7-Hydroxymethotrexate as a urinary metabolite in human subjects and rhesus monkeys receiving high dose methotrexate.

AUTOR(ES)

Jacobs, S A

RESUMO

Human subjects and rhesus monkeys receiving the antitumor agent methotrexate at the high dose levels recently introduced into clinical use (greater than 50 mg/kg) excrete significant amounts of the metabolite 7-hydroxymethotrexate. The metabolite is not detected in these species after methotrexate therapy at conventional dose levels. The evidence indicates that in primates, the in vivo conversion of methotrexate to 7-hydroxymethotrexate is a dose-dependent phenomenon, with the enzyme system(s) catalyzing the reaction having a low affinity for the drug.

Documentos Relacionados

• Accumulation of methotrexate polyglutamates in lymphoblasts is a determinant of antileukemic effects in vivo. A rationale for high-dose methotrexate.
• Fatal varicella zoster infection in a severe steroid dependent asthmatic patient receiving methotrexate.
• Acute fever and delayed leukoencephalopathy following low dose intraventricular methotrexate.
• Folate supplementation and methotrexate.
• Polyglutamation of methotrexate. Is methotrexate a prodrug?