Ability of a New Antitumor Agent, AZQ, to Penetrate into Cerebrospinal Fluid

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Abstract
The ability of a new antitumor agent, AZQ (2,5-diaziridinyl-3,6-bis-carboethoxyamino-l,4-benzoquinone), NSC No. 182986, to enter the cerebrospinal fluid (CSF) was studied in nonhuman primates. Following parenteral administration of 14C-AZQ, CSF radioactivity rose quickly and reached a maximum value 60 min after administration. Total radioactivity in the CSF was about 25–35% of the corresponding plasma level at time points subsequent to maximum CSF concentration. Chloroform extraction and thin-layer chromatography revealed that much of the total radioactivity was not parent AZQ and that parent AZQ declined rapidly in both plasma and CSF with a half-life less than 1 h. AZQ clearly entered the CSF and yielded CSF concentrations comparable to plasma values.