Compounds based on 2-amino-4-hydroxypteridine.
DrugDrug NameDrug Indication
DB00116Tetrahydrofolic acidFor nutritional supplementation, also for treating dietary shortage or imbalance.
DB00158Folic AcidFor treatment of folic acid deficiency, megaloblastic anemia and in anemias of nutritional supplements, pregnancy, infancy, or childhood.
DB00360SapropterinFor the treatment of tetrahydrobiopterin (BH4) deficiency.
DB00563MethotrexateMethotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole. In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate is also indicated in the treatment of meningeal leukemia. Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas. Methotrexate is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis. Methotrexate is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis.
DB00650LeucovorinFor the treatment of osteosarcoma (after high dose methotrexate therapy). Used to diminish the toxicity and counteract the effects of impaired methotrexate elimination and of inadvertent overdosages of folic acid antagonists, and to treat megaloblastic anemias due to folic acid deficiency. Also used in combination with 5-fluorouracil to prolong survival in the palliative treatment of patients with advanced colorectal cancer.
DB02385D-threo-neopterinNot Available
DB03886BiopterinNot Available
DB04400L-erythro-7,8-dihydrobiopterinNot Available
DB044257,8-DihydroneopterinNot Available
DB047895-methyltetrahydrofolic acidNot Available
DB05168VintafolideInvestigated for use/treatment in solid tumors.
DB06813PralatrexateTreatment of relapsed or refractory peripheral T-cell lymphoma.
DB08878AminopterinPrior 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, yielding dramatic lesion clearing. Aminopterin was later supplanted by methotrexate for treating cancer because of its better therapeutic index. Aminopterin (as well as methotrexate) has also been explored for use as an abortifacient. However, their association with severe congenital malformations and teratogenic effects have become known as fetal aminopterin syndrome.
DB11596LevoleucovorinLevoleucovorin is indicated for use as rescue therapy following high-dose methotrexate in the treatment of osteosarcoma or for diminishing the toxicity associated with inadvertent overdosage of folic acid antagonists. Levoleucovorin, as the product Fusilev (FDA, dosed at one-half the usual dose of racemic d,l-leucovorin), has an additional indication for use in combination chemotherapy with 5-fluorouracil in the palliative treatment of patients with advanced metastatic colorectal cancer (although they should not be mixed in the same infusion as a precipitate may form).
DB12266EpofolateNot Available
DB12575RonopterinNot Available
DB12769LometrexolNot Available
DrugDrug NameTargetType
DB00116Tetrahydrofolic acidC-1-tetrahydrofolate synthase, cytoplasmictarget
DB00116Tetrahydrofolic acidBifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase, mitochondrialtarget
DB00116Tetrahydrofolic acidAminomethyltransferase, mitochondrialtarget
DB00116Tetrahydrofolic acidCytosolic 10-formyltetrahydrofolate dehydrogenasetarget
DB00116Tetrahydrofolic acidMethionine synthasetarget
DB00116Tetrahydrofolic acidFormimidoyltransferase-cyclodeaminasetarget
DB00116Tetrahydrofolic acidBifunctional purine biosynthesis protein PURHtarget
DB00116Tetrahydrofolic acidSerine hydroxymethyltransferase, cytosolictarget
DB00116Tetrahydrofolic acidSerine hydroxymethyltransferase, mitochondrialtarget
DB00116Tetrahydrofolic acidMethylenetetrahydrofolate reductasetarget
DB00116Tetrahydrofolic acidSerine hydroxymethyltransferasetarget
DB00116Tetrahydrofolic acidMethionyl-tRNA formyltransferase, mitochondrialtarget
DB00116Tetrahydrofolic acidCanalicular multispecific organic anion transporter 1transporter
DB00158Folic AcidFolate receptor gammatarget
DB00158Folic AcidFolate receptor betatarget
DB00158Folic AcidMethylenetetrahydrofolate reductaseenzyme
DB00158Folic AcidMultidrug resistance-associated protein 4transporter
DB00158Folic AcidSolute carrier family 22 member 6transporter
DB00158Folic AcidCanalicular multispecific organic anion transporter 2transporter
DB00158Folic AcidATP-binding cassette sub-family C member 11transporter
DB00158Folic AcidATP-binding cassette sub-family G member 2transporter
DB00158Folic AcidCytochrome P450 2E1enzyme
DB00158Folic AcidProton-coupled folate transportertransporter
DB00158Folic AcidMitochondrial folate transporter/carriertransporter
DB00158Folic AcidGamma-glutamyl hydrolaseenzyme
DB00158Folic AcidSerum albumincarrier
DB00158Folic AcidFolate receptor alphatarget
DB00360SapropterinPhenylalanine-4-hydroxylasetarget
DB00360SapropterinNitric oxide synthase, endothelialtarget
DB00360SapropterinTyrosine 3-monooxygenasetarget
DB00360SapropterinTryptophan 5-hydroxylase 1target
DB00360SapropterinProstaglandin G/H synthase 2enzyme
DB00563MethotrexateDihydrofolate reductasetarget
DB00563MethotrexateAldehyde oxidaseenzyme
DB00563MethotrexateMethylenetetrahydrofolate reductaseenzyme
DB00563MethotrexateSerum albumincarrier
DB00563MethotrexateCanalicular multispecific organic anion transporter 2transporter
DB00563MethotrexateMultidrug resistance-associated protein 4transporter
DB00563MethotrexateMultidrug resistance-associated protein 1transporter
DB00563MethotrexateSolute carrier family 22 member 6transporter
DB00563MethotrexateMultidrug resistance-associated protein 7transporter
DB00563MethotrexateSolute carrier family 22 member 8transporter
DB00563MethotrexateCanalicular multispecific organic anion transporter 1transporter
DB00563MethotrexateMultidrug resistance protein 1transporter
DB00563MethotrexateSolute carrier organic anion transporter family member 1A2transporter
DB00563MethotrexateMonocarboxylate transporter 1transporter
DB00563MethotrexateATP-binding cassette sub-family C member 11transporter
DB00563MethotrexateSolute carrier organic anion transporter family member 1B3transporter
DB00563MethotrexateSolute carrier family 22 member 11transporter
DB00563MethotrexateSolute carrier organic anion transporter family member 1C1transporter
DB00563MethotrexateSolute carrier organic anion transporter family member 3A1transporter
DB00563MethotrexateATP-binding cassette sub-family G member 2transporter
DB00563MethotrexateSolute carrier family 22 member 7transporter
DB00563MethotrexateSolute carrier organic anion transporter family member 1B1transporter
DB00563Methotrexate6-phosphogluconate dehydrogenase, decarboxylatingenzyme
DB00563MethotrexateProton-coupled folate transportertransporter
DB00563MethotrexateFolylpolyglutamate synthase, mitochondrialenzyme
DB00563MethotrexateGamma-glutamyl hydrolaseenzyme
DB00563MethotrexateDihydrofolate reductaseenzyme
DB00563MethotrexateThymidylate synthaseenzyme
DB00563MethotrexateBifunctional purine biosynthesis protein PURHenzyme
DB00563MethotrexateSolute carrier organic anion transporter family member 4C1transporter
DB00563MethotrexateFolate transporter 1transporter
DB00563MethotrexateFolate receptor alphatransporter
DB03886BiopterinSepiapterin reductasetarget
DB03886Biopterin6-pyruvoyl tetrahydrobiopterin synthasetarget
DB03886BiopterinDihydrofolate reductasetarget
DB04400L-erythro-7,8-dihydrobiopterinPhenylalanine-4-hydroxylasetarget
DB04400L-erythro-7,8-dihydrobiopterinPteridine reductase 1target
DB04400L-erythro-7,8-dihydrobiopterinNitric oxide synthase, inducibletarget
DB04400L-erythro-7,8-dihydrobiopterinTyrosine 3-monooxygenasetarget
DB04400L-erythro-7,8-dihydrobiopterinPterin-4-alpha-carbinolamine dehydratasetarget
DB04400L-erythro-7,8-dihydrobiopterinDihydroneopterin aldolasetarget
DB044257,8-DihydroneopterinDihydroneopterin aldolasetarget
DB047895-methyltetrahydrofolic acidAminomethyltransferase, mitochondrialtarget
DB047895-methyltetrahydrofolic acidCanalicular multispecific organic anion transporter 1transporter
DB05168VintafolideFolate receptor betatarget
DB05168VintafolideFolate receptor gammatarget
DB05168VintafolideFolate receptor alphatarget
DB06813PralatrexateFolylpolyglutamate synthase, mitochondrialenzyme
DB06813PralatrexateDihydrofolate reductasetarget
DB06813PralatrexateThymidylate synthasetarget
DB06813PralatrexateFolate transporter 1transporter
DB08878AminopterinProton-coupled folate transportertransporter
DB08878AminopterinDihydrofolate reductaseenzyme
DB11596LevoleucovorinSerine hydroxymethyltransferasetarget
DB11596LevoleucovorinDihydrofolate reductasetarget
DB12769LometrexolDihydrofolate reductasetarget