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Table 4-1

Antifolate Medications, Oncologic Use, and Differences in Structures as Compared to Folic Acid

Folic Acid
DRUGTARGETCOMMON ONCOLOGIC USESCHEMICAL STRUCTURE
Methotrexate (MTX)DHFRHigh dose: ALL, NHL, osteosarcoma
Low dose: various; including breast, CTCL, ALL maintenance, etc.
Pemetrexed (PMX)DHFR, TS, GARFT, AIRCARFTNonsquamous NSCLC, mesothelioma
Pralatrexate (PDX)DHFRPTCL

AIRCARFT, aminoimidazole carboxamide ribonucleotide formyltransferase; ALL, acute lymphocytic leukemia; CTCL, cutaneous T-cell lymphoma; DHFR, dihydrofolate reductase; GARFT, glycinamide ribonucleotide formyltransferase; MTX, methotrexate; NHL, non-Hodgkin lymphoma; NSCLC, non-small cell lung cancer; PTCL, peripheral T-cell lymphoma; TS, thymidylate synthase.