Fexofenadine
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Also known as FexofenadinaTelfastSID50105687SID90341422FEXOFENADINE HYDROCHLORIDE
Summary
Fexofenadine (CHEMBL914) is an approved small-molecule H1-receptor antagonist (ATC R06AX26) targeting HRH1; indicated across 12 conditions including allergic disease and seasonal allergic rhinitis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AX26
- Targets: 1 (HRH1)
- Indications: 12 conditions
- Clinical trials: 64
- Chemistry: 501.7 Da · C32H39NO4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL914 |
| Name | Fexofenadine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 3348 |
| ChEBI | CHEBI:5050 |
| ATC | R06AX26 |
| Molecular formula | C32H39NO4 |
| Molecular weight | 501.7 |
| InChIKey | RWTNPBWLLIMQHL-UHFFFAOYSA-N |
SMILES: CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O
IUPAC name: 2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid
ChEBI definition: A piperidine-based anti-histamine compound.
Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent.
Also known as: Fexofenadina, Fexofenadine, Telfast, fexofenadine, SID50105687, SID90341422, FEXOFENADINE, FEXOFENADINE HYDROCHLORIDE
Parent form; salt/anhydrous children: CHEMBL1200618
Patent coverage: 7,517 distinct patent families (28,893 SureChEMBL compound mentions), from 1 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 |
|---|---|---|---|---|---|
| HRH1 | H1 receptor | Antagonist | 7.57 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Prelamin-A/C, RecQ-like DNA helicase BLM, 5-hydroxytryptamine receptor 2B, Cannabinoid receptor 1, 5-hydroxytryptamine receptor 2A, Histamine H1 receptor, D(3) dopamine receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4A.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| BLM | 8.05 | Potency | 8.9 | nM | CHEMBL_ACT_4753923 |
| BLM | 8.05 | Potency | 8.9 | nM | CHEMBL_ACT_4945854 |
| HRH1 | 7.82 | IC50 | 15 | nM | CHEMBL_ACT_15240063 |
| HRH1 | 7.57 | Ki | 27 | nM | CHEMBL_ACT_3001661 |
| HRH1 | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_2681927 |
| HRH1 | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_2681966 |
| HRH1 | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_6198203 |
| HRH1 | 6.92 | AC50 | 120 | nM | CHEMBL_ACT_25212985 |
| LMNA | 6.8 | Potency | 158.5 | nM | CHEMBL_ACT_3663967 |
| HTR2B | 5.24 | AC50 | 5788 | nM | CHEMBL_ACT_25227966 |
| HTR2A | 5.08 | AC50 | 8320 | nM | CHEMBL_ACT_25173767 |
Target pathways
Aggregated over 1 target gene(s): HRH1.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Histamine receptors | 1 | HRH1 |
| G alpha (q) signalling events | 1 | HRH1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| inflammatory response | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| chemical synaptic transmission | 1 |
| memory | 1 |
| visual learning | 1 |
| regulation of vascular permeability | 1 |
| positive regulation of vasoconstriction | 1 |
| regulation of synaptic plasticity | 1 |
| cellular response to histamine | 1 |
| signal transduction | 1 |
| phospholipase C-activating serotonin receptor signaling pathway | 1 |
Indications & clinical
Indications
12 indications (1 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 |
|---|---|---|---|
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
| seasonal allergic rhinitis | 3 | MONDO:0005324 | EFO:0003956 |
| diabetic kidney disease | 3 | MONDO:0005016 | EFO:0000401 |
| asthma | 3 | MONDO:0004979 | MONDO:0004979 |
| atopic eczema | 2 | MONDO:0004980 | EFO:0000274 |
| gastroesophageal reflux disease | 2 | MONDO:0007186 | EFO:0003948 |
| perennial allergic rhinitis | 2 | MONDO:0024332 | EFO:1001417 |
| non-small cell lung carcinoma | 1 | MONDO:0005233 | EFO:0003060 |
| rheumatoid arthritis | 1 | MONDO:0008383 | EFO:0000685 |
| prostate adenocarcinoma | 1 | MONDO:0005082 | EFO:0000673 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 64.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 22 |
| PHASE1 | 20 |
| PHASE3 | 8 |
| PHASE2 | 5 |
| Not specified | 4 |
| PHASE2/PHASE3 | 3 |
| PHASE1/PHASE2 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00261079 | PHASE4 | COMPLETED | Fexofenadine in Pruritic Skin Disease |
| NCT00435461 | PHASE4 | COMPLETED | Fluticasone Furoate Nasal Spray Versus Oral Fexofenadine |
| NCT00502775 | PHASE4 | COMPLETED | Fluticasone Furoate Nasal Spray Versus Oral Fexofenadine |
| NCT00636870 | PHASE4 | COMPLETED | Fexofenadine (Allegra®) in Healthy Adults Who Have Been Identified as Slow Metabolizers for Desloratadine |
| NCT00637585 | PHASE4 | COMPLETED | Fexofenadine HCl 180 mg, Desloratadine 5 mg and Placebo in Suppression of Wheal and Flare Induced by Histamine |
| NCT00638118 | PHASE4 | COMPLETED | Fexofenadine HCl 180 mg, Montelukast Sodium 10 mg and Placebo in Suppression of Wheal and Flare Induced by Seasonal Allergen |
| NCT00741897 | PHASE4 | COMPLETED | Fexofenadine Study On Filipino Children for The Relief of Perennial And Intermittent Allergic Rhinitis |
| NCT00783133 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs. Allegra Tablets in Patients With Seasonal Allergies (Study P03177) |
| NCT00783146 | PHASE4 | COMPLETED | Efficacy and Safety of Desloratadine vs. Fexofenadine 180 mg. vs. Placebo for Treating Seasonal Allergic Rhinitis (SAR) (Study P04054) |
| NCT00783211 | PHASE4 | COMPLETED | Efficacy and Safety of Desloratadine vs. Fexofenadine 180 mg. vs. Placebo for Treating Seasonal Allergic Rhinitis (SAR)(Study P04053)(COMPLETED) |
| NCT00794248 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs. Allegra Tablets in Patients With Seasonal Allergies (Study P03179) |
| NCT00794768 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs Allegra Tablets in Patients With Seasonal Allergies (P03178) |
| NCT01469234 | PHASE4 | COMPLETED | A Study of Onset of Action of Loratadine and Fexofenadine in Participants With Seasonal Allergic Rhinitis (P08712) |
| NCT01940393 | PHASE4 | COMPLETED | Evaluation of the Inhibitory Effect of 5 Anti-Histamines in Urticaria |
| NCT02175485 | PHASE4 | COMPLETED | Evaluation of Efficacy of Dellegra in Exposure Unit |
| NCT02551536 | PHASE4 | COMPLETED | Montelukast and Fexofenadine Versus Montelukast and Levocetrizine Combination in Allergic Rhinitis |
| NCT03078777 | PHASE4 | UNKNOWN | The Effect Dialysis on the Pharmacokinetics of Fexofenadine |
| NCT03933007 | PHASE4 | TERMINATED | Relation Between Blood Concentration of Colchicine and Response to Colchicine Treatment in Gout Flare |
| NCT03994731 | PHASE4 | COMPLETED | Study of KRYSTEXXA® (Pegloticase) Plus Methotrexate in Participants With Uncontrolled Gout |
| NCT05720455 | PHASE4 | COMPLETED | Study to Assess Safety and Efficacy of Fexofenadine Hydrochloride (HCL) + Pseudoephedrine HCL Fixed Dose Combination in Indian Male and Female Participants With Allergic Rhinitis (AR) Who Are 12 Years and Above |
| NCT06019728 | PHASE4 | COMPLETED | A Prospective Study to Investigate Safety and Tolerability of Shorter Infusion of Fabrazyme |
| NCT06466421 | PHASE4 | COMPLETED | Fexofenadine Versus Gabapentin for Uremic Pruritus in Patients on Regular Hemodialysis |
| NCT04688788 | PHASE3 | ACTIVE_NOT_RECRUITING | Non-inferiority Study of Ocrelizumab and Rituximab in Active Multiple Sclerosis |
| NCT06785298 | PHASE2/PHASE3 | RECRUITING | Fexofenadine as Adjuvant Therapy in Parkinson Disease |
| NCT00044811 | PHASE3 | COMPLETED | Efficacy and Safety of Fexofenadine in Mild to Moderate Persistent Asthma |
| NCT00044824 | PHASE3 | COMPLETED | Efficacy and Safety of Fexofenadine in Mild to Moderate Persistent Asthma |
| NCT00045955 | PHASE3 | COMPLETED | Long-Term Safety Performance of Fexofenadine in Asthma |
| NCT01244217 | PHASE2/PHASE3 | COMPLETED | Safety, Efficacy and Pharmacokinetic Study of Allegra in Pediatric Patients With Perennial Allergic Rhinitis (PAR) |
| NCT01244230 | PHASE2/PHASE3 | COMPLETED | Safety, Efficacy and Pharmacokinetic Study of Allegra in Pediatric Patients With Atopic Dermatitis (AD) |
| NCT01306721 | PHASE3 | COMPLETED | Fexofenadine HCL - Pseudoephedrine HCL Combination Versus Allegra in Patients With Seasonal Allergic Rhinitis |
| NCT03664882 | PHASE3 | COMPLETED | Study Evaluating the Efficacy and Safety of Fexofenadine in Subjects Suffering From Seasonal Allergic Rhinitis in Presence of Pollutants |
| NCT04224428 | PHASE3 | COMPLETED | Role of Fexofenadine in Diabetic Kidney Disease |
| NCT05692154 | PHASE3 | COMPLETED | A Placebo-controlled Study of 2-day Pre-treatment With Fexofenadine in Seasonal Allergic Rhinitis |
| NCT05264025 | PHASE1/PHASE2 | RECRUITING | Fexofenadine in Patients With Active Rheumatoid Arthritis |
| NCT07526558 | PHASE2 | NOT_YET_RECRUITING | Mast Cell Treatment in Post-tick Bite Illness (PTBI) |
| NCT00420082 | PHASE2 | COMPLETED | A Randomized, Double-Blind, 4-way Crossover Study to Evaluate the Efficacy of Bilastine in the Vienna Challenge Chamber |
| NCT01172522 | PHASE2 | COMPLETED | Topical Treatment of Under Eye Dark Circles and Swelling |
| NCT01683552 | PHASE2 | COMPLETED | Aprepitant in the Management of Biological Therapies-related Severe Pruritus |
| NCT03425097 | PHASE2 | TERMINATED | Fexofenadine Use in Gastroesophageal Reflux Symptoms |
| NCT02966665 | PHASE1 | RECRUITING | : Vascular Function in Health and Disease |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
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.
295 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACLIDINIUM BROMIDE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DESLORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PALIPERIDONE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| PRAMIPEXOLE | ChEMBL + PubChem | Phase 4 (approved) | HRH1 |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | HRH1 |
| ACETOPHENAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ACRIVASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMISULPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMOXAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASENAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| ATOMOXETINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZATADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| AZELASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | HRH1 |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BENZTROPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | HRH1 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | HRH1 |
| BIPERIDEN | ChEMBL | Phase 4 (approved) | HRH1 |
| BREXPIPRAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | HRH1 |
| BROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUPROPION | ChEMBL | Phase 4 (approved) | HRH1 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | HRH1 |
| BUTRIPTYLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CABERGOLINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CAPTOPRIL | ChEMBL | Phase 4 (approved) | HRH1 |
| CARBINOXAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CARIPRAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CETIRIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORDIAZEPOXIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPHENTERMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | HRH1 |
| CINACALCET | ChEMBL | Phase 4 (approved) | HRH1 |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | HRH1 |
| CITALOPRAM | ChEMBL | Phase 4 (approved) | HRH1 |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOFAZIMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOMIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYPROHEPTADINE | ChEMBL | Phase 4 (approved) | HRH1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | HRH1 |
| DESIPRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Diseases: allergic disease, seasonal allergic rhinitis, diabetic kidney disease, asthma
- Drugs: Aclidinium Bromide, Desloratadine, Dihydroergotamine, Paliperidone, Pramipexole, Abemaciclib, Acetophenazine, Acrivastine, Amiodarone, Amisulpride, Amitriptyline, Amoxapine, Amsacrine, Antazoline, Apomorphine, Aripiprazole, Asenapine, Astemizole, Atomoxetine, Azatadine, Azelastine, Benfluorex, Benperidol, Benzbromarone, Benztropine, Bepridil, Betamethasone Phosphoric Acid, Biperiden, Brexpiprazole, Bromperidol, Brompheniramine, Buclizine, Bupropion, Buspirone, Butriptyline, Cabergoline, Candesartan Cilexetil, Captopril, Carbinoxamine, Cariprazine, Cetirizine, Chlordiazepoxide, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine