The pyrimethamine (5- (4-chlorophenyl)-6-ethyl- 24-pyrimidinediamine) is a well reported antifolate drug
which has been utilized against malaria to target DHFR protein.
The antifolate drug
pemetrexed proved effective in patients with adenocarcinoma but not patients with squamous cell carcinoma.
In a pharmacogenetic context, inheritance of an MTHFR 677T-1298A haplotype and an MTHFDI 1958A allele was associated with a lower probability of event-free survival in children treated with the antifolate drug
methotrexate for acute lymphoblastic leukemia, particularly when in combination with the thymidylate synthase triple repeat associated with increased thymidylate synthase concentrations (24).
The synthesis of novel nucleoside transport inhibitors will allow for the antifolate drug
effectiveness to be maximized through in vitro and eventually in vivo studies.
Methotrexate (MTX) is an antifolate drug
that inhibits dihydrofolate reductase, thereby depleting the cells of reduced folates, including 5-methyltetrahydrofolate (5).
Rapid genotyping of loci involved in antifolate drug
resistance in Plasmodium falciparum by primer extension.
Co-trimoxazole, the antifolate drug
combination of trimethoprim and sulfamethoxazole, is the drug of choice for the prophylaxis and treatment of Pneumocystis carinii pneumonia (PCP), a life-threatening disease in immunosuppressed patients.