The role of 7-hydroxymethotrexate during methotrexate anti-cancer therapy.
Plasma concentrations of 7-hydroxymethotrexate were measured in 10 individuals receiving methotrexate, 8 of them per infusion. After the end of infusion, the plasma concentration of formed 7-hydroxymethotrexate fell less rapidly than that of methotrexate. At 24 h after infusion, plasma concentration ratios of 7-hydroxymethotrexate ranged from 30 to 1 (n = 8). The presence of 7-hydroxymethotrexate was shown to influence the transport of methotrexate into Ehrlich ascites tumor cells and human KB cells, cultured in vitro. These findings suggest that monitoring of 7-OHMTX is important in MTX treatment.
D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism; D002294:Carcinoma, Squamous Cell / Q000378:metabolism; D002478:Cells, Cultured / Q000187:drug effects; D005493:Folic Acid Antagonists / Q000097:blood*; D006207:Half-Life; D006801:Humans; D006900:Hydroxylation; D007263:Infusions, Parenteral; D007275:Injections, Intravenous; D008727:Methotrexate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood* / Q000627:therapeutic use*; D009369:Neoplasms / Q000188:drug therapy*
D005493:Folic Acid Antagonists; C011864:7-hydroxymethotrexate; D008727:Methotrexate