Folic Acid
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Also known as Acide foliqueAcido folicoAcidum folicumB03BB01Bio scienceFolacinFolateFoldineFolettesFoliaminFolic acid component of folvronFolic acid component of vitapedFolicareFolicetFolipacFolsanFolviteIncafolicLexpec
Summary
Folic Acid (CHEMBL1622) is an approved small molecule (ATC V04CX02) targeting SLC19A1 and SLC46A1; indicated across 72 conditions including iron deficiency anemia and chronic kidney disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: V04CX02 (+2 more)
- Targets: 2 (SLC19A1, SLC46A1)
- Indications: 72 conditions
- Clinical trials: 285
- Chemistry: 441.4 Da · C19H19N7O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1622 |
| Name | Folic Acid |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 135398658 |
| ChEBI | CHEBI:27470 |
| ATC | V04CX02, B03BB01, B03BB51 |
| Molecular formula | C19H19N7O6 |
| Molecular weight | 441.4 |
| InChIKey | OVBPIULPVIDEAO-LBPRGKRZSA-N |
SMILES: C1=CC(=CC=C1C(=O)N[C@@H](CCC(=O)O)C(=O)O)NCC2=CN=C3C(=N2)C(=O)NC(=N3)N
IUPAC name: (2S)-2-[[4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid
ChEBI definition: An N-acyl-amino acid that is a form of the water-soluble vitamin B9. Its biologically active forms (tetrahydrofolate and others) are essential for nucleotide biosynthesis and homocysteine remethylation.
Pharmacological roles (ChEBI): nutrient.
Other ChEBI roles (chemical / environmental): human metabolite, mouse metabolite.
Also known as: Acide folique, Acido folico, Acidum folicum, B03BB01, Bio science, Folacin, Folate, Foldine, Folettes, Foliamin, Folic acid, Folic acid component of folvron
Parent form; salt/anhydrous children: CHEMBL2107429
Patent coverage: 199,776 distinct patent families (525,158 SureChEMBL compound mentions), from 8 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| SLC19A1 | Reduced folate transporter 1 | 31.4% | P41440 | ||
| SLC46A1 | Proton-coupled folate transporter | 2.7% | Q96NT5 |
Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Lysine-specific demethylase 4E, Fructose-bisphosphate aldolase, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Dihydrofolate reductase, Aldo-keto reductase family 1 member B1, Thymidylate synthase, Thyrotropin receptor, Solute carrier organic anion transporter family member 1A3.
Bioactivity
ChEMBL activities: 6 potent at pChembl ≥ 5 of 21 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P0ABQ4 | 6.09 | Kd | 810 | nM | CHEMBL_ACT_817143 |
| P0ABQ4 | 5.36 | Kd | 4400 | nM | CHEMBL_ACT_817144 |
| P0ABQ4 | 5.32 | Kd | 4800 | nM | CHEMBL_ACT_817145 |
| TSHR | 5.1 | Potency | 7943 | nM | CHEMBL_ACT_3918974 |
| Q63921 | 5 | AC50 | 10000 | nM | CHEMBL_ACT_25174327 |
| KDM4E | 5 | Potency | 10000 | nM | CHEMBL_ACT_3714365 |
Target pathways
Aggregated over 2 target gene(s): SLC19A1, SLC46A1.
Top Reactome pathways
6 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Metabolism of folate and pterines | 2 | SLC19A1, SLC46A1 |
| Metabolism | 1 | SLC19A1 |
| Metabolism of water-soluble vitamins and cofactors | 1 | SLC19A1 |
| Metabolism of vitamins and cofactors | 1 | SLC19A1 |
| Iron uptake and transport | 1 | SLC46A1 |
| Heme signaling | 1 | SLC46A1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| folic acid transport | 2 |
| folic acid metabolic process | 2 |
| methotrexate transport | 2 |
| folate transmembrane transport | 2 |
| folate import across plasma membrane | 2 |
| xenobiotic transmembrane transport | 1 |
| female pregnancy | 1 |
| response to xenobiotic stimulus | 1 |
| response to toxic substance | 1 |
| obsolete organic anion transport | 1 |
| cyclic-GMP-AMP transmembrane import across plasma membrane | 1 |
| positive regulation of cGAS/STING signaling pathway | 1 |
| transport across blood-brain barrier | 1 |
| vitamin transmembrane transport | 1 |
| vitamin transport | 1 |
Indications & clinical
Indications
72 indications (11 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| iron deficiency anemia | 4 | MONDO:0001356 | HP:0001891 |
| chronic kidney disease | 4 | MONDO:0005300 | EFO:0003884 |
| anemia | 4 | MONDO:0002280 | EFO:0004272 |
| osteoporosis | 4 | MONDO:0005298 | EFO:0003882 |
| acne | 4 | MONDO:0011438 | EFO:0003894 |
| depressive disorder | 4 | MONDO:0002050 | MONDO:0002050 |
| type 2 diabetes mellitus | 4 | MONDO:0005148 | MONDO:0005148 |
| epilepsy | 3 | MONDO:0005027 | EFO:0000474 |
| heart disorder | 3 | MONDO:0005267 | EFO:0003777 |
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| hypertensive disorder | 3 | MONDO:0005044 | EFO:0000537 |
| malaria | 3 | MONDO:0005136 | EFO:0001068 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| cleft lip | 3 | MONDO:0004747 | EFO:0003959 |
| colorectal neoplasm | 3 | MONDO:0005335 | EFO:0004142 |
| male infertility | 3 | MONDO:0005372 | EFO:0004248 |
| cleft palate | 3 | MONDO:0016064 | HP:0000175 |
| gingival overgrowth | 3 | MONDO:0002507 | MONDO:0002507 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| Alzheimer disease | 3 | MONDO:0004975 | MONDO:0004975 |
| type 1 diabetes mellitus | 3 | MONDO:0005147 | MONDO:0005147 |
| neural tube defect | 3 | MONDO:0018075 | MONDO:0018075 |
| tuberculosis | 3 | MONDO:0018076 | MONDO:0018076 |
| premature ejaculation | 3 | MONDO:0001780 | EFO:0803321 |
| systemic lupus erythematosus | 3 | MONDO:0007915 | MONDO:0007915 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000764 |
| autism | 2 | MONDO:0005260 | EFO:0003758 |
| habitual spontaneous abortion | 2 | MONDO:0006774 | EFO:1000954 |
| peripheral T-cell lymphoma, not otherwise specified | 2 | MONDO:0004964 | EFO:0000211 |
| diabetic kidney disease | 2 | MONDO:0005016 | EFO:0000401 |
| infertility disorder | 2 | MONDO:0005047 | EFO:0000545 |
| lymphoma | 2 | MONDO:0005062 | EFO:0000574 |
| mesothelioma | 2 | MONDO:0005065 | EFO:0000588 |
| heart failure | 2 | MONDO:0005252 | EFO:0003144 |
| breast neoplasm | 2 | MONDO:0021100 | EFO:0003869 |
| atherosclerosis | 2 | MONDO:0005311 | EFO:0003914 |
| upper aerodigestive tract neoplasm | 2 | MONDO:0005398 | EFO:0004284 |
| psychotic disorder | 2 | MONDO:0005485 | EFO:0005407 |
| head and neck cancer | 2 | MONDO:0005627 | EFO:0006859 |
| uveitis | 2 | MONDO:0020283 | EFO:1001231 |
| heavy metal poisoning | 2 | MONDO:0023305 | EFO:1001518 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| myocardial infarction | 2 | MONDO:0005068 | EFO:0000612 |
| myocardial ischemia | 2 | MONDO:0024644 | EFO:1001375 |
| mucositis | 2 | MONDO:0020579 | EFO:1001898 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| coronary artery disorder | 2 | MONDO:0005010 | EFO:0001645 |
| rectal cancer | 2 | MONDO:0006519 | EFO:1000657 |
| sickle cell disease | 2 | MONDO:0011382 | MONDO:0011382 |
| Parkinson disease | 2 | MONDO:0005180 | MONDO:0005180 |
| polycystic ovary syndrome | 1 | MONDO:0008487 | EFO:0000660 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| primary cutaneous T-cell non-Hodgkin lymphoma | 1 | MONDO:0000607 | EFO:0002913 |
| anaplastic large cell lymphoma | 1 | MONDO:0020325 | EFO:0003032 |
| Sezary syndrome | 1 | MONDO:0017844 | EFO:1000785 |
| mycosis fungoides | 1 | MONDO:0009691 | EFO:1001051 |
| peritoneal neoplasm | 1 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 1 | MONDO:0021092 | MONDO:0002158 |
| ovarian cancer | 1 | MONDO:0008170 | MONDO:0008170 |
| pulmonary alveolar proteinosis | 1 | MONDO:0001437 | MONDO:0001437 |
12 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 285.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 93 |
| PHASE2 | 60 |
| PHASE4 | 50 |
| PHASE3 | 36 |
| PHASE1 | 18 |
| PHASE2/PHASE3 | 13 |
| PHASE1/PHASE2 | 10 |
| EARLY_PHASE1 | 5 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04579848 | PHASE4 | ACTIVE_NOT_RECRUITING | Methotrexate in Erosive Inflammatory Hand Osteoarthritis |
| NCT04974138 | PHASE4 | RECRUITING | China Stroke Primary Prevention Trial 2 for Participants With H-type Hypertension and MTHFR 677 CC/CT Genotype (CSPPT2-CC/CT) |
| NCT04974151 | PHASE4 | RECRUITING | China Stroke Primary Prevention Trial 2 for Participants With Hypertension and MTHFR 677 TT Genotype |
| NCT06610266 | PHASE4 | RECRUITING | Efficacy and Safety of Weifuchun Tablet in Reversing Gastric Intestinal Metaplasia |
| NCT06943482 | PHASE4 | NOT_YET_RECRUITING | Comparing Effectiveness of Steroids and Methotrexate in Treatment of Chronic Inflammatory Breast Disease |
| NCT07029698 | PHASE4 | RECRUITING | A Study to See if a Combination of Vitamins That is Injected Into a Muscle is as Good and Safe as a Vitamin That is Taken by Mouth |
| NCT00130065 | PHASE4 | COMPLETED | The Effect of Folic Acid on Efficacy of Sulfadoxine-pyrimethamine in Pregnant Women in Western Kenya |
| NCT00164970 | PHASE4 | COMPLETED | Can Oral Vitamin B12 and Folate Supplementation Preserve Cognitive Function of Patients With Early Dementia? |
| NCT00226356 | PHASE4 | COMPLETED | Natural Supplements for Unipolar Depression |
| NCT00249288 | PHASE4 | COMPLETED | Folate Supplementation in Schizophrenia |
| NCT00317005 | PHASE4 | COMPLETED | Uremic Hyperhomocysteinemia -A Folate Trial for Possible Prevention of Cardiovascular Events |
| NCT00462345 | PHASE4 | COMPLETED | A Study of MabThera (Rituximab) in Combination With Methotrexate in Patients With Rheumatoid Arthritis Who Have Had an Inadequate Response to Anti-TNF Therapies. |
| NCT00491907 | PHASE4 | TERMINATED | Effect of Folic Acid on Endothelial and Baroreceptor Function in Patients With Heart Failure |
| NCT00514410 | PHASE4 | COMPLETED | Folate Augmentation of Treatment - Evaluation for Depression: a Randomised Controlled Trial |
| NCT00570856 | PHASE4 | TERMINATED | Trial of Folic Acid Effect on Hcy and cIMT After Kidney Tx |
| NCT00611806 | PHASE4 | COMPLETED | Effectiveness of Vitamin Supplementation in Treating People With Residual Symptoms of Schizophrenia |
| NCT00794885 | PHASE4 | COMPLETED | China Stroke Primary Prevention Trial |
| NCT01050556 | PHASE4 | COMPLETED | Folic Acid and Creatine as Therapeutic Approaches for Lowering Blood Arsenic |
| NCT01263080 | PHASE4 | COMPLETED | Evaluation of Mirtazapine and Folic Acid for Schizophrenia: |
| NCT01283971 | PHASE4 | TERMINATED | A Study of RoActemra/Actemra (Tocilizumab) Versus Adalimumab in Combination With Methotrexate (MTX) in Patients With Moderate to Severe Active Rheumatoid Arthritis And an Inadequate Response to Treatment With Only One Tumor Necrosis Factor (TNF)-Inhibitor |
| NCT01308255 | PHASE4 | COMPLETED | Infliximab as Induction Therapy in Early Rheumatoid Arthritis (IDEA) |
| NCT01493674 | PHASE4 | COMPLETED | Folic Acid Supplementation in Eating Disorder |
| NCT01511835 | PHASE4 | UNKNOWN | Efficacy of Myo-inositol in Preventing Gestational Diabetes in High-risk Pregnant Women |
| NCT01514942 | PHASE4 | COMPLETED | Myo-inositol Versus D-chiro-inositol in the Treatment of Polycystic Ovary Syndrome and Insulin Resistance: Evaluation of Clinical, Metabolic, Endocrine and Ultrasound Parameters |
| NCT01540747 | PHASE4 | COMPLETED | Role of Melatonin Supplementation in Follicular Fluid of in Vitro Fertilization (IVF) Patients With Polycystic Ovarian Syndrome |
| NCT01560065 | PHASE4 | COMPLETED | Effect of Treatment With Myo-inositol on Human Semen Parameters in Patients Undergoing In Vitro Fertilization Cycles |
| NCT01583959 | PHASE4 | COMPLETED | Study of Different Doses of Folic Acid in Combination With Methotrexate in Rheumatoid Arthritis |
| NCT01608347 | PHASE4 | COMPLETED | Low Molecular Weight Heparin in Recurrent Miscarriage With Negative Antiphospholipid Antibodies |
| NCT01608750 | PHASE4 | UNKNOWN | The Efficacy of Pantoprazole Treatment in Patients With Functional Dyspepsia |
| NCT01626443 | PHASE4 | COMPLETED | Role of Myo-inositol and D-chiro Inositol on the Ovaric and Metabolic Functions |
| NCT01733329 | PHASE4 | COMPLETED | Buccal Misoprostol During Cesarean Section for Preventing Postpartum Hemorrhage |
| NCT01766310 | PHASE4 | COMPLETED | Effect of Folic Acid Supplementation on Plasma Homocysteine Level in Obese Children |
| NCT01871740 | PHASE4 | WITHDRAWN | CSPPT- Chronic Kidney Diseases Study |
| NCT02031289 | PHASE4 | COMPLETED | Impact of Preoperative Treatment of Anemia and Iron Deficiency in Cardiac Surgery on Outcome. |
| NCT02150291 | PHASE4 | UNKNOWN | A Pilot Study to Assess the Efficacy and Safety of Folic Acid and/or Vitamin B Complex on Hepatitis C Infected Patients Treated With Pegylated Interferon and Ribavirin. |
| NCT02300948 | PHASE4 | COMPLETED | Optimizing Periconceptional and Prenatal Folic Acid Supplementation |
| NCT02344888 | PHASE4 | UNKNOWN | Adding Prednisolone During Ovulation Induction With CC in Lean Women With CC Resistant PCOS |
| NCT02444013 | PHASE4 | UNKNOWN | Folic Acid for Prevention of Contrast Induced Nephropathy |
| NCT02644499 | PHASE4 | COMPLETED | Comparison of Combination Disease Modifying Antirheumatic Drugs With Methotrexate Therapy in Early Rheumatoid Arthritis |
| NCT03040219 | PHASE4 | UNKNOWN | Folic Acid Supplementation as an Appetizer in Primary Malnourished Egyptian Infants and Children |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
6 molecules share ≥1 primary target. Top 6 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| METHOTREXATE | ChEMBL + PubChem | Phase 4 (approved) | SLC19A1, SLC46A1 |
| PEMETREXED | ChEMBL + PubChem | Phase 4 (approved) | SLC19A1, SLC46A1 |
| PRALATREXATE | ChEMBL + PubChem | Phase 4 (approved) | SLC19A1, SLC46A1 |
| RALTITREXED | ChEMBL | Phase 4 (approved) | SLC19A1, SLC46A1 |
| Indomethacin | PubChem | Approved | SLC46A1 |
| Leucovorin | PubChem | Approved | SLC19A1 |
Related Atlas pages
- Genes: SLC19A1, SLC46A1
- Diseases: iron deficiency anemia, chronic kidney disease, anemia, osteoporosis, acne, depressive disorder, type 2 diabetes mellitus, epilepsy, heart disorder, rheumatoid arthritis, hypertensive disorder, malaria, non-small cell lung carcinoma, cleft lip, colorectal neoplasm, male infertility, cleft palate, gingival overgrowth, severe acute respiratory syndrome, Alzheimer disease, type 1 diabetes mellitus, neural tube defect, tuberculosis, premature ejaculation, systemic lupus erythematosus
- Drugs: Methotrexate, Pemetrexed, Pralatrexate, Raltitrexed, Indomethacin