Citric Acid
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Also known as Acidum citricumAcidum citricum monohydrateAcilettenAnhydrous citric acidB1650CitrateCitric acid anhydrousCitric acid bpCitric acid component of clenpiqCitric acid component of phexxiCitric acid component of prepopikCitric acid component of renacidinCitric acid hydrateCitric acid monoglycerideanhydroushydrousCitricum acidumE-330E330
Summary
Citric Acid (CHEMBL1261) is an approved small-molecule chelator (ATC A09AB04) targeting PKD2L1 and TRPV4; indicated across 6 conditions including kidney failure and nephrocalcinosis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A09AB04
- Targets: 2 (PKD2L1, TRPV4)
- Indications: 6 conditions
- Clinical trials: 52
- Chemistry: 192.12 Da · C6H8O7
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1261 |
| Name | Citric Acid |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 311 |
| ChEBI | CHEBI:30769 |
| ATC | A09AB04 |
| Molecular formula | C6H8O7 |
| Molecular weight | 192.12 |
| InChIKey | KRKNYBCHXYNGOX-UHFFFAOYSA-N |
SMILES: C(C(=O)O)C(CC(=O)O)(C(=O)O)O
IUPAC name: 2-hydroxypropane-1,2,3-tricarboxylic acid
ChEBI definition: A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms.
Pharmacological roles (ChEBI): chelator, antimicrobial agent, calcium chelator.
Other ChEBI roles (chemical / environmental): food acidity regulator, fundamental metabolite.
Also known as: Acidum citricum, Acidum citricum monohydrate, Aciletten, Anhydrous citric acid, B1650, Citrate, Citric acid, Citric acid anhydrous, Citric acid bp, Citric acid component of clenpiq, Citric acid component of phexxi, Citric acid component of prepopik
Parent form; salt/anhydrous children: CHEMBL2107737
Patent coverage: 709,560 distinct patent families (1,859,420 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,856,402 (100%) of the total. 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 |
|---|---|---|---|---|---|
| PKD2L1 | TRPP2 | Agonist | 1.7 | 0% | Q9P0L9 |
| TRPV4 | TRPV4 | Agonist | 5.6 | 0.6% | Q9HBA0 |
Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Aldehyde dehydrogenase 1A1, 3-dehydroquinate dehydratase, 3-dehydroquinate dehydratase.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| Q48255 | 5.6 | Kd | 2500 | nM | CHEMBL_ACT_1681145 |
| P15474 | 5.14 | Kd | 7300 | nM | CHEMBL_ACT_1681148 |
Target pathways
Aggregated over 2 target gene(s): PKD2L1, TRPV4.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| TRP channels | 1 | TRPV4 |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 1 | TRPV4 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| monoatomic ion transport | 2 |
| calcium ion transport | 2 |
| monoatomic ion transmembrane transport | 2 |
| calcium ion transmembrane transport | 2 |
| detection of chemical stimulus involved in sensory perception of sour taste | 1 |
| monoatomic cation transport | 1 |
| smoothened signaling pathway | 1 |
| response to water | 1 |
| sodium ion transmembrane transport | 1 |
| detection of chemical stimulus involved in sensory perception of taste | 1 |
| sensory perception of sour taste | 1 |
| detection of mechanical stimulus | 1 |
| protein homotetramerization | 1 |
| cellular response to acidic pH | 1 |
| potassium ion transmembrane transport | 1 |
Indications & clinical
Indications
6 indications (0 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 |
|---|---|---|---|
| kidney failure | 3 | MONDO:0001106 | HP:0000083 |
| nephrocalcinosis | 3 | MONDO:0001567 | HP:0000121 |
| nephrolithiasis | 2 | MONDO:0008171 | EFO:0004253 |
| cataract | 2 | MONDO:0005129 | MONDO:0005129 |
| osteoarthritis | 1 | MONDO:0005178 | MONDO:0005178 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 52.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 19 |
| PHASE4 | 10 |
| PHASE3 | 7 |
| PHASE2 | 5 |
| PHASE1 | 5 |
| EARLY_PHASE1 | 3 |
| PHASE2/PHASE3 | 2 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06580366 | PHASE4 | NOT_YET_RECRUITING | Comparing Sennosid A+B and Sodium Picosulfate/Magnesium Oxide/Citric Acid for Bowel Preparation |
| NCT07518303 | PHASE4 | NOT_YET_RECRUITING | Nafamostat Mesylate Versus Regional Citrate Anticoagulation for Continuous Renal Replacement Therapy in Sepsis-Associated Acute Kidney Injury |
| NCT00718289 | PHASE4 | COMPLETED | Citrate- Versus Acetate-Based Dialysate in Bicarbonate Haemodialysis: Consequences on Haemodynamics, Coagulation, Acid-Base Status and Electrolytes |
| NCT01329042 | PHASE4 | COMPLETED | Efficacy of Potassium Sodium Hydrogen Citrate Therapy on Renal Stone Recurrence and/or Residual Fragments After Shockwave Lithotripsy and Percutaneous Nephrolithotomy in Calcium Oxalate Urolithiasis |
| NCT01481714 | PHASE4 | UNKNOWN | Efficacy and Safety of Split-dose Citrafleet Administered From 2 to 6 Hours Before Morning Colonoscopies |
| NCT01711437 | PHASE4 | UNKNOWN | Different Bowel Preparations for Colonoscopy In Children |
| NCT02669589 | PHASE4 | COMPLETED | Investigating Different Anticoagulants for Renal Replacement Therapy |
| NCT02860299 | PHASE4 | COMPLETED | Biological and Clinical Measurements Following Systemic Leakage When a Citrate or Heparin Lock is Used |
| NCT03769402 | PHASE4 | COMPLETED | The Influence of Citric Acid Bone Surface Etching and Bone Defect Fill on GCF BMP-2 Release Profile |
| NCT06807905 | PHASE4 | COMPLETED | Efficiency and Biocompatibility in Hemodiafiltration Procedure |
| NCT05918029 | PHASE2/PHASE3 | RECRUITING | Bone in CKD Alkali Response (BICARb Pilot Trial) |
| NCT07601048 | PHASE3 | NOT_YET_RECRUITING | A Trial of HRS-7058 in Advanced or Metastatic Non-Small Cell Lung Cancer Patients Who Have Failed Standard Treatment |
| NCT00249951 | PHASE3 | COMPLETED | Alkaline Citrate Treatment to Lower the Risk of Nephrocalcinosis in Preterm Infants |
| NCT00749619 | PHASE3 | COMPLETED | Addition of Heparin to Taurolock-TM CLS in HD Patients With TCC Dose it Improve Catheter Patency Problems ? |
| NCT01012349 | PHASE2/PHASE3 | UNKNOWN | Efficacy and Safety Clinical Trial of the Combination of Acetylsalicylic Acid, Sodium Bicarbonate and Citric Acid, Produced by Geolab Pharmaceutical Industries Ltd., Compared to Acetylsalicylic Acid (Aspirin ® - Bayer) in Patients With Episodic Tension-type Headache. |
| NCT01820962 | PHASE3 | TERMINATED | Concentrated Citrate Locking to Reduce the Incidence of CVC-related Complications in Hematological Patients |
| NCT01962116 | PHASE3 | COMPLETED | Citrate Versus Heparin for the Lock of Non-tunneled Hemodialysis Catheters in Patients Hospitalised in ICU |
| NCT03017235 | PHASE3 | COMPLETED | A Study Comparing the Sodium Picosulfate, Magnesium Oxide and Anhydrous Citric Acid Oral Solution With PREPOPIK® for Colon Cleansing in Preparation for Colonoscopy |
| NCT05814341 | PHASE3 | COMPLETED | Citrate Anticoagulation in Renal Replacement Therapy: Impact of a High Post-filter Calcium Target on Efficacy |
| NCT07140874 | PHASE2 | RECRUITING | Zinc as an Adjunctive Therapy for Cervical Dystonia |
| NCT01074918 | PHASE1/PHASE2 | WITHDRAWN | Potassium-Magnesium Citrate as a Blood Pressure Lowering Agent in Hypertensive Patients |
| NCT01754779 | PHASE2 | COMPLETED | Treatment for Calcium Phosphate Kidney Stone Disease |
| NCT03114722 | PHASE2 | UNKNOWN | Citrate 4% Versus Heparinised Saline in Preventing Peripherally Inserted Central Catheter (PICC) Occlusions |
| NCT03116945 | PHASE2 | UNKNOWN | Novel Gallium Imaging in Hepatocellular Carcinoma |
| NCT04395768 | PHASE2 | UNKNOWN | International ALLIANCE Study of Therapies to Prevent Progression of COVID-19 |
| NCT00645879 | PHASE1 | COMPLETED | Anaplerotic Therapy in Propionic Acidemia |
| NCT00698425 | PHASE1 | COMPLETED | Safety and Tolerability Study of Transscleral Iontophoresis by the EyeGate® II Drug Delivery Device System |
| NCT01291069 | PHASE1 | COMPLETED | Effect of Tadalafil on Exercise Capacity in Pediatric Fontan Patients |
| NCT01421160 | PHASE1 | WITHDRAWN | Regulating Urine pH Levels to Alleviate Chronic Joint Pain |
| NCT05154968 | PHASE1 | COMPLETED | A Study of Two Formulations (Both Refrigerated and Room Temperature) Using an Autoinjector Device in Healthy Participants |
| NCT02391025 | EARLY_PHASE1 | COMPLETED | Gallium-68 Citrate PET Used in Prostate Cancer |
| NCT04361175 | EARLY_PHASE1 | UNKNOWN | Cost Effectiveness Analysis for Induction of Ovulation in the Polycystic Ovary Syndrome by Letrozole Versus Clomiphene Citrate |
| NCT06778733 | EARLY_PHASE1 | COMPLETED | Effectiveness of Low Dose Gonadotropin Stimulation Protocol Vs High Dose Gonadotropin Protocol in Poor Responders |
| NCT07536568 | Not specified | RECRUITING | Sublingual Caffeine on Reducing Recovery Time and Postoperative Agitation in Elderly Patients Undergoing General Anesthesia |
| NCT07567963 | Not specified | NOT_YET_RECRUITING | Magnesium Supplementation as a Nutritional Intervention in Sarcopenia |
| NCT00862966 | Not specified | UNKNOWN | Central Venous Catheter Lock Solution |
| NCT01576627 | Not specified | COMPLETED | Zinc Absorption From Zinc Citrate, Zinc Gluconate and Zinc Oxide |
| NCT01951300 | Not specified | COMPLETED | 68Ga-Citrate PET of Healthy Volunteers |
| NCT02194569 | Not specified | COMPLETED | Magnesium Balance of Citrate-based Continuous Venovenous Hemofiltration, Effect of Citrate Dose. |
| NCT02269306 | Not specified | COMPLETED | Predictors of Ovarian Response During Clomiphene Citrate Ovulation Induction in Patients With Polycystic Ovary Syndrome |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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.
5 molecules share ≥1 primary target. Top 5 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CANNABINOL | ChEMBL | Phase 3 | TRPV4 |
| CANNABIDIVARIN | ChEMBL | Phase 2 | TRPV4 |
| CANNABIGEROL | ChEMBL | Phase 2 | TRPV4 |
| GSK2798745 | ChEMBL | Phase 2 | TRPV4 |
| TETRAHYDROCANNABIVARIN | ChEMBL | Phase 2 | TRPV4 |
Related Atlas pages
- Genes: PKD2L1, TRPV4
- Diseases: kidney failure, nephrocalcinosis
- Drugs: Cannabinol