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. 2020 Dec 11;58(2):158–170. doi: 10.3892/ijo.2020.5158

Table I.

Antimetabolite drugs for the treatment of various types of cancer.

Drug name Targets Therapeutic uses Refs.
Methotrexate DHFR Used to treat multiple cancers (131)
Pemetrexed DHFR, TYMS and SHMT Used to treat multiple cancers, especially non-small cell lung carcinoma and pleural mesothelioma (131)
Pralatrexate DHFR Peripheral T-cell lymphoma (125)
Raltitrexed DHFR and TYMS Metastatic colorectal cancer (126)
5-FU TYMS Used to treat multiple cancers, especially colorectal cancer (127)
Gemcitabine Ribonucleotide reductase Used to treat multiple cancers, especially pancreatic cancer (128)
Cytarabine Ribonucleotide reductase Acute leukemia (129)
Azanucleotides DNA methyltransferases Myeloid leukemia (130)
DMFO Ornithine decaroboxylase Clinical trial (133)
SAM analogues Histone methyltransferases Clinical trial (134)
MGBG and SMA486A S-adenosyl decaroboxylase Preclinical studies (134)

5-FU, 5-fluoruoracil; DHFR, dihydrofolate reductase; TYMS, thymidylate synthase; SHMT, serine hydroxymethyltransferase; DMFO, 2-diflu-oromethyl orinithine; MGBG, methylglyoxal bis (guanylhydrazone); SMA486A, (E)-2-(4-carbamimidoyl-2,3-dihydro-1H-inden-1-ylidene) hydrazinecarboximidamide.