Diaziquone, 2,5-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone, plasma and cerebrospinal fluid kinetics

Abstract
Plasma and CSF kinetics of [the antineoplastic drug] diaziquone, (2,5-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone; AZQ), were evaluated after i.v. injection in patients with implanted Ommaya reservoirs. After a 30 min infusion plasma disappearance was very rapid, with a disposition half-life of 2-6 min and an elimination half-life of 25-35 min. Area under the concentration-time curve for CSF was 22%-42% of the corresponding plasma area. Based upon total plasma AZQ concentration, volume of distribution for AZQ was 2.0-10.0 l/m2. Plasma binding of AZQ was 79% in 1 normal subject. When the effect of plasma binding is considered, distribution volumes are more plausible; it appears that free plasma AZQ is completely available to the CSF.

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