Table 1 Established antifolate antineoplastic agents

From: One-carbon metabolism in cancer

Drug name

Targets

Therapeutic uses

Aminopterin

DHFR

Initially found to reduce leukaemic cells in children; no longer in use

Methotrexate

DHFR

Used to treat a wide range of neoplastic disease

Pemetrexed

DHFR, TYMS (and SHMT; Daidone et al, 2011)

Non-small cell lung carcinoma; pleural mesothelioma

Pralatrexate

DHFR

Peripheral T-cell lymphoma

Raltitrexed

DHFR and TYMS

Metastatic colorectal cancer

5-Fluoruoracil

TYMS

Used to treat a wide range of neoplastic disease

  1. Abbreviations: DHFR=dihydrofolate reductase; SHMT=serine hydroxymethyltransferase; TYMS=thymidylate synthase.
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