Trimetrexate: a new antifol entering clinical trials.
Trimetrexate, a 2,4-diaminoquinazoline derivative, is a new antifol recently introduced into clinical trials. It differs from methotrexate principally in its transport (not carrier-mediated), and its intracellular retention (not polyglutamylated). Trimetrexate is active against tumors which are methotrexate-resistant on the basis of impaired transport, and has a broader range of antitumor activity in preclinical models. Animal studies predict toxicity principally to the central nervous system, gastrointestinal tract and bone marrow.
O'Dwyer
P J
PJ
Shoemaker
D D
DD
Plowman
J
J
Cradock
J
J
Grillo-Lopez
A
A
Leyland-Jones
B
B
D000818:Animals; D001682:Biological Availability; D001692:Biological Transport; D002478:Cells, Cultured; D002986:Clinical Trials as Topic; D004247:DNA / Q000096:biosynthesis; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D005493:Folic Acid Antagonists / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009705:Nucleosides / Q000378:metabolism; D011799:Quinazolines / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D016597:Trimetrexate
D005493:Folic Acid Antagonists; D009705:Nucleosides; D011799:Quinazolines; D004247:DNA; D016597:Trimetrexate