- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | Folate; PGA; Pteroyl-L-glutamic acid; Pteroyl-L-monoglutamic acid; Pteroylglutamic acid; Pteroylmonoglutamic acid; Vitamin B9; Vitamin Bc; Vitamin Be; Vitamin M |
|---|---|
| Trade Names: | Acifolic; Apo-Folic; Cytofol; Dosfolat B activ; Folacid; Folacin; Folbal; Folcidin; Foldine; Folettes; Foliamin; Folicet; Folipac; Folsan; Folsaure; Folsav; Folvite; Folvron; Incafolic; Millafol |
| PharmGKB Accession Id: | PA449692 |
Description
A member of the vitamin B family that stimulates the hematopoietic system. It is present in the liver and kidney and is found in mushrooms, spinach, yeast, green leaves, and grasses (poaceae). Folic acid is used in the treatment and prevention of folate deficiencies and megaloblastic anemia. PubChem (source: Drug Bank)
Indication
For treatment of folic acid deficiency, megaloblastic anemia and in anemias of nutritional supplements, pregnancy, infancy, or childhood. (source: Drug Bank)
ATC Therapeutic Category
- B03BB:Folic acid and derivatives
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Folic acid, as it is biochemically inactive, is converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase. 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. (source: Drug Bank)
Pharmacology
Folic acid, a water-soluble B-complex vitamin, is found in foods such as liver, kidneys, yeast, and leafy, green vegetables. Folic acid is used to diagnose folate deficiency and to treat topical sprue and megaloblastic and macrocytic anemias, hematologic complications resulting from a deficiency in folic acid. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
Very high to plasma protein (source: Drug Bank)
Toxicity
IPR-MUS LD<sub>50</sub> 85 mg/kg,IVN-GPG LD<sub>50</sub> 120 mg/kg, IVN-MUS LD<sub>50</sub> 239 mg/kg, IVN-RAT LD<sub>50</sub> 500 mg/kg, IVN-RBT LD<sub>50</sub> 410 mg/kg (source: Drug Bank)
Isomeric SMILES Code:
c1cc(ccc1C(=O)N[C@@H](CCC(=O)O)C(=O)O)NCc2cnc3c(n2)c(nc(n3)N)O (source: Drug Bank)
In-Depth Annotations (
)
-
rs1801131
at chr1:11777063
in
MTHFR
Well studied, associated with multiple phenotypes.- Variant Name:
- MTHFR:1298A>C
- Related Drugs:
- folic acid, methotrexate
- Evidence:
-
http://www.pharmgkb.org/.../variant.jsp
-
rs1801133
at chr1:11778965
in
CLCN6,
MTHFR
Well studied, associated with multiple phenotypes.- Variant Name:
- MTHFR:677C>T
- Related Drugs:
- fluorouracil, folic acid, methotrexate
- Evidence:
-
http://www.pharmgkb.org/.../variant.jsp#ImportantVariantInformationforMTHFR-677CT
Curated Annotations (
)
-
rs1801131
at chr1:11777063
in
MTHFR
At 6 months methotrexate and folic acid therapy, of early rheumatoid arthritis patients with the MTHFR 1298AA genotype showed good improvement relative to combined CA and AA genotypes (OR 2.3), while 1298C allele carriers developed more adverse drug events (OR 2.5) (e.g. pneumonitis, gastrointestinal ADEs, skin and mucosal ADEs, and elevated liver enzyme levels). Patients with MTHFR 1298AA / 677CC diplotype showed greater clinical improvement.- Variant Name:
- MTHFR:1298A>C
- Related Drugs:
- folic acid, methotrexate
- Related Diseases:
- Arthritis, Rheumatoid
- Evidence:
-
PMID:16572443
-
rs1801131
at chr1:11777063
in
MTHFR
In 330 patients who completed 3 months methotrexate treatment for psoriasis, no significant genotypic associations were found between clinical outcome (e.g. efficacy, toxicity) and 50 SNPs in pathway genes for methotrexate metabolism (ATIC, FPGS, GGH, MTHFR), including 47 common ( >5% minor allele frequency) haplotype-tagging SNPs (r(2) > 0.8) plus 3 additional SNPs.- Variant Name:
- MTHFR:298A>C
- Related Drugs:
- folic acid, methotrexate
- Related Diseases:
- Psoriasis
- Evidence:
-
PMID:19016697
-
rs1801133
at chr1:11778965
in
CLCN6,
MTHFR
Given methotrexate and folic acid therapy, patients with the MTHFR 1298AA / 677CC diplotype showed greater clinical improvement for early rheumatoid arthritis.- Variant Name:
- MTHFR:677C>T
- Related Drugs:
- folic acid, methotrexate
- Related Diseases:
- Arthritis, Rheumatoid
- Evidence:
-
PMID:16572443
-
rs1801133
at chr1:11778965
in
CLCN6,
MTHFR
In 330 patients who completed 3 months methotrexate treatment for psoriasis, no significant genotypic associations were found between clinical outcome (e.g. efficacy, toxicity) and 50 SNPs in pathway genes for methotrexate metabolism (ATIC, FPGS, GGH, MTHFR), including 47 common ( >5% minor allele frequency) haplotype-tagging SNPs (r(2) > 0.8) plus 3 additional SNPs.- Variant Name:
- MTHFR:667C>T
- Related Drugs:
- folic acid, methotrexate
- Related Diseases:
- Psoriasis
- Evidence:
-
PMID:19016697
-
rs2372536
at chr2:215898265
in
ATIC
In 330 patients who completed 3 months methotrexate treatment for psoriasis, no significant genotypic associations were found between clinical outcome (e.g. efficacy, toxicity) and 50 SNPs in pathway genes for methotrexate metabolism (ATIC, FPGS, GGH, MTHFR), including 47 common ( >5% minor allele frequency) haplotype-tagging SNPs (r(2) > 0.8) plus 3 additional SNPs.- Variant Name:
- ATIC:347C>G
- Related Drugs:
- folic acid, methotrexate
- Related Diseases:
- Psoriasis
- Evidence:
-
PMID:19016697
-
rs70991108
at chr5:79985919
in
DHFR,
MSH3
Risk or phenotype-associated allele: del/del Phenotype: Women with the del/del genotype had increased serum and red blood cell folate concentrations. Study size: 197 Study population/ethnicity: Females from the Young Hearts Study; 20-26 years old; Northern Ireland Significance metric(s): p = 0.02 (serum folate); p = 0.16 (red blood cell folate) Type of association: PD- Variant Name:
- DHFR c.86 + 60_78; DHFR:19bp deletion in intron 1;
- Related Drugs:
- folic acid
- Evidence:
-
PMID:18247058
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ABCB1 |
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Publications |
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ABCC1 |
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Publications |
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ABCC2 |
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Publications |
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ABCC3 |
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Publications |
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ABCC4 |
|
Publications |
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ABCG2 |
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Publications |
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BHMT |
|
Publications |
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BHMT2 |
|
Publications |
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CBS |
|
Publications |
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CLCN6 |
|
Variants |
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COMT |
|
Publications |
|
|
DHFR |
|
Publications, Variants |
|
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FOLR1 |
|
Publications |
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FOLR2 |
|
Publications |
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FOLR3 |
|
Publications |
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MSH3 |
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Variants |
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MTHFD1 |
|
Publications |
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MTHFD2 |
|
Publications |
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MTHFR |
|
Publications, Variants |
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MTHFS |
|
Publications |
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MTR |
|
Publications |
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MTRR |
|
Publications |
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NNMT |
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Publications |
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NOS3 |
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Publications |
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SHMT1 |
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Publications |
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SLC19A1 |
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Publications |
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SLC46A1 |
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Publications |
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TCN1 |
|
Publications |
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TYMS |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| FOLR2 |
|
(source: Drug Bank) |
| FOLR3 |
|
(source: Drug Bank) |
| GGH |
|
(source: Drug Bank) |
| SLC25A32 |
|
(source: Drug Bank) |
| SLC46A1 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amobarbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| butalbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| hexobarbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| mephenytoin |
|
Folic acid decreases the levels of hydantoin (source: Drug Bank) |
| methylphenobarbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| pentobarbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| phenobarbital |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
| phenytoin |
|
Folic acid decreases the levels of hydantoin (source: Drug Bank) |
| primidone |
|
Folic acid decreases the effect of anticonvulsant (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Adenoma |
|
Publications |
|
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Anemia, Megaloblastic |
|
Publications |
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Chromosome Breakage |
|
Publications |
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Cleft Lip |
|
Publications |
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Colorectal Neoplasms |
|
Publications |
|
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Heart Defects, Congenital |
|
Publications |
|
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Hyperhomocysteinemia |
|
Publications |
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Hypertension |
|
Publications |
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Leukemia |
|
Publications |
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Lung Neoplasms |
|
Publications |
|
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Malabsorption Syndromes |
|
Publications |
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Metabolic Diseases |
|
Publications |
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Nervous System Malformations |
|
Publications |
|
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Neural Tube Defects |
|
Publications |
|
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Precursor Cell Lymphoblastic Leukemia-Lymphoma |
|
Publications |
|
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Spina Bifida Cystica |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
