Clinical Pharmacokinetics of Altretamine

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Abstract

Altretamine (hexamethylmelamine) is an antitumour drug with demonstrated antitumour activity in refractory ovarian cancer. Due to its poor water solubility, the drug has been given by the oral route. In all animal species, including humans, altretamine undergoes oxidative N-demethylation with the formation of hydroxymethyl derivatives as intermediates. Hydroxymethylmelamines are believed to be responsible for the cytotoxic and antitumour activity of the drug. The inter- and intrapatient variability of the bioavailability of altretamine after oral administration represents an important drawback for effective clinical use of this drug. The variability appears to be mostly related to the first-pass effect and therefore may be overcome by intravenous administration of the drug. Although attempts to administer the drug intravenously have not been successful in the past, some investigations on the use of the new parental formulation of altretamine are in progress.

Original languageEnglish
Pages (from-to)439-448
Number of pages10
JournalClinical Pharmacokinetics
Volume28
Issue number6
DOIs
Publication statusPublished - 1995

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology
  • Pharmacology, Toxicology and Pharmaceutics(all)

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