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Folic Acid Antagonists

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Definition: Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)  DF: FOLIC ACID ANTAG    Other names Antifolates; Antagonists, Folic Acid; Acid Antagonists, Folic
Substances having this pharmacologic action: piritrexim; cycloguanil; CB 3717; brodimoprim; edatrexate; 3',5'-dichloromethotrexate; BRL 6231; methodichlorophen; Pyrimethamine; Trimetrexate; Trimethoprim; Methotrexate; Aminopterin; Dapsone; 7-hydroxymethotrexate; triazinate; 2,4-diamino-5-adamantyl-6-methylpyrimidine; 10-deazaaminopterin; iclaprim; nolatrexed; 1843U89; pemetrexed; raltitrexed; ICI 198583; lometrexol
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
10-propargyl-10-deazaaminopterin  0   Aminopterin/*analogs & derivatives Folic Acid Antagonists. Clin Cancer Res 2000 Sep;6(9):3493-8FOLOTYN
bastadin 14  146345-73-5   *Peptides, Cyclic *Halogenated Diphenyl Ethers DNA Topoisomerases, Type II/antagonists & inhibitors Folic Acid Antagonists. J Nat Prod 1993 Jan;56(1):153-7

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012

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