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

doi:10.1007/BF00252965

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

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Abstract

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 language	English (US)
Pages (from-to)	78-80
Number of pages	3
Journal	Cancer Chemotherapy and Pharmacology
Volume	20
Issue number	1
DOIs	https://doi.org/10.1007/BF00252965
State	Published - Aug 1 1987

ASJC Scopus subject areas

Oncology
Toxicology
Pharmacology
Cancer Research
Pharmacology (medical)

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abstract = "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.",

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AU - Winick, Naomi J.

AU - Kamen, Barton A.

AU - Streckfuss, Anita

AU - Craig, Johnny

AU - McGuirt, Fred

AU - Capizzi, Robert L.

AU - Sklar, Frederick

AU - Coln, Dale

PY - 1987/8/1

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AB - 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.

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

Abstract

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