Intracerebral penetration and tissue distribution of 2,5-diaziridinyl 3,6-bis(carboethoxyamino) 1,4-benzoquinone (AZQ, NSC-182986)

Niramol Savaraj, Katherine Lu, Lynn G Feun, Milam E. Leavens, David Stewart, Michael A. Burgess, Robert S. Benjamin, Ti Li Loo

Research output: Contribution to journalArticle

25 Citations (Scopus)

Abstract

[14C]AZQ (2-4 mg/m2, 100-200 mCi) was administered at varying times to five patients undergoing surgical resection of intracerebral tumors. Plasma, cerebrospinal fluid (CSF), edematous brain, and tumor specimens were obtained during surgery and the concentration of AZQ was determined radiochemically and chromatographically. Total [14C]AZQ equivalent concentration in tumor for two patients was determined to be 47.5% and 85% of concurrent plasma concentration which was similar to that found in normal brain (60.4% and 75.5% respectively). Only 18-45% of the total radioactivity in tumor tissue and 30-56% in plasma were accounted for by unchanged AZQ. These findings suggest that AZQ may be metabolized to a certain extent. Tissue samples from various organs were obtained during autopsy in a patient who expired ten days after AZQ administration. The highest AZQ concentration was found in the liver, followed by the kidney. Comparable amounts were found in normal brain and brain tumor (22 ng/ g vs. 31 ng/ g respectively). These results indicate that AZQ penetrates readily into the normal brain and brain tumor with a tendency to persist.

Original languageEnglish
Pages (from-to)15-19
Number of pages5
JournalJournal of Neuro-Oncology
Volume1
Issue number1
DOIs
StatePublished - Mar 1 1983
Externally publishedYes

Fingerprint

diaziquone
Tissue Distribution
Brain Neoplasms
Brain
Neoplasms
Radioactivity
Cerebrospinal Fluid
Autopsy

Keywords

  • AZQ
  • CSF
  • intracerebral tumor

ASJC Scopus subject areas

  • Neuroscience(all)
  • Oncology
  • Clinical Neurology
  • Cancer Research

Cite this

Intracerebral penetration and tissue distribution of 2,5-diaziridinyl 3,6-bis(carboethoxyamino) 1,4-benzoquinone (AZQ, NSC-182986). / Savaraj, Niramol; Lu, Katherine; Feun, Lynn G; Leavens, Milam E.; Stewart, David; Burgess, Michael A.; Benjamin, Robert S.; Loo, Ti Li.

In: Journal of Neuro-Oncology, Vol. 1, No. 1, 01.03.1983, p. 15-19.

Research output: Contribution to journalArticle

Savaraj, Niramol ; Lu, Katherine ; Feun, Lynn G ; Leavens, Milam E. ; Stewart, David ; Burgess, Michael A. ; Benjamin, Robert S. ; Loo, Ti Li. / Intracerebral penetration and tissue distribution of 2,5-diaziridinyl 3,6-bis(carboethoxyamino) 1,4-benzoquinone (AZQ, NSC-182986). In: Journal of Neuro-Oncology. 1983 ; Vol. 1, No. 1. pp. 15-19.
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