Folic Acid Antagonists

Name
Folic Acid Antagonists
Accession Number
DBCAT000523  (DBCAT003298, DBCAT003350, DBCAT003375)
Description

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)

Drugs
DrugDrug Description
PyrimethamineAn antiparasitic drug used in the prevention and treatment of toxoplasmosis and malaria.
DapsoneA sulfone drug used to treat acne vulgaris, Hansen's disease, and dermatitis herpetiformis.
RaltitrexedA folate analog thymidylate synthase inhibitor used in the treatment of advanced colorectal cancer.
TrimetrexateA folate antagonist used for the treatment of moderate-to-severe Pneumocystis carinii pneumonia (PCP) in immunocompromised patients as an alternative therapy in combination with leucovorin.
MetoprineNot Available
IclaprimInvestigated for use/treatment in bacterial infection, skin infections/disorders, obesity, liver disease, kidney disease, and pneumonia.
AminopterinPrior to its withdrawal, aminopterin was initially used in the treatment of childhood leukemia; specifically to induce remissions. Later, aminopterin was used off-label in the United States to treat psoriasis,...
LometrexolLometrexol has been used in trials studying the treatment of Lung Cancer, Drug/Agent Toxicity by Tissue/Organ, and Unspecified Adult Solid Tumor, Protocol Specific.
NolatrexedNolatrexed is under investigation in clinical trial NCT00012324 (Nolatrexed Dihydrochloride Compared With Doxorubicin in Treating Patients With Recurrent or Unresectable Liver Cancer).
BrodimoprimNot Annotated
TrimethoprimAn antifolate antibiotic often used in combination with sulfamethoxazole to treat a number of infections, including those of the urinary tract, respiratory tract, and gastrointestinal tract.
MethotrexateAn antineoplastic agent used the treatment of a wide variety of cancers as well as severe psoriasis, severe rheumatoid arthritis, and juvenile rheumatoid arthritis.
PemetrexedA folate analog used to treat mesothelioma and non-small cell lung cancer.
PralatrexateAn antineoplastic agent used for the treatment of relapsed or refractory peripheral T-cell lymphoma.
ProguanilA medication indicated for prophylaxis and treatment of Plasmodium falciparum malaria.
PiritreximPiritrexim has been used in trials studying the treatment of Bladder Cancer, Urethral Cancer, and Transitional Cell Cancer of the Renal Pelvis and Ureter.
CycloguanilCycloguanil is the active metabolite of proguanil.
5'-S-methyl-5'-thioadenosineNot Available
Drugs & Drug Targets
DrugTargetType
PyrimethamineBifunctional dihydrofolate reductase-thymidylate synthasetarget
PyrimethamineDihydrofolate reductasetarget
PyrimethamineCytochrome P450 2C8enzyme
PyrimethamineBeta-hexosaminidase subunit betatarget
PyrimethamineMultidrug and toxin extrusion protein 1transporter
PyrimethamineMultidrug and toxin extrusion protein 2transporter
DapsoneInactive dihydropteroate synthase 2target
DapsoneDihydropteroate synthase 1target
DapsoneCytochrome P450 2C9enzyme
DapsoneCytochrome P450 2E1enzyme
DapsoneCytochrome P450 3A4enzyme
DapsoneDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DapsoneProstaglandin G/H synthase 1enzyme
DapsoneProstaglandin G/H synthase 2enzyme
DapsoneCytochrome P450 2C8enzyme
DapsoneCytochrome P450 2C19enzyme
DapsoneArylamine N-acetyltransferase 2enzyme
DapsoneCytochrome P450 3A5enzyme
DapsoneCytochrome P450 3A7enzyme
DapsoneMyeloperoxidaseenzyme
DapsoneCytochrome P450 2C18enzyme
RaltitrexedThymidylate synthasetarget
RaltitrexedFolylpolyglutamate synthase, mitochondrialtarget
TrimetrexateDihydrofolate reductasetarget
TrimetrexateDihydrofolate reductaseenzyme
TrimetrexateFolate transporter 1transporter
MetoprineHistamine N-methyltransferasetarget
IclaprimDihydrofolate reductasetarget
AminopterinProton-coupled folate transportertransporter
AminopterinDihydrofolate reductaseenzyme
LometrexolDihydrofolate reductasetarget
TrimethoprimDihydrofolate reductasetarget
TrimethoprimCytochrome P450 2C8enzyme
TrimethoprimCytochrome P450 3A4enzyme
TrimethoprimP-glycoprotein 1transporter
TrimethoprimCytochrome P450 2C9enzyme
TrimethoprimCytochrome P450 1A2enzyme
TrimethoprimMultidrug and toxin extrusion protein 1transporter
TrimethoprimMultidrug and toxin extrusion protein 2transporter
MethotrexateDihydrofolate reductasetarget
MethotrexateAldehyde oxidaseenzyme
MethotrexateMethylenetetrahydrofolate reductaseenzyme
MethotrexateSerum albumincarrier
MethotrexateCanalicular multispecific organic anion transporter 2transporter
MethotrexateMultidrug resistance-associated protein 4transporter
MethotrexateMultidrug resistance-associated protein 1transporter
MethotrexateSolute carrier family 22 member 6transporter
MethotrexateMultidrug resistance-associated protein 7transporter
MethotrexateSolute carrier family 22 member 8transporter
MethotrexateCanalicular multispecific organic anion transporter 1transporter
MethotrexateP-glycoprotein 1transporter
MethotrexateSolute carrier organic anion transporter family member 1A2transporter
MethotrexateMonocarboxylate transporter 1transporter
MethotrexateATP-binding cassette sub-family C member 11transporter
MethotrexateSolute carrier organic anion transporter family member 1B3transporter
MethotrexateSolute carrier family 22 member 11transporter
MethotrexateSolute carrier organic anion transporter family member 1C1transporter
MethotrexateSolute carrier organic anion transporter family member 3A1transporter
MethotrexateATP-binding cassette sub-family G member 2transporter
MethotrexateSolute carrier family 22 member 7transporter
MethotrexateSolute carrier organic anion transporter family member 1B1transporter
Methotrexate6-phosphogluconate dehydrogenase, decarboxylatingenzyme
MethotrexateProton-coupled folate transportertransporter
MethotrexateFolylpolyglutamate synthase, mitochondrialenzyme
MethotrexateGamma-glutamyl hydrolaseenzyme
MethotrexateDihydrofolate reductaseenzyme
MethotrexateThymidylate synthaseenzyme
MethotrexateBifunctional purine biosynthesis protein PURHenzyme
MethotrexateSolute carrier organic anion transporter family member 4C1transporter
MethotrexateFolate transporter 1transporter
MethotrexateFolate receptor alphatransporter
MethotrexateCytochrome P450 3A4enzyme
MethotrexateThymidylate synthasetarget
MethotrexateBifunctional purine biosynthesis protein PURHtarget
MethotrexateFolate receptor betatransporter
MethotrexateSolute carrier family 15 member 1transporter
MethotrexateProton-coupled amino acid transporter 1transporter
PemetrexedThymidylate synthasetarget
PemetrexedDihydrofolate reductasetarget
PemetrexedTrifunctional purine biosynthetic protein adenosine-3target
PemetrexedDeoxycytidine kinaseenzyme
PemetrexedBifunctional purine biosynthesis protein PURHtarget
PemetrexedEquilibrative nucleoside transporter 1enzyme
PemetrexedSolute carrier family 22 member 8transporter
PralatrexateFolylpolyglutamate synthase, mitochondrialenzyme
PralatrexateDihydrofolate reductasetarget
PralatrexateThymidylate synthasetarget
PralatrexateFolate transporter 1transporter
PralatrexateCanalicular multispecific organic anion transporter 1transporter
PralatrexateATP-binding cassette sub-family G member 2transporter
ProguanilBifunctional dihydrofolate reductase-thymidylate synthasetarget
ProguanilDihydrofolate reductasetarget
ProguanilCytochrome P450 2C19enzyme
ProguanilCytochrome P450 2D6enzyme
ProguanilCytochrome P450 2C9enzyme
PiritreximDihydrofolate reductasetarget
5'-S-methyl-5'-thioadenosineModification methylase RsrItarget
5'-S-methyl-5'-thioadenosineS-methyl-5'-thioadenosine phosphorylasetarget