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Trimetrexate: a new antifol entering clinical trials

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Summary

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.

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O'Dwyer, P.J., Shoemaker, D.D., Plowman, J. et al. Trimetrexate: a new antifol entering clinical trials. Invest New Drugs 3, 71–75 (1985). https://doi.org/10.1007/BF00176828

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