Phase i and pharmacological studies of pentamethylmelamine administered by 24-hour intravenous infusion

Ephraim S. Casper, Richard J. Gralla, Garrett R. Lynch, Thomas M. Woodcock, Charles W. Young, David P. Kelsen, Brian R. Jones, Clara Gordon

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Abstract

A Phase I study of pentamethylmelamine (PMM) was conducted, administering the drug as a 24-hr i.v. infusion once weekly for 3 weeks. Doses ranged from 80 to 3000 mg/sq m/week. Twenty-six evaluable patients received a total of 30 courses of PMM. The median performance status of the patients was 60% (range, 40 to 90%), and the median age was 58 years (range, 43 to 72 years). The highest tolerated dose was 2000 mg/sq m/week. Nausea and vomiting were the dose-limiting toxicities; myelosuppression was neither consistent nor severe. One objective response lasting 10 months was noted in a patient with renal cancer. Pharmacokinetic studies using [ring-14C]PMM demonstrated a postinfusion half-life of 14C of approximately 12 hr, with the majority of the radiolabel excreted in the urine. PMM was introduced as a parenteral form of hexamethylmelamine. The present schedule does not permit administration of PMM in a dose greater than the tolerated dose of hexamethylmelamine and does not appear to offer an advantage over the p.o. use of the parent compound.

Original languageEnglish (US)
Pages (from-to)1402-1406
Number of pages5
JournalCancer Research
Volume41
Issue number4
Publication statusPublished - Apr 1 1981

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ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Casper, E. S., Gralla, R. J., Lynch, G. R., Woodcock, T. M., Young, C. W., Kelsen, D. P., ... Gordon, C. (1981). Phase i and pharmacological studies of pentamethylmelamine administered by 24-hour intravenous infusion. Cancer Research, 41(4), 1402-1406.