Abstract
The antitumor agent 3-deazauridine (DAU) was administered rapidly to four patients before surgical removal of intracerebral tumor. Tumor, adjacent brain tissue, and temporalis muscle were assayed for DAU by high-pressure liquid chromatogrphy. DAU penetrated comparably into tumor, brain, and muscle; in one patient, tissue concentrations were higher than concurrent plasma concentrations. The active metabolite 3-deazauridine 5'-triphosphate was quantitated in one tumor sample and greatly exceeded its K(i) for cytidine 5'-triphosphate synthetase. DAU was also present in autopsy brain specimens from two patients treated shortly anetmortem. Cerebrospinal fluid concentrations were 22.1 and 59.0%, respectively, of concurrent plasma concentrations during continuous infusion of DAU in two patients. Cerebrospinal fluid concentration was 3.1 μg/ml 2 hr after a 30-min infusion of 1.5 g of drug per sq m and fell to 1.9 μg/ml at 16 hr. Thus, DAU is capable of penetrating into intracerebral tumor, brain, and cerebrospinal fluid and is worthy of investigation in the treatment of intracerebral and meningeal neoplasms.
Original language | English (US) |
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Pages (from-to) | 4119-4122 |
Number of pages | 4 |
Journal | Cancer Research |
Volume | 39 |
Issue number | 10 |
State | Published - 1979 |
ASJC Scopus subject areas
- Oncology
- Cancer Research