radioactivity was measured as soluble drug products and as RNA-, DNA- and protein-bound radioactivity. The ICA administration of BCNU achieved 190% to 280% higher brain nucleic acid-bound drug levels than use of the i.v. route in the infused hemisphere and 130% to 280% higher levels than in the noninfused hemisphere. Some brain regions directly subserved by the middle cerebral artery had bound drug levels 4- to 5-fold greater than those found in regions of noninfused brain. A need for BCNU dose reduction due to myelotoxicity may be an indication for ICA therapy in selected brain-tumor cases.