Central nervous system (CNS) penetration of homoharringtonine (HHT)

Niramol Savaraj, Lynn G. Feun, Katherine Lu, Maam Leavens, Richard Moser, William S. Fields, Ti Li Loo

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

Generally tritiated homoharringtonine ([3H]HHT, 150 μCi, 430 μg) was administered intravenously to seven patients at varying times before surgical resection of malignant brain tumor. Plasma, urine, cerebrospinal fluid (CSF), and tumor specimens were obtained during surgery, and the concentrations of HHT, its major metabolite, and [3H]HHT equivalent were determined chromatographically and radiochemically. For [3H]HHT equivalent, the concentration in tumor ranged from 0.6 to 4.3 ng/g and the ratio of tumor to plasma concentration from 0.5 to 1.8. In one patient who had CSF available for drug determination, the CSF to plasma ratio of total [3H]HHT was 0.3 at 45 minutes after drug administration and less than 0.2 ng/ml was unchanged HHT. For unchanged HHT, drug concentration in tumor ranged from undetectable (4 patients) to 1.8 ng/g. A major metabolite of HHT was detectable in the tumor specimens of all the patients. These results indicate that homoharringtonine can penetrate into brain tumors; in 3 patients with brain tumors, the ratios of HHT concentration in the tumor to that in the concurrent plasma were greater than one.

Original languageEnglish (US)
Pages (from-to)77-81
Number of pages5
JournalJournal of neuro-oncology
Volume5
Issue number1
DOIs
StatePublished - Mar 1 1987

Keywords

  • central nervous system
  • homoharringtonine
  • penetration

ASJC Scopus subject areas

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

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