Identification

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Name
Folic acid
Accession Number
DB00158  (NUTR00025)
Type
Small Molecule
Groups
Approved, Nutraceutical, Vet approved
Description

Folic acid, also known as folate or Vitamin B9, is a member of the B vitamin family and an essential cofactor for enzymes involved in DNA and RNA synthesis. More specifically, folic acid is required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. Folic acid is particularly important during phases of rapid cell division, such as infancy, pregnancy, and erythropoiesis, and plays a protective factor in the development of cancer. As humans are unable to synthesize folic acid endogenously, diet and supplementation is necessary to prevent deficiencies. For example, folic acid is present in green vegetables, beans, avocado, and some fruits.9

In order to function within the body, folic acid must first be reduced by the enzyme dihydrofolate reductase (DHFR) into the cofactors dihydrofolate (DHF) and tetrahydrofolate (THF). This important pathway, which is required for de novo synthesis of nucleic acids and amino acids, is disrupted by anti-metabolite therapies such as Methotrexate as they function as DHFR inhibitors to prevent DNA synthesis in rapidly dividing cells, and therefore prevent the formation of DHF and THF. When used in high doses such as for cancer therapy, or in low doses such as for Rheumatoid Arthritis or psoriasis, Methotrexate impedes the body's ability to create folic acid. This results in a deficiency of coenzymes and a resultant buildup of toxic substances that are responsible for numerous adverse side effects. As a result, supplementation with 1-5mg of folic acid is recommended to prevent deficiency and a number of side effects associated with MTX therapy including mouth ulcers and gastrointestinal irritation. Leucovorin (also known as folinic acid) supplementation is typically used for high-dose MTX regimens for the treatment of cancer. Levoleucovorin and leucovorin are analogs of tetrahydrofolate (THF) and are able to bypass DHFR reduction to act as a cellular replacement for the co-factor THF.

There are also several antiepileptic drugs (AEDs) that are associated with reduced serum and red blood cell folate, including Carbamazepine (CBZ), Phenytoin (PHT), or barbiturates.7 Folic acid is therefore often provided as supplementation to individuals using these medications, particularly to women of child-bearing age.

Inadequate folate levels can result in a number of health concerns including cardiovascular disease, megaloblastic anemias, cognitive deficiencies, and neural tube defects (NTDs). Folic acid is typically supplemented during pregnancy to prevent the development of NTDs and in individuals with alcoholism to prevent the development of neurological disorders, for example.

Structure
Thumb
Synonyms
  • ácido fólico
  • Folacin
  • Folate
  • Folic acid
  • Folsäure
  • N-[(4-{[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino}phenyl)carbonyl]-L-glutamic acid
  • N-pteroyl-L-glutamic acid
  • PGA
  • PteGlu
  • Pteroyl-L-glutamate
  • Pteroyl-L-glutamic acid
  • Pteroyl-L-monoglutamic acid
  • Pteroylglutamic acid
  • Vitamin B9
  • Vitamin Bc
  • Vitamin M
External IDs
NSC-3073
Product Ingredients
IngredientUNIICASInChI Key
Folate sodium9P9W8GGU786484-89-5SWIRFWUEJODNRG-CURYUGHLSA-L
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acide Folique 5 TabTabletOralPro Doc Limitee1982-12-312010-07-13Canada
Folic AcidTablet1 mg/1OralWest Ward Pharmaceutical2007-05-28Not applicableUs
Folic AcidTablet1 mg/1OralMutual Pharmaceutical2006-09-20Not applicableUs
Folic AcidTablet5 mgOralAa Pharma Inc1978-12-31Not applicableCanada
Folic AcidTablet1 mg/1OralWatson Labs2006-04-07Not applicableUs
Folic AcidTablet1 mg/1OralApace Packaging2009-12-23Not applicableUs
Folic Acid Inj 5mg/ml USPLiquidIntramuscular; Intravenous; SubcutaneousLyphomed, Division Of Fujisawa Canada Inc.1993-12-311996-09-10Canada
Folic Acid InjectionSolutionIntramuscular; Intravenous; SubcutaneousFresenius Kabi1996-08-14Not applicableCanada
Folic Acid Injection USPLiquidIntramuscular; Intravenous; SubcutaneousSandoz Canada Incorporated1990-12-31Not applicableCanada
Folic Acid Tab 25mgTabletOralKripps Pharmacy Ltd.1975-12-31Not applicableCanada
Additional Data Available
  • Application Number
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    Product Code

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Folic AcidTablet1 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1972-03-312014-06-30Us
Folic AcidTablet1 mg/1Oralbryant ranch prepack2009-12-022018-05-29Us
Folic AcidTablet1 mg/1OralPreferreed Pharmaceuticals Inc.2012-04-30Not applicableUs68788 979520180913 8702 1kolkfg
Folic AcidTablet1 mg/1OralPD-Rx Pharmaceuticals, Inc.2015-08-04Not applicableUs
Folic AcidTablet1 mg/1OralWest Ward Pharmaceutical2009-06-09Not applicableUs0143 971720180907 15195 1pe5bdz
Folic AcidTablet1 mg/1OralRemedy Repack2011-11-272014-04-02Us
Folic AcidTablet1 mg/1OralSt. Marys Medical Park Pharmacy2013-05-092015-08-31Us
Folic AcidTablet1 mg/1OralNucare Pharmaceuticals,inc.2015-03-01Not applicableUs
Folic AcidTablet1 mg/1OralContract Pharmacy Services Pa2010-11-09Not applicableUs
Folic AcidTablet1 mg/1OralRemedy Repack2012-08-162013-08-17Us
Additional Data Available
  • Application Number
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  • Product Code
    Product Code

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Folic AcidCapsule1 mgOralSisu Inc.1999-08-032006-07-31Canada
Folic Acid (1mg Tablet)TabletOralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1997-10-102002-07-31Canada
Folic Acid 0.4 Mg TabletTabletOralSwiss Herbal Remedies Ltd.1999-12-062007-07-31Canada
Folic Acid 0.4mgTabletOralGreat Earth Companies, Inc.1998-08-252002-10-02Canada
Folic Acid 0.4mg Dietary SupplementTabletOralGarden State Nutritionals1998-08-312000-06-07Canada
Folic Acid 0.8mgTabletOralGreat Earth Companies, Inc.1998-08-252002-10-02Canada
Folic Acid 1 mgTabletOralPreferred Nutrition Inc.2004-04-282005-08-04Canada
Folic Acid 1 Mg - TabletTabletOralHealth Wise Nutrition Inc.1996-10-222002-07-18Canada
Folic Acid 1mgTabletOralJamieson Laboratories Ltd1994-12-311997-08-13Canada
Folic Acid 1mgTabletOralWn Pharmaceuticals Ltd.2002-04-152006-08-08Canada
Additional Data Available
  • Application Number
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  • Product Code
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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
24 Multivitamins + MineralsFolic acid (.8 mg) + Ascorbic acid (150 mg) + Beta carotene (10000 unit) + Biotin (25 mcg) + Calcium (130 mg) + Cholecalciferol (400 unit) + Choline bitartrate (25 mg) + Chromium (20 mcg) + Copper (1 mg) + Cyanocobalamin (25 mcg) + Ferrous fumarate (15 mg) + Inositol (25 mg) + Magnesium (65 mg) + Manganese (2 mg) + Molybdenum (20 mcg) + Niacin (25 mg) + Calcium pantothenate (25 mg) + Potassium (15 mg) + Potassium Iodide (.1 mg) + Pyridoxine hydrochloride (25 mg) + Racemethionine (25 mg) + Riboflavin (25 mg) + Selenium (20 mcg) + Thiamine hydrochloride (25 mg) + Vanadium (20 mcg) + Vitamin A palmitate (5000 unit) + Vitamin E (50 unit) + Zinc (10 mg)TabletOralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1997-04-302002-07-31Canada
50 PlusFolic acid (.2 mg) + Ascorbic acid (200 mg) + Biotin (20 mcg) + Choline bitartrate (20 mg) + Cyanocobalamin (20 mcg) + Inositol (20 mg) + Niacin (20 mg) + Calcium pantothenate (20 mg) + Pyridoxine hydrochloride (20 mg) + Racemethionine (20 mg) + Riboflavin (20 mg) + Thiamine hydrochloride (20 mg) + Vitamin A palmitate (10000 unit) + Vitamin D (400 unit) + Vitamin E (20 unit)TabletOralQuest Vitamins A Div Of Purity Life Health Products1998-08-042001-07-06Canada
50 Plus Multiple Vitamins & MineralsFolic acid (0.4 mg) + Ascorbic acid (90 mg) + Biotin (45 mcg) + Calcium (200 mg) + Cholecalciferol (400 unit) + Chromium (10 mcg) + Copper (2 mg) + Cyanocobalamin (25 mcg) + Magnesium (100 mg) + Manganese (5 mg) + Molybdenum (25 mcg) + Nicotinamide (40 mg) + Pantothenic acid (10 mg) + Potassium Iodide (0.15 mg) + Pyridoxine hydrochloride (3 mg) + Riboflavin (3.2 mg) + Selenium (25 mcg) + Thiamine mononitrate (2.25 mg) + Vanadium (10 mcg) + Vitamin A palmitate (6000 unit) + Zinc (15 mg)TabletOralGfr Pharma Ltd.2002-10-202004-06-15Canada
A.R.T.H. Away FormulaFolic acid (0.025 mg) + Calcium (24 mg) + Cholecalciferol (45 unit) + Copper (0.232 mg) + Manganese (0.58 mg) + Pyridoxine hydrochloride (0.5 mg) + Selenium (1.54 mcg) + Zinc (0.63 mg)CapsuleOralAbundance Naturally Ltd1999-02-012006-06-16Canada
A/o-26 - CapletFolic acid (.4 mg) + Beta carotene (7500 unit) + Calcium (75 mg) + Calcium ascorbate (250 mg) + Copper (1 mg) + DL-alpha tocopheryl acetate (100 unit) + Manganese (2.5 mg) + Racemethionine (50 mg) + Selenium (100 mcg) + Zinc (7.5 mg)TabletOralEnviro Tech International Canada1996-12-191999-07-26Canada
Acti-folic + Dibencozide CapletsFolic acid (1 mg) + Cobamamide (40 mcg)TabletOralActi Form Ltd.1991-12-312005-03-21Canada
Adult Formula 50+Folic acid (0.4 mg) + Ascorbic acid (120 mg) + Beta carotene (3000 unit) + Biotin (30 mcg) + Calcium (220 mg) + Cholecalciferol (400 unit) + Chromium (10 mcg) + Copper (2 mg) + Cyanocobalamin (25 mcg) + Iodine (0.15 mg) + Magnesium (100 mg) + Manganese (2.5 mg) + Molybdenum (10 mcg) + Nicotinamide (20 mg) + Calcium pantothenate (20 mg) + Potassium (37.5 mg) + Pyridoxine hydrochloride (6 mg) + Riboflavin (3.4 mg) + Selenium (10 mcg) + Thiamine hydrochloride (4.5 mg) + Vitamin A palmitate (3000 unit) + Zinc (15 mg) + alpha-Tocopherol acetate (60 unit)TabletOralWn Pharmaceuticals Ltd.2002-04-252009-09-28Canada
Adult Infuvite Multiple VitaminsFolic acid (600 ug/10mL) + Ascorbic acid (200 mg/10mL) + Biotin (60 ug/10mL) + Cholecalciferol (200 [iU]/10mL) + Cyanocobalamin (5 ug/10mL) + Dexpanthenol (15 mg/10mL) + Riboflavin 5'-phosphate sodium (3.6 mg/10mL) + Nicotinamide (40 mg/10mL) + Phylloquinone (150 ug/10mL) + Pyridoxine hydrochloride (6 mg/10mL) + Thiamine hydrochloride (6 mg/10mL) + Vitamin A palmitate (3300 [iU]/10mL) + alpha-Tocopherol acetate (10 [iU]/10mL)Injection, solutionIntravenousSandoz Inc2005-05-18Not applicableUs
Adult Infuvite Multiple VitaminsFolic acid (600 ug/10mL) + Ascorbic acid (200 mg/10mL) + Biotin (60 ug/10mL) + Cholecalciferol (200 [iU]/10mL) + Cyanocobalamin (5 ug/10mL) + Dexpanthenol (15 mg/10mL) + Riboflavin 5'-phosphate sodium (3.6 mg/10mL) + Nicotinamide (40 mg/10mL) + Phylloquinone (150 ug/10mL) + Pyridoxine hydrochloride (6 mg/10mL) + Thiamine hydrochloride (6 mg/10mL) + Vitamin A palmitate (3300 [iU]/10mL) + alpha-Tocopherol acetate (10 [iU]/10mL)Injection, solutionIntravenousSandoz Inc2003-06-16Not applicableUs
Adult Infuvite Multiple VitaminsFolic acid (600 ug/10mL) + Ascorbic acid (200 mg/10mL) + Biotin (60 ug/10mL) + Cholecalciferol (200 [iU]/10mL) + Cyanocobalamin (5 ug/10mL) + Dexpanthenol (15 mg/10mL) + Riboflavin 5'-phosphate sodium (3.6 mg/10mL) + Nicotinamide (40 mg/10mL) + Phylloquinone (150 ug/10mL) + Pyridoxine hydrochloride (6 mg/10mL) + Thiamine hydrochloride (6 mg/10mL) + Vitamin A palmitate (3300 [iU]/10mL) + alpha-Tocopherol acetate (10 [iU]/10mL)Injection, solutionIntravenousSandoz Inc2003-06-16Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Active FEFolic acid (1250 ug/1) + Ascorbic acid (160 mg/1) + Beta carotene (2100 [iU]/1) + Cholecalciferol (400 [iU]/1) + Cupric oxide (1 mg/1) + Cyanocobalamin (30 ug/1) + DL-alpha tocopheryl acetate (40 [iU]/1) + Iron (75 mg/1) + Magnesium oxide (30 mg/1) + Nicotinamide (20 mg/1) + Pyridoxine hydrochloride (20 mg/1) + Riboflavin (4 mg/1) + Thiamine hydrochloride (4 mg/1) + Zinc oxide (20 mg/1)TabletOralGm Pharmaceuticals2013-11-11Not applicableUs
Active OBFolic acid (1 mg/1) + Ascorbic acid (100 mg/1) + Cholecalciferol (400 [iU]/1) + Cupric sulfate pentahydrate (2 mg/1) + Cyanocobalamin (30 ug/1) + D-alpha-Tocopherol acetate (30 [iU]/1) + Doconexent (320 mg/1) + Iron (20 mg/1) + Pyridoxine hydrochloride (20 mg/1) + Riboflavin (4 mg/1) + Thiamine mononitrate (2 mg/1) + Zinc oxide (30 mg/1)Capsule, liquid filledOralGm Pharmaceuticals2013-10-282017-03-31Us
Animi-3Folic acid (1 mg/1) + Cholecalciferol (1000 [iU]/1) + Cyanocobalamin (500 ug/1) + Doconexent (250 mg/1) + Icosapent (35 mg/1) + Omega-3 fatty acids (500 mg/1) + Pyridoxine hydrochloride (12.5 mg/1) + Soy sterol (200 mg/1)CapsuleOralPbm Pharmaceuticals Inc.2011-06-01Not applicableUs
Animi-3 with Vitamin DFolic acid (1 mg/1) + Cholecalciferol (1000 [iU]/1) + Cyanocobalamin (500 ug/1) + Doconexent (250 mg/1) + Icosapent (35 mg/1) + Omega-3 fatty acids (500 mg/1) + Pyridoxine hydrochloride (12.5 mg/1) + Soy sterol (200 mg/1)CapsuleOralPbm Pharmaceuticals Inc.2011-06-01Not applicableUs
Av-VITE FBFolic acid (2.5 mg/1) + Cyanocobalamin (1 mg/1) + Pyridoxine hydrochloride (25 mg/1)TabletOralAv Kare, Inc.2015-11-052016-01-13Us
B-NexaFolic acid (1.22 mg/1) + Calcium (124.23 mg/1) + Ginger (100 mg/1) + Pyridoxine (42 mg/1)TabletOralUpsher Smith Laboratories2012-08-152015-04-30Us
B-NexaFolic acid (1.2 mg/1) + Calcium (124.1 mg/1) + Ginger (100 mg/1) + Pyridoxine (40 mg/1)TabletOralUpsher Smith Laboratories2011-12-082014-02-28Us
BacminFolic acid (1 mg/1) + Ascorbic acid (500 mg/1) + Biotin (150 ug/1) + Chromium Cr-51 chloride (0.1 mg/1) + Cupric oxide (3 mg/1) + Cyanocobalamin (50 ug/1) + Ferrous fumarate (27 mg/1) + Flavone (50 mg/1) + Magnesium oxide (50 mg/1) + Manganese gluconate (5 mg/1) + Nicotinamide (100 mg/1) + Calcium pantothenate (25 mg/1) + Pyridoxine hydrochloride (25 mg/1) + Riboflavin (20 mg/1) + Selenomethionine (50 ug/1) + Thiamine mononitrate (20 mg/1) + Vitamin A acetate (2000 [iU]/1) + Zinc oxide (22.5 mg/1) + alpha-Tocopherol acetate (30 [iU]/1)Tablet, coatedOralMarnel Pharmaceuticals, Llc2000-04-01Not applicableUs
Bal-Care DHAFolic acid (1 mg/1) + Ascorbic acid (120 mg/1) + Beta carotene (2850 [iU]/1) + Calcium carbonate (219 mg/1) + Cholecalciferol (840 [iU]/1) + Cupric oxide (2 mg/1) + Cyanocobalamin (.012 mg/1) + DL-alpha tocopheryl acetate (3 mg/1) + Iodine (.223 mg/1) + Iron sucrose (1.35 mg/1) + Magnesium oxide (25 mg/1) + Nicotinamide (20 mg/1) + Omega-3 fatty acids (430 mg/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (4 mg/1) + Sodium feredetate (25.65 mg/1) + Thiamine mononitrate (1.8 mg/1) + Zinc oxide (25 mg/1)KitOralPru Gen Pharmaceuticals2012-05-01Not applicableUs
Bal-Care DHA EssentialFolic acid (1 mg/1) + Ascorbic acid (120 mg/1) + Beta carotene (2850 [iU]/1) + Calcium carbonate (219 mg/1) + Cholecalciferol (840 [iU]/1) + Cupric oxide (2 mg/1) + Cyanocobalamin (.012 mg/1) + DL-alpha tocopheryl acetate (3 mg/1) + Iodine (.223 mg/1) + Iron sucrose (1.35 mg/1) + Magnesium oxide (25 mg/1) + Nicotinamide (20 mg/1) + Omega-3 fatty acids (374 mg/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (4 mg/1) + Sodium feredetate (25.65 mg/1) + Thiamine mononitrate (1.8 mg/1) + Zinc oxide (25 mg/1)KitOralPru Gen Pharmaceuticals2012-05-01Not applicableUs
International/Other Brands
Acfol (Cazi) / Fefol (GlaxoSmithKline)
Categories
UNII
935E97BOY8
CAS number
59-30-3
Weight
Average: 441.3975
Monoisotopic: 441.139681375
Chemical Formula
C19H19N7O6
InChI Key
OVBPIULPVIDEAO-LBPRGKRZSA-N
InChI
InChI=1S/C19H19N7O6/c20-19-25-15-14(17(30)26-19)23-11(8-22-15)7-21-10-3-1-9(2-4-10)16(29)24-12(18(31)32)5-6-13(27)28/h1-4,8,12,21H,5-7H2,(H,24,29)(H,27,28)(H,31,32)(H3,20,22,25,26,30)/t12-/m0/s1
IUPAC Name
(2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino}phenyl)formamido]pentanedioic acid
SMILES
NC1=NC(=O)C2=NC(CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)=CN=C2N1

Pharmacology

Indication

Folic acid is indicated for the treatment of folic acid deficiency, megaloblastic anemia, and in anemias of nutritional origins, pregnancy, infancy, or childhood.

Associated Conditions
Pharmacodynamics

Folic acid is a water-soluble B-complex vitamin found in foods such as liver, kidney, yeast, and leafy, green vegetables. Also known as folate or Vitamin B9, folic acid is an essential cofactor for enzymes involved in DNA and RNA synthesis. More specifically, folic acid is required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. Folic acid is the precursor of tetrahydrofolic acid, which is involved as a cofactor for transformylation reactions in the biosynthesis of purines and thymidylates of nucleic acids. Impairment of thymidylate synthesis in patients with folic acid deficiency is thought to account for the defective deoxyribonucleic acid (DNA) synthesis that leads to megaloblast formation and megaloblastic and macrocytic anemias. Folic acid is particularly important during phases of rapid cell division, such as infancy, pregnancy, and erythropoiesis, and plays a protective factor in the development of cancer. As humans are unable to synthesize folic acid endogenously, diet and supplementation is necessary to prevent deficiencies. In order to function properly within the body, folic acid must first be reduced by the enzyme dihydrofolate reductase (DHFR) into the cofactors dihydrofolate (DHF) and tetrahydrofolate (THF). This important pathway, which is required for de novo synthesis of nucleic acids and amino acids, is disrupted by anti-metabolite therapies such as Methotrexate as they function as DHFR inhibitors to prevent DNA synthesis in rapidly dividing cells, and therefore prevent the formation of DHF and THF.

In general, folate serum levels below 5 ng/mL indicate folate deficiency, and levels below 2 ng/mL usually result in megaloblastic anemia.

Mechanism of action

Folic acid, as it is biochemically inactive, is converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase (DHFR). These folic acid congeners are transported across cells by receptor-mediated endocytosis where they are needed to maintain normal erythropoiesis, synthesize purine and thymidylate nucleic acids, interconvert amino acids, methylate tRNA, and generate and use formate. Using vitamin B12 as a cofactor, folic acid can normalize high homocysteine levels by remethylation of homocysteine to methionine via methionine synthetase.

TargetActionsOrganism
UFolate receptor gamma
binder
Humans
UFolate receptor beta
binder
Humans
UFolate receptor alphaNot AvailableHumans
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Absorption

Folic acid is absorbed rapidly from the small intestine, primarily from the proximal portion. Naturally occurring conjugated folates are reduced enzymatically to folic acid in the gastrointestinal tract prior to absorption. Folic acid appears in the plasma approximately 15 to 30 minutes after an oral dose; peak levels are generally reached within 1 hour.Label

Volume of distribution

Tetrahydrofolic acid derivatives are distributed to all body tissues but are stored primarily in the liver.

Protein binding

Very high to plasma protein

Metabolism

Folic acid is metabolized in the liver into the cofactors dihydrofolate (DHF) and tetrahydrofolate (THF) by the enzyme dihydrofolate reductase (DHFR).

Route of elimination

After a single oral dose of 100 mcg of folic acid in a limited number of normal adults, only a trace amount of the drug appeared in the urine. An oral dose of 5 mg in 1 study and a dose of 40 mcg/kg of body weight in another study resulted in approximately 50% of the dose appearing in the urine. After a single oral dose of 15 mg, up to 90% of the dose was recovered in the urine. A majority of the metabolic products appeared in the urine after 6 hours; excretion was generally complete within 24 hours. Small amounts of orally administered folic acid have also been recovered in the feces. Folic acid is also excreted in the milk of lactating mothers.

Half life
Not Available
Clearance
Not Available
Toxicity

IPR-MUS LD50 85 mg/kg,IVN-GPG LD50 120 mg/kg, IVN-MUS LD50 239 mg/kg, IVN-RAT LD50 500 mg/kg, IVN-RBT LD50 410 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Methylenetetrahydrofolate Reductase Deficiency (MTHFRD)Disease
Folate MetabolismMetabolic
Methotrexate Action PathwayDrug action
Folate Malabsorption, HereditaryDisease
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
5-fluorouridineThe risk or severity of adverse effects can be increased when Folic acid is combined with 5-fluorouridine.
AbacavirFolic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbemaciclibAbemaciclib may decrease the excretion rate of Folic acid which could result in a higher serum level.
AcarboseFolic acid may decrease the excretion rate of Acarbose which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Folic acid which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Folic acid which could result in a higher serum level.
AcetaminophenFolic acid may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Folic acid which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Folic acid which could result in a higher serum level.
AclidiniumFolic acid may decrease the excretion rate of Aclidinium which could result in a higher serum level.
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Food Interactions
Not Available

References

Synthesis Reference

Carroll G. Temple, Jr., Robert D. Elliott, Jerry D. Rose, John A. Montgomery, "Preparation of tetrahydrofolic acid from folic acid." U.S. Patent US4206307, issued April, 1956.

US4206307
General References
  1. Kamen B: Folate and antifolate pharmacology. Semin Oncol. 1997 Oct;24(5 Suppl 18):S18-30-S18-39. [PubMed:9420019]
  2. Fenech M, Aitken C, Rinaldi J: Folate, vitamin B12, homocysteine status and DNA damage in young Australian adults. Carcinogenesis. 1998 Jul;19(7):1163-71. [PubMed:9683174]
  3. Zittoun J: [Anemias due to disorder of folate, vitamin B12 and transcobalamin metabolism]. Rev Prat. 1993 Jun 1;43(11):1358-63. [PubMed:8235383]
  4. Alaimo K, McDowell MA, Briefel RR, Bischof AM, Caughman CR, Loria CM, Johnson CL: Dietary intake of vitamins, minerals, and fiber of persons ages 2 months and over in the United States: Third National Health and Nutrition Examination Survey, Phase 1, 1988-91. Adv Data. 1994 Nov 14;(258):1-28. [PubMed:10138938]
  5. Raiten DJ, Fisher KD: Assessment of folate methodology used in the Third National Health and Nutrition Examination Survey (NHANES III, 1988-1994). J Nutr. 1995 May;125(5):1371S-1398S. [PubMed:7738698]
  6. Cylwik B, Chrostek L: [Disturbances of folic acid and homocysteine metabolism in alcohol abuse]. Pol Merkur Lekarski. 2011 Apr;30(178):295-9. [PubMed:21595178]
  7. Morrell MJ: Folic Acid and Epilepsy. Epilepsy Curr. 2002 Mar;2(2):31-34. doi: 10.1046/j.1535-7597.2002.00017.x. [PubMed:15309159]
  8. Scott JM, Weir DG, Molloy A, McPartlin J, Daly L, Kirke P: Folic acid metabolism and mechanisms of neural tube defects. Ciba Found Symp. 1994;181:180-7; discussion 187-91. [PubMed:8005024]
  9. Health Canada Prenatal Nutrition Guidelines for Health Professionals - Folate Contributes to a Healthy Pregnancy [Link]
External Links
Human Metabolome Database
HMDB0000121
KEGG Drug
D00070
KEGG Compound
C00504
PubChem Compound
6037
PubChem Substance
46508092
ChemSpider
5815
BindingDB
50367343
ChEBI
27470
ChEMBL
CHEMBL1622
Therapeutic Targets Database
DAP001309
PharmGKB
PA449692
HET
FOL
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Folic_Acid
ATC Codes
B03AE02 — Iron, multivitamins and folic acidB03BB01 — Folic acidB03AE01 — Iron, vitamin b12 and folic acidB03BB51 — Folic acid, combinations
AHFS Codes
  • 88:08.00 — Vitamin B Complex
PDB Entries
1cd2 / 1dhf / 1drf / 1dyi / 1pj6 / 1qzf / 1ra2 / 1ra8 / 1rb2 / 1rd7
show 62 more
FDA label
Download (298 KB)
MSDS
Download (73.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentFallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Endometrioid Tumor / Fallopian Tube Mucinous Neoplasm / Fallopian Tube Serous Neoplasm / Fallopian Tube Transitional Cell Carcinoma / Malignant Ovarian Mixed Epithelial Tumor / Ovarian Clear Cell Cystadenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Cystadenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Cystadenocarcinoma / Ovarian Transitional Cell Carcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Stage IIIC Fallopian Tube Cancer / Stage IIIC Ovarian Cancer / Stage IIIC Primary Peritoneal Cancer / Stage IV Fallopian Tube Cancer / Stage IV Ovarian Cancer / Stage IV Primary Peritoneal Cancer / Undifferentiated Fallopian Tube Carcinoma / Undifferentiated Ovarian Carcinoma1
1CompletedBasic ScienceCancer of the Ovary1
1CompletedDiagnosticPrimary Hyperparathyroidism1
1CompletedOtherHeart Rate / Heart Rate Variability / Inflammatory Reaction1
1CompletedPreventionContraception / Drug Drug Interaction (DDI) / Pharmacokinetics1
1CompletedPreventionContraception / Female Contraception / Pharmacokinetics / Therapeutic Equivalency1
1CompletedPreventionDrug Drug Interaction (DDI) / Healthy Volunteers / Pharmacokinetics1
1CompletedPreventionHealthy Volunteers / Pharmacokinetics1
1CompletedPreventionOral Contraceptives (OC) / Pharmacokinetics / Therapeutic Equivalency1
1CompletedPreventionRecurrent Neural Tube Defects1
1CompletedTreatmentAcne Vulgaris1
1CompletedTreatmentAdvanced Non-Small Cell Lung Cancer (NSCLC) / Cancer of the Ovary / Non Small Cell Lung Carcinoma (NSCLC) / Triple-Negative Breast Cancer (TNBC) / Tumors, Solid1
1CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
1CompletedTreatmentContraception1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentLeptomeningeal Metastases1
1CompletedTreatmentMalignancies3
1CompletedTreatmentMalignancies / Metastases1
1CompletedTreatmentRecurrent Breast Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Stage IIA Breast Cancer / Stage IIA Fallopian Tube Cancer / Stage IIA Ovarian Cancer / Stage IIB Breast Cancer / Stage IIB Fallopian Tube Cancer / Stage IIB Ovarian Cancer / Stage IIC Fallopian Tube Cancer / Stage IIC Ovarian Cancer / Stage IIIA Breast Cancer / Stage IIIA Fallopian Tube Cancer / Stage IIIA Ovarian Cancer / Stage IIIA Primary Peritoneal Cancer / Stage IIIB Breast Cancer / Stage IIIB Fallopian Tube Cancer / Stage IIIB Ovarian Cancer / Stage IIIB Primary Peritoneal Cancer / Stage IIIC Breast Cancer / Stage IIIC Fallopian Tube Cancer / Stage IIIC Ovarian Cancer / Stage IIIC Primary Peritoneal Cancer / Stage IV Fallopian Tube Cancer / Stage IV Ovarian Cancer / Stage IV Primary Peritoneal Cancer1
1CompletedTreatmentRecurrent Miscarriages1
1CompletedTreatmentRheumatoid Arthritis3
1RecruitingDiagnosticMetastatic Cancer Lung / Ovarian Cancer Metastatic1
1, 2CompletedPreventionCancer of the Ovary / Cancer, Breast1
1, 2CompletedPreventionDeficiency, Vitamin D / Prophylaxis of preeclampsia1
1, 2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
1, 2CompletedTreatmentRetinal Vein Occlusions(RVO)1
1, 2CompletedTreatmentRheumatoid Arthritis1
1, 2CompletedTreatmentSickle Cell Disorders1
1, 2Not Yet RecruitingTreatmentGastric Precancerous Condition1
1, 2RecruitingTreatmentPolycystic Ovaries Syndrome1
1, 2RecruitingTreatmentPostpartum Anemia1
1, 2TerminatedPreventionCervical Cancers1
1, 2TerminatedTreatmentPsoriasis1
1, 2Unknown StatusTreatmentOther Sickle-cell Disorders With Crisis, Unspecified1
2Active Not RecruitingTreatmentLung Cancers / Neoplasms Metastasis1
2Active Not RecruitingTreatmentMetastatic Colorectal Cancers1
2CompletedPreventionAdenoma benign / Colorectal Polyps / Malignant Neoplasm of Colon1
2CompletedPreventionCardiovascular Disease (CVD) / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
2CompletedPreventionDepression / Depressive Disorders1
2CompletedPreventionRefractory Peripheral T-cell Lymphoma Unspecified / Relapsed Peripheral T-Cell Lymphoma1
2CompletedTreatmentAnemias1
2CompletedTreatmentBlood Pressures / Plasma Total Homocysteine Level1
2CompletedTreatmentCardiovascular Disease (CVD) / Endothelial Dysfunction1
2CompletedTreatmentChronic Arsenic Poisoning1
2CompletedTreatmentChronic Renal Failure (CRF)1
2CompletedTreatmentEfficacy / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentEsophageal Cancers1
2CompletedTreatmentHead and Neck Carcinoma1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentLupus / Systemic Lupus Erythematosus (SLE)1
2CompletedTreatmentRheumatoid Arthritis6
2Not Yet RecruitingTreatmentAdenocarcinomas of the Esophagogastric Junction / Malignant Neoplasm of Stomach1
2Not Yet RecruitingTreatmentRheumatoid Arthritis1
2RecruitingTreatmentBilateral Breast Carcinoma / Estrogen Receptor Negative / HER2/Neu Negative / Progesterone Receptor Negative / Stage IB Breast Cancer / Stage IB Breast Cancer AJCC v7 / Stage II Breast Cancer / Stage II Breast Cancer AJCC v6 and v7 / Stage IIA Breast Cancer / Stage IIA Breast Cancer AJCC v6 and v7 / Stage IIB Breast Cancer / Stage IIB Breast Cancer AJCC v6 and v7 / Stage III Breast Cancer / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v7 / Triple-Negative Breast Carcinoma / Unilateral Breast Carcinoma1
2RecruitingTreatmentHuman Immunodeficiency Virus (HIV)1
2RecruitingTreatmentMucositis1
2RecruitingTreatmentNeoadjuvant Chemotherapy / Pancreatic Adenocarcinoma Resectable1
2TerminatedTreatmentInfertilities1
2TerminatedTreatmentRenal Cell Adenocarcinoma1
2TerminatedTreatmentRheumatoid Arthritis1
2Unknown StatusPreventionArsenic Poisoning / Toxic Effect of Arsenic and Its Compounds1
2Unknown StatusPreventionCoronary Artery Disease1
2Unknown StatusTreatmentAfter Resection of Liver Metastases / Colorectal Cancers / KRAS Wildtype1
2Unknown StatusTreatmentAnemias1
2WithdrawnPreventionAging / Inflammatory Reaction1
2WithdrawnTreatmentNeoplasms, Breast1
2, 3CompletedPreventionAdenoma benign / Colorectal Cancers / Polyps1
2, 3CompletedPreventionNausea / Vomiting1
2, 3CompletedTreatmentAtherosclerosis1
2, 3CompletedTreatmentDiabetic Nephropathies1
2, 3CompletedTreatmentFirst Episode Psychosis1
2, 3CompletedTreatmentRheumatoid Arthritis1
2, 3Not Yet RecruitingTreatmentCancer of the Ovary / Cancer, Breast / Folic acid antagonist overdose1
2, 3RecruitingPreventionNeoplasms, Colorectal1
2, 3RecruitingTreatmentAngioplasty, Balloon, Coronary / Contrast Media / Coronary Heart Disease (CHD) / High Blood Pressure (Hypertension) / Homocysteine / Renal Dysfunction1
2, 3RecruitingTreatmentMyocardial Infarction, Anterior Wall / Myocardial Remodeling, Ventricular1
2, 3Unknown StatusTreatmentOsteoarthritis (OA)1
3Active Not RecruitingTreatmentIron-Deficiency Anemias1
3CompletedPreventionCerebral Infarctions / Myocardial Infarction / Strokes1
3CompletedPreventionCerebrovascular Stroke / Coronary Artery Disease / Myocardial Infarction1
3CompletedPreventionCleft Lip / Cleft Palates2
3CompletedPreventionComplications, Pregnancy / Preeclampsia1
3CompletedPreventionGingival Overgrowth1
3CompletedPreventionNutrition1
3CompletedPreventionPlasmodium Infections1
3CompletedTreatmentActive Rheumatoid Arthritis1
3CompletedTreatmentAlzheimer's Disease (AD)1
3CompletedTreatmentContraception1
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3CompletedTreatmentMale Infertility1
3CompletedTreatmentMycobacterium Tuberculosis1
3CompletedTreatmentNeoplasms, Colorectal1
3CompletedTreatmentPremature Ejaculation1
3CompletedTreatmentRheumatoid Arthritis7
3CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
3RecruitingScreeningCervical Intraepithelial Neoplasia Grade 2/31
3RecruitingTreatmentBladder Cancers / Transitional Cell Carcinoma / Ureteral Cancer1
3RecruitingTreatmentInfertility, Female / Polycystic Ovarian Syndrome1
3TerminatedPreventionBlood Loss / Pregnancy termination therapy1
3Unknown StatusPreventionCongenital Malformations1
3Unknown StatusPreventionEpilepsies1
3WithdrawnTreatmentCongenital, Hereditary, and Neonatal Diseases and Abnormalities / Nervous System Malformations / Neural Tube Defects (NTDs)1
4Active Not RecruitingBasic SciencePsoriasis1
4CompletedNot AvailableMetabolic Syndromes1
4CompletedNot AvailablePolycystic Ovarian Syndrome1
4CompletedPreventionAnovulatory cycle / Polycystic Ovaries Syndrome1
4CompletedPreventionCardiovascular Disease (CVD) / Chronic Renal Failure (CRF) / Hemodialysis Treatment / Hyperhomocysteinaemia / Uremia1
4CompletedPreventionDyslipidemias / Homocystinaemia / Menopause1
4CompletedPreventionHypertension,Essential1
4CompletedPreventionPolycystic Ovaries Syndrome / Pregnancy1
4CompletedPreventionPostpartum Haemorrhage (PPH)1
4CompletedTreatmentAnemias / Iron Deficiency1
4CompletedTreatmentBMI >30 kg/m2 / Hyperhomocysteinaemia1
4CompletedTreatmentDepression1
4CompletedTreatmentDiabetic Macular Edema (DME)1
4CompletedTreatmentDiabetic Peripheral Neuropathic Pain (DPN)1
4CompletedTreatmentHyperemesis Gravidarum / Morning Sickness / Nausea / Pregnancy / Vomiting1
4CompletedTreatmentHyperpigmentation1
4CompletedTreatmentIron Deficiency Anemia (IDA)1
4CompletedTreatmentNegative Symptoms / Schizophrenic Disorders1
4CompletedTreatmentPlasmodium Infections1
4CompletedTreatmentPolycystic Ovaries Syndrome1
4CompletedTreatmentPregnancy1
4CompletedTreatmentRecurrent Miscarriages1
4CompletedTreatmentRheumatoid Arthritis2
4CompletedTreatmentSchizophrenic Disorders2
4CompletedTreatmentUnipolar Depression1
4Enrolling by InvitationTreatmentHigh Blood Pressure (Hypertension) / Hyperhomocysteinaemia1
4Not Yet RecruitingTreatmentFaltering Growth / Primary Malnurtrition1
4RecruitingPreventionKidney Diseases / Urologic Diseases1
4RecruitingTreatmentAntioxidants / Male Infertility / Semen Quality1
4RecruitingTreatmentHigh Blood Pressure (Hypertension)1
4RecruitingTreatmentHyperuricemia1
4RecruitingTreatmentInfertilities / Polycystic Ovarian Syndrome1
4RecruitingTreatmentInflammatory Bowel Diseases (IBD)1
4RecruitingTreatmentRheumatoid Arthritis2
4TerminatedDiagnosticTransplantation, Kidney1
4TerminatedTreatmentAnemias1
4TerminatedTreatmentHeart Failure1
4TerminatedTreatmentRheumatoid Arthritis1
4Unknown StatusNot AvailableGestational Diabetes Mellitus (GDM)1
4Unknown StatusPreventionAtherosclerosis / Cardiovascular Disease (CVD)1
4Unknown StatusTreatmentNPDR - Non Proliferative Diabetic Retinopathy / Proliferative Diabetic Retinopathy (PDR)1
4Unknown StatusTreatmentNonulcer Dyspepsia1
4WithdrawnPreventionHigh Blood Pressure (Hypertension) / Hyperhomocysteinaemia1
Not AvailableCompletedNot AvailableAnemias1
Not AvailableCompletedNot AvailableAtherosclerosis / Human Immunodeficiency Virus (HIV) / Inflammatory Reaction1
Not AvailableCompletedNot AvailableInflammatory Bowel Diseases (IBD) / Psoriasis1
Not AvailableCompletedDiagnosticCoronary Artery Disease / Major Surgery1
Not AvailableCompletedPreventionBipolar Disorder (BD) / Depression1
Not AvailableCompletedPreventionCardiovascular Abnormalities1
Not AvailableCompletedPreventionDeep Vein Thrombosis (DVT) / Pulmonary Embolism (PE)1
Not AvailableCompletedPreventionInfection NOS / Sickle Cell Disorders / Zinc Deficiency1
Not AvailableCompletedPreventionIron Deficiency Anemia (IDA)1
Not AvailableCompletedPreventionMorbidity / Pneumonia / Severe or persistent diarrhea / The Mortality Rate1
Not AvailableCompletedPreventionNeural Tube Defects - Spina Bifida and Anencephaly1
Not AvailableCompletedPreventionSpina Bifida and Anencephaly1
Not AvailableCompletedTreatmentAcute Myocardial Infarction (AMI)1
Not AvailableCompletedTreatmentDiabetic Nephropathies / Hyperhomocysteinaemia1
Not AvailableCompletedTreatmentEnd Stage Renal Disease (ESRD) / Hyperhomocysteinaemia1
Not AvailableCompletedTreatmentHyperandrogenism / Menstrual Pattern / Metabolic Features / Polycystic Ovaries Syndrome1
Not AvailableCompletedTreatmentHyperhomocysteinaemia / Inflammatory Reaction / The Mortality Rate1
Not AvailableCompletedTreatmentMale Pattern of Hair Loss, Androgenic Alopecia1
Not AvailableEnrolling by InvitationOtherCochlear Hearing Loss / Homocysteine / Propofol / Sevoflurane1
Not AvailableRecruitingPreventionPost Operative Cognitive Dysfunction1
Not AvailableTerminatedTreatmentAbortion, Therapeutic / Pregnancy Trimester, Second1
Not AvailableUnknown StatusTreatmentAbnormal Uterine Bleeding Unrelated to Menstrual Cycle1
Not AvailableUnknown StatusTreatmentFolic acid antagonist overdose1
Not AvailableUnknown StatusTreatmentHirsutism / Menstrual Irregularities / Polycystic Ovaries Syndrome1
Not AvailableWithdrawnPreventionStrokes / Transient Ischaemic Attack (TIA)1

Pharmacoeconomics

Manufacturers
  • App pharmaceuticals llc
  • Ben venue laboratories inc
  • Wyeth pharmaceuticals inc
  • Barr laboratories inc
  • Cadista pharmaceuticals inc
  • Contract pharmacal corp
  • Everylife
  • Excellium pharmaceutical inc
  • Halsey drug co inc
  • Impax laboratories inc
  • Invagen pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lannett co inc
  • Eli lilly and co
  • Mk laboratories inc
  • Mutual pharmaceutical co inc
  • Nexgen pharma inc
  • Pharmax group inc
  • Pharmeral inc
  • Pioneer pharmaceuticals inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Tablicaps inc
  • Udl laboratories inc
  • Usl pharma inc
  • Valeant pharmaceuticals international
  • Vangard laboratories inc div midway medical co
  • Vintage pharmaceuticals llc
  • Vintage pharmaceuticals inc
  • Watson laboratories
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Whiteworth towne paulsen inc
  • Mission pharmacal co
Packagers
  • Accucaps Industries Ltd.
  • Advanced Pharmaceutical Services Inc.
  • Ajanta Pharma Ltd.
  • Amend
  • Amerisource Health Services Corp.
  • Apace Packaging
  • Apotheca Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Avkare Incorporated
  • Avpak
  • Blu Pharmaceuticals LLC
  • Breckenridge Pharmaceuticals
  • Bryant Ranch Prepack
  • Cadista Pharmaceuticals Inc.
  • Cardinal Health
  • Carlisle Laboratories Inc.
  • Chemins Co. Inc.
  • Comprehensive Consultant Services Inc.
  • Consolidated Midland Corp.
  • Contract Pharm
  • Coupler Enterprises Inc.
  • CVS Pharmacy
  • Cypress Pharmaceutical Inc.
  • DAVA Pharmaceuticals
  • Deca Pharmaceuticals LLC
  • Dept Health Central Pharmacy
  • DHHS Program Support Center Supply Service Center
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • ESI Lederle
  • Excellium Pharmaceutical Inc.
  • Heartland Repack Services LLC
  • Ivax Pharmaceuticals
  • JLM Pharmatech
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Merit Pharmaceuticals
  • Mission Pharmacal
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nexgen Pharma Inc.
  • Nnodum Pharmaceutical Corporation
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmics Inc.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Qualitest
  • Re Por Laboratories
  • Remedy Repack
  • Richmond Pharmacy
  • Rising Pharmaceuticals
  • Rugby Laboratories
  • Sandhills Packaging Inc.
  • Savage Labs
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Tya Pharmaceuticals
  • UDL Laboratories
  • US Pharmaceutical Corp.
  • Vangard Labs Inc.
  • Walgreen Co.
  • Watson Pharmaceuticals
  • West-Ward Pharmaceuticals
Dosage forms
FormRouteStrength
SolutionOral
PatchTransdermal
Granule, effervescentOral
Capsule, liquid filledOral
CapsuleOral
Tablet, effervescentOral
Capsule, delayed release pelletsOral
LozengeOral
CapsuleOral1 mg
Injection, solutionIntramuscular; Intravenous; Subcutaneous5 mg/1mL
TabletOral1 mg/1
TabletOral400 ug/1
TabletOral5 mg
TabletOral800 ug/1
CapsuleOral
Tablet, extended releaseOral
LiquidIntramuscular; Intravenous; Subcutaneous
SolutionIntramuscular; Intravenous; Subcutaneous
TabletOral
Tablet, coatedOral
PowderOral
Solution / dropsOral
LiquidOral
Injection, powder, lyophilized, for solutionIntravenous
Tablet, chewableOral
SolutionIntravenous
TabletOral
LiquidIntravenous
Capsule, gelatin coatedOral
Tablet, orally disintegratingOral
KitOral100 mg/1
Powder, for solutionOral
KitIntravenous
Injection, solutionIntravenous
Tablet, film coatedOral
PillOral
WaferOral
Capsule, extended releaseOral
Tablet, extended releaseOral
Capsule, coatedOral
StripOral
KitOral
Prices
Unit descriptionCostUnit
Folic acid 5 mg/ml vial2.14USD ml
Folic Acid 5 mg/ml2.04USD ml
Folic acid powder1.68USD g
Folvite 5 mg/ml vial1.38USD ml
Folic Acid 1 mg tablet0.15USD tablet
Folic acid 400 mcg tablet0.07USD tablet
Apo-Folic 5 mg Tablet0.04USD tablet
CVS Pharmacy folic acid 800 mcg tablet0.02USD tablet
Folic acid 0.4 mg tablet0.02USD tablet
Folic acid 0.8 mg tablet0.02USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP-2.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0761 mg/mLALOGPS
logP-0.04ALOGPS
logP-0.68ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)3.37ChemAxon
pKa (Strongest Basic)2.09ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count6ChemAxon
Polar Surface Area208.99 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity111.01 m3·mol-1ChemAxon
Polarizability42.06 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7956
Blood Brain Barrier+0.7609
Caco-2 permeable-0.844
P-glycoprotein substrateSubstrate0.687
P-glycoprotein inhibitor INon-inhibitor0.9795
P-glycoprotein inhibitor IINon-inhibitor0.9969
Renal organic cation transporterNon-inhibitor0.876
CYP450 2C9 substrateNon-substrate0.8276
CYP450 2D6 substrateNon-substrate0.7947
CYP450 3A4 substrateNon-substrate0.6212
CYP450 1A2 substrateNon-inhibitor0.9281
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9435
CYP450 2C19 inhibitorNon-inhibitor0.916
CYP450 3A4 inhibitorNon-inhibitor0.9075
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.974
Ames testNon AMES toxic0.8724
CarcinogenicityNon-carcinogens0.9521
BiodegradationNot ready biodegradable0.9191
Rat acute toxicity2.4490 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9529
hERG inhibition (predictor II)Non-inhibitor0.8444
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0006-9410000000-7cba521e870757539424
MS/MS Spectrum - Quattro_QQQ 10V, PositiveLC-MS/MSsplash10-0006-0000900000-4208ea3c2f5d9026c19f
MS/MS Spectrum - Quattro_QQQ 25V, PositiveLC-MS/MSsplash10-0006-0050900000-2c8ad037dc3b270765c4
MS/MS Spectrum - Quattro_QQQ 40V, PositiveLC-MS/MSsplash10-0007-0090300000-ebdec84cbb7fe5afbc0b
LC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) , NegativeLC-MS/MSsplash10-0007-0903600000-e5d91e4f2ab79d130b76
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0007-0903600000-e5d91e4f2ab79d130b76
MS/MS Spectrum - , positiveLC-MS/MSsplash10-002b-0960000000-108d96993dc78f1e4b61
1H NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as glutamic acid and derivatives. These are compounds containing glutamic acid or a derivative thereof resulting from reaction of glutamic acid at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Glutamic acid and derivatives
Alternative Parents
N-acyl-alpha amino acids / Hippuric acids / Pterins and derivatives / Aminobenzamides / Phenylalkylamines / Aniline and substituted anilines / Benzoyl derivatives / Secondary alkylarylamines / Hydroxypyrimidines / Pyrazines
show 10 more
Substituents
Glutamic acid or derivatives / N-acyl-alpha-amino acid / N-acyl-alpha amino acid or derivatives / Hippuric acid / Hippuric acid or derivatives / Pterin / Aminobenzamide / Aminobenzoic acid or derivatives / Pteridine / Benzamide
show 30 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-acyl-amino acid, folic acids (CHEBI:27470) / Water-soluble vitamins (C00504)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Folic acid binding
Specific Function
Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate to the interior of cells. Isoform Short does not bind folate.
Gene Name
FOLR3
Uniprot ID
P41439
Uniprot Name
Folate receptor gamma
Molecular Weight
27638.0 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Shen F, Ross JF, Wang X, Ratnam M: Identification of a novel folate receptor, a truncated receptor, and receptor type beta in hematopoietic cells: cDNA cloning, expression, immunoreactivity, and tissue specificity. Biochemistry. 1994 Feb 8;33(5):1209-15. [PubMed:8110752]
  4. Shen F, Wu M, Ross JF, Miller D, Ratnam M: Folate receptor type gamma is primarily a secretory protein due to lack of an efficient signal for glycosylphosphatidylinositol modification: protein characterization and cell type specificity. Biochemistry. 1995 Apr 25;34(16):5660-5. [PubMed:7727426]
  5. Prasad PD, Ramamoorthy S, Moe AJ, Smith CH, Leibach FH, Ganapathy V: Selective expression of the high-affinity isoform of the folate receptor (FR-alpha) in the human placental syncytiotrophoblast and choriocarcinoma cells. Biochim Biophys Acta. 1994 Aug 11;1223(1):71-5. [PubMed:8061055]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Methotrexate binding
Specific Function
Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells. Has high affinity for folate and folic acid analo...
Gene Name
FOLR2
Uniprot ID
P14207
Uniprot Name
Folate receptor beta
Molecular Weight
29279.31 Da
References
  1. Dixit V, Van den Bossche J, Sherman DM, Thompson DH, Andres RP: Synthesis and grafting of thioctic acid-PEG-folate conjugates onto Au nanoparticles for selective targeting of folate receptor-positive tumor cells. Bioconjug Chem. 2006 May-Jun;17(3):603-9. [PubMed:16704197]
  2. Wlodarczyk BJ, Cabrera RM, Hill DS, Bozinov D, Zhu H, Finnell RH: Arsenic-induced gene expression changes in the neural tube of folate transport defective mouse embryos. Neurotoxicology. 2006 Jul;27(4):547-57. Epub 2006 Apr 18. [PubMed:16620997]
  3. Boyles AL, Billups AV, Deak KL, Siegel DG, Mehltretter L, Slifer SH, Bassuk AG, Kessler JA, Reed MC, Nijhout HF, George TM, Enterline DS, Gilbert JR, Speer MC: Neural tube defects and folate pathway genes: family-based association tests of gene-gene and gene-environment interactions. Environ Health Perspect. 2006 Oct;114(10):1547-52. [PubMed:17035141]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Receptor activity
Specific Function
Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells. Has high affinity for folate and folic acid analo...
Gene Name
FOLR1
Uniprot ID
P15328
Uniprot Name
Folate receptor alpha
Molecular Weight
29818.94 Da
References
  1. Wang L, Desmoulin SK, Cherian C, Polin L, White K, Kushner J, Fulterer A, Chang MH, Mitchell-Ryan S, Stout M, Romero MF, Hou Z, Matherly LH, Gangjee A: Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits beta-glycinamide ribonucleotide formyltransferase. J Med Chem. 2011 Oct 27;54(20):7150-64. doi: 10.1021/jm200739e. Epub 2011 Sep 22. [PubMed:21879757]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Omega peptidase activity
Specific Function
Hydrolyzes the polyglutamate sidechains of pteroylpolyglutamates. Progressively removes gamma-glutamyl residues from pteroylpoly-gamma-glutamate to yield pteroyl-alpha-glutamate (folic acid) and fr...
Gene Name
GGH
Uniprot ID
Q92820
Uniprot Name
Gamma-glutamyl hydrolase
Molecular Weight
35964.045 Da
References
  1. Schneider E, Ryan TJ: Gamma-glutamyl hydrolase and drug resistance. Clin Chim Acta. 2006 Dec;374(1-2):25-32. Epub 2006 Jun 10. [PubMed:16859665]
  2. Eisele LE, Chave KJ, Lehning AC, Ryan TJ: Characterization of Human gamma-glutamyl hydrolase in solution demonstrates that the enzyme is a non-dissociating homodimer. Biochim Biophys Acta. 2006 Sep;1764(9):1479-86. Epub 2006 Jul 12. [PubMed:16945597]
  3. Chen L, Eitenmiller RR: Optimization of the trienzyme extraction for the microbiological assay of folate in vegetables. J Agric Food Chem. 2007 May 16;55(10):3884-8. Epub 2007 Apr 17. [PubMed:17439143]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein complex binding
Specific Function
Catalyzes the conversion of 5,10-methylenetetrahydrofolate to 5-methyltetrahydrofolate, a co-substrate for homocysteine remethylation to methionine.
Gene Name
MTHFR
Uniprot ID
P42898
Uniprot Name
Methylenetetrahydrofolate reductase
Molecular Weight
74595.895 Da
References
  1. West AA, Caudill MA: Genetic variation: impact on folate (and choline) bioefficacy. Int J Vitam Nutr Res. 2010 Oct;80(4-5):319-29. doi: 10.1024/0300-9831/a000040. [PubMed:21462116]
  2. Kim YI: Role of the MTHFR polymorphisms in cancer risk modification and treatment. Future Oncol. 2009 May;5(4):523-42. doi: 10.2217/fon.09.26. [PubMed:19450180]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Nadph binding
Specific Function
Key enzyme in folate metabolism. Contributes to the de novo mitochondrial thymidylate biosynthesis pathway. Catalyzes an essential reaction for de novo glycine and purine synthesis, and for DNA pre...
Gene Name
DHFR
Uniprot ID
P00374
Uniprot Name
Dihydrofolate reductase
Molecular Weight
21452.61 Da

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Purine nucleotide transmembrane transporter activity
Specific Function
Participates in physiological processes involving bile acids, conjugated steroids and cyclic nucleotides. Enhances the cellular extrusion of cAMP and cGMP. Stimulates the ATP-dependent uptake of a ...
Gene Name
ABCC11
Uniprot ID
Q96J66
Uniprot Name
ATP-binding cassette sub-family C member 11
Molecular Weight
154299.625 Da
References
  1. Chen ZS, Guo Y, Belinsky MG, Kotova E, Kruh GD: Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). Mol Pharmacol. 2005 Feb;67(2):545-57. Epub 2004 Nov 10. [PubMed:15537867]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
Gene Name
ABCC3
Uniprot ID
O15438
Uniprot Name
Canalicular multispecific organic anion transporter 2
Molecular Weight
169341.14 Da
References
  1. Zeng H, Chen ZS, Belinsky MG, Rea PA, Kruh GD: Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32. [PubMed:11585759]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. Kuze K, Graves P, Leahy A, Wilson P, Stuhlmann H, You G: Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells. J Biol Chem. 1999 Jan 15;274(3):1519-24. [PubMed:9880528]
  2. Uwai Y, Okuda M, Takami K, Hashimoto Y, Inui K: Functional characterization of the rat multispecific organic anion transporter OAT1 mediating basolateral uptake of anionic drugs in the kidney. FEBS Lett. 1998 Nov 6;438(3):321-4. [PubMed:9827570]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Chen ZS, Lee K, Walther S, Raftogianis RB, Kuwano M, Zeng H, Kruh GD: Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50. [PubMed:12036927]
  2. Rius M, Nies AT, Hummel-Eisenbeiss J, Jedlitschky G, Keppler D: Cotransport of reduced glutathione with bile salts by MRP4 (ABCC4) localized to the basolateral hepatocyte membrane. Hepatology. 2003 Aug;38(2):374-84. [PubMed:12883481]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Chen ZS, Robey RW, Belinsky MG, Shchaveleva I, Ren XQ, Sugimoto Y, Ross DD, Bates SE, Kruh GD: Transport of methotrexate, methotrexate polyglutamates, and 17beta-estradiol 17-(beta-D-glucuronide) by ABCG2: effects of acquired mutations at R482 on methotrexate transport. Cancer Res. 2003 Jul 15;63(14):4048-54. [PubMed:12874005]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Methotrexate transporter activity
Specific Function
Has been shown to act both as an intestinal proton-coupled high-affinity folate transporter and as an intestinal heme transporter which mediates heme uptake from the gut lumen into duodenal epithel...
Gene Name
SLC46A1
Uniprot ID
Q96NT5
Uniprot Name
Proton-coupled folate transporter
Molecular Weight
49770.04 Da
References
  1. Nakai Y, Inoue K, Abe N, Hatakeyama M, Ohta KY, Otagiri M, Hayashi Y, Yuasa H: Functional characterization of human proton-coupled folate transporter/heme carrier protein 1 heterologously expressed in mammalian cells as a folate transporter. J Pharmacol Exp Ther. 2007 Aug;322(2):469-76. Epub 2007 May 2. [PubMed:17475902]
  2. Ashokkumar B, Mohammed ZM, Vaziri ND, Said HM: Effect of folate oversupplementation on folate uptake by human intestinal and renal epithelial cells. Am J Clin Nutr. 2007 Jul;86(1):159-66. [PubMed:17616776]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Folic acid transporter activity
Specific Function
Transports folate across the inner membranes of mitochondria.
Gene Name
SLC25A32
Uniprot ID
Q9H2D1
Uniprot Name
Mitochondrial folate transporter/carrier
Molecular Weight
35406.83 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Drug created on June 13, 2005 07:24 / Updated on September 17, 2019 03:30