Methotrexate (MTX) concentration in tumors following low-dose MTX

Naomi J. Winick, Barton A. Kamen, Anita Streckfuss, Johnny Craig, Fred McGuirt, Robert L. Capizzi, Frederick Sklar, Dale Coln

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


Methotrexate (MTX) is a folate analog competitive with reduced folates for cellular transport and metabolism. Since the normal plasma folate concentration is only 10-8M, we tested the possibility that there may be a saturable uptake of MTX by proliferating tumor tissue at plasma MTX concentrations of only 10-7 to 10-6M. Patients with advanced malignancies, refractory to accepted therapy, were given low-dose oral MTX (30-60 mg/m2 total dose in four to eight divided doses). Tumor tissue was biopsied 18-24 h after the last oral dose of MTX. The concentrations of MTX and its polyglutamated derivatives were measured in these samples. Forty-eight percent of the drug in the tumor samples was present as a polyglutamated derivative.

Original languageEnglish (US)
Pages (from-to)78-80
Number of pages3
JournalCancer Chemotherapy and Pharmacology
Issue number1
StatePublished - Aug 1 1987

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)


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