PENETRATION OF 3-DEAZAURIDINE INTO HUMAN-BRAIN, INTRA-CEREBRAL TUMOR, AND CEREBROSPINAL-FLUID

  • 1 January 1979
    • journal article
    • research article
    • Vol. 39  (10) , 4119-4122
Abstract
The antitumor agent 3-deazauridine (DAU) was administered rapidly to 4 patients before surgical removal of intracerebral tumor. Tumor, adjacent brain tissue and temporalis muscle were assayed for DAU by high-pressure liquid chromatography. DAU penetrated comparably into tumor, brain and muscle; in 1 patient, tissue concentrations were higher than concurrent plasma concentrations. The active metabolite 3-deazauridine 5''-triphosphate was quantitated in 1 tumor sample and greatly exceeded its Ki for CTP synthetase. DAU was also present in autopsy brain specimens from 2 patients treated shortly antemortem. CSF concentrations were 22.1 and 59.0%, respectively, of concurrent plasma concentrations during continuous infusion of DAU in 2 patients. CSF concentration was 3.1 .mu.g/ml 2 h after a 30 min infusion of 1.5 g of drug/m2 and fell to 1.9 .mu.g/ml at 16 h. Thus, DAU is capable of penetrating into intracerebral tumor, brain and CSF and is worthy of investigation in the treatment of intracerebral and meningeal neoplasms.

This publication has 0 references indexed in Scilit: