Abstract: | Methotrexate (MTX), a potent folate antagonist by virtue of its ability to inhibit the enzyme dihydrofolate reductase 1], continues to be a useful cancer chemotherapeutic agent 2]. Information not only on its mechanism of action, but also its pharmacology has led to improved dosage schedules of this drug alone and in combination. The use of high (gm) doses of MTX followed by leucovorin “rescue” has required close attention to the blood levels of this drug and has stimulated further studies of its clinical pharmacology, especially of high-dose regimens. This review summarizes the present status of the clinical pharmacology of MTX. |