Levocetirizine
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Also known as (-)-cetirizine(r)-cetirizineCetirizine (r)-formCetirizine, (-)-Cetirizine, (r)-LevocetirizinaXazalXyzalSID26719822SID49681558C0164915LEVOCETIRIZINE DIHYDROCHLORIDE
Summary
Levocetirizine (CHEMBL1201191) is an approved small molecule (ATC R06AE09) targeting HRH1; indicated across 12 conditions including allergic disease and allergic rhinitis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AE09
- Targets: 1 (HRH1)
- Indications: 12 conditions
- Clinical trials: 61
- Chemistry: 388.9 Da · C21H25ClN2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201191 |
| Name | Levocetirizine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 1549000 |
| ATC | R06AE09 |
| Molecular formula | C21H25ClN2O3 |
| Molecular weight | 388.9 |
| InChIKey | ZKLPARSLTMPFCP-OAQYLSRUSA-N |
SMILES: C1CN(CCN1CCOCC(=O)O)[C@H](C2=CC=CC=C2)C3=CC=C(C=C3)Cl
IUPAC name: 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid
Also known as: (-)-cetirizine, (r)-cetirizine, Cetirizine (r)-form, Cetirizine, (-)-, Cetirizine, (r)-, Levocetirizina, Levocetirizine, Xazal, Xyzal, SID26719822, SID49681558, LEVOCETIRIZINE
Parent form; salt/anhydrous children: CHEMBL1201190
Patent coverage: 2,492 distinct patent families (8,816 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 | Inverse agonist | 8.5 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Histamine H1 receptor.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 8.1 | Ki | 7.94 | nM | CHEMBL_ACT_29118532 |
| HRH1 | 8.1 | Kd | 7.94 | nM | CHEMBL_ACT_29118598 |
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 |
| allergic rhinitis | 3 | MONDO:0011786 | EFO:0005854 |
| urticaria | 3 | MONDO:0005492 | EFO:0005531 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
| seasonal allergic rhinitis | 3 | MONDO:0005324 | EFO:0003956 |
| vasomotor rhinitis | 3 | MONDO:0006004 | EFO:0007533 |
| rhinitis | 3 | MONDO:0003014 | EFO:0008521 |
| dermatitis | 3 | MONDO:0002406 | MONDO:0002406 |
| asthma | 3 | MONDO:0004979 | MONDO:0004979 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| diabetic kidney disease | 2 | MONDO:0005016 | EFO:0000401 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 61.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 22 |
| PHASE3 | 18 |
| PHASE1 | 10 |
| PHASE2 | 6 |
| Not specified | 4 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00150761 | PHASE4 | COMPLETED | Facial Thermography Study of Levocetirizine Versus Cetirizine |
| NCT00160537 | PHASE4 | COMPLETED | POPULAR (Preference Of Patient Using Levocetirizine in Allergic Rhinitis) |
| NCT00160589 | PHASE4 | COMPLETED | LEADER (LEvocetirizine And DEsloratadine in Allergic Rhinitis) |
| NCT00160680 | PHASE4 | COMPLETED | ATAREAL (Antihistamine Treatment for Allergic Rhinitis in Real Life) |
| NCT00264303 | PHASE4 | COMPLETED | CUTE (Chronic Urticaria Treatment Evaluation) |
| NCT00295022 | PHASE4 | COMPLETED | Compare the Efficacy of Levocetirizine and Montelukast to Placebo in Reducing Seasonal Allergic Rhinitis (SAR) Symptoms in Ragweed Sensitive Subjects |
| NCT00355771 | PHASE4 | COMPLETED | Levocetirizine 5 mg: Reduction of Symptoms, Airway Resistance and Sleep Impairment in Persistent Allergic Rhinitis |
| NCT00359138 | PHASE4 | COMPLETED | The Duration of the Suppressive Effects of Desloratadine on Allergen Prick Tests After Discontinuation (P04441) |
| NCT00439712 | PHASE4 | COMPLETED | Levocetirizine in the Treatment of Nasal Obstruction Due to Perennial Allergic Rhinitis |
| NCT00521131 | PHASE4 | COMPLETED | Evaluation of Efficacy and Safety of Levocetirizine to Subjects With Perennial Allergic Rhinitis to House Dust Mites |
| NCT00542607 | PHASE4 | COMPLETED | Efficacy and Safety of Levocetirizine and Fexofenadine in Reducing Symptoms of Seasonal Allergic Rhinitis |
| NCT00621959 | PHASE4 | COMPLETED | A Study Evaluating the Efficacy and Impact on Health-related Quality of Life of Levocetirizine in Adults With Seasonal Allergic Rhinitis |
| NCT00653224 | PHASE4 | COMPLETED | A Study Evaluating the Efficacy and Impact on Health-related Quality of Life of Levocetirizine in Adults With Seasonal Allergic Rhinitis |
| NCT00679250 | PHASE4 | COMPLETED | To Evaluate Adenosine Monophosphate and Allergen Challenge in Allergic Rhinitis |
| NCT00826943 | PHASE4 | COMPLETED | Is Levocetirizine Less Sedating Than Cetirizine? |
| NCT00894231 | PHASE4 | COMPLETED | Levocetirizine Effect on Nasal Nitric Oxide and Nasal Eosinophils in Subjects With Perennial Allergic Rhinitis |
| NCT01250652 | PHASE4 | COMPLETED | Levocetirizine Plus Bed-Time Hydroxyzine in the Management of Corticodependent Chronic Urticaria Versus Levocetirizine Alone in High Doses |
| NCT01430260 | PHASE4 | COMPLETED | Omnaris Versus Levocetirizine Phase 4 Study |
| NCT01496911 | PHASE4 | COMPLETED | Effects of Levocetirizine and Hydroxyzine on Cognitive and Psychomotor Functioning During Simulated Diving |
| NCT01586091 | PHASE4 | COMPLETED | Safety Study of Levocetirizine and Fexofenadine |
| NCT02507635 | PHASE4 | COMPLETED | Anti-inflammatory H1 Antihistamines Allergic Rhinitis |
| NCT03789422 | PHASE4 | UNKNOWN | Tranexamic Acid and Spontaneous Chronic Urticaria |
| NCT04699604 | PHASE3 | RECRUITING | A Histamine Pharmacodynamic Biomarker to Guide Treatment in Pediatric Asthma (HAS3) |
| NCT00152464 | PHASE3 | COMPLETED | Prevention of Asthma With Levocetirizine 18 Month Treatment in Infants (12 - 24 Months) Suffering From Eczema (Atopic Dermatitis) and Sensitized to Grass Pollen and/or House Dust Mite (HDM) |
| NCT00160563 | PHASE3 | TERMINATED | Prevention of Asthma With Levocetirizine (36 Month Treatment) in Young Children Suffering From Eczema (Atopic Dermatitis) and Sensitized to Grass Pollen and House Dust Mite and Having Completed the Previous EPAAC Trial (NCT00152464) |
| NCT00315523 | PHASE3 | COMPLETED | Compare the Efficacy of Levocetirizine to Montelukast in Reducing Symptoms of SAR in Sensitive Subjects Exposed to Ragweed Pollen |
| NCT00375713 | PHASE3 | COMPLETED | Randomized Phase III Study to Evaluate the Efficacy and Safety of Xyzal® (Levocetirizine) vs Zyrtec® (Cetirizine) in Subjects With Dermatitis and Eczema |
| NCT00421109 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Chronic Idiopathic Urticaria |
| NCT00524836 | PHASE3 | COMPLETED | Efficacy and Safety of Levocetirizine Versus Loratadine for the Treatment of Perennial Allergic Rhinitis |
| NCT00525278 | PHASE3 | COMPLETED | To Evaluate the Efficacy and Safety of Levocetirizine Versus Loratadine for Treatment of Seasonal Allergic Rhinitis |
| NCT00525382 | PHASE3 | COMPLETED | Study to Compare the Efficacy and Safety Between Levocetirizine and Loratadine for Chronic Idiopathic Urticaria |
| NCT00544388 | PHASE3 | COMPLETED | Efficacy of Levocetirizine and Cetirizine in Reducing Symptoms of Seasonal Allergic Rhinitis in Ragweed Sensitive Subjects |
| NCT00619801 | PHASE3 | COMPLETED | Safety Study of Levocetirizine Dihydrochloride Oral Liquid Formulation in Children Aged 1 to Less Than 6 Years Suffering From Allergic Rhinitis or Chronic Urticaria of Unknown Origin |
| NCT00628108 | PHASE3 | COMPLETED | Safety Study of Levocetirizine Dihydrochloride Oral Liquid Formulation in Children Aged 6 Months to 11 Months |
| NCT00789152 | PHASE3 | COMPLETED | The Effect of Desloratadine and Levocetirizine on Nasal Obstruction (Study P03609) |
| NCT01000792 | PHASE3 | COMPLETED | 3-D Visualization of the Anti-Obstructive Effect of Levocetirizine |
| NCT01392859 | PHASE2/PHASE3 | COMPLETED | Characterization of the Role of Histamine in Children With Asthma |
| NCT01509209 | PHASE3 | COMPLETED | Efficacy/Safety of Pseudoephedrine Plus Levocetirizine Versus Placebo in Patients With Vasomotor Rhinitis |
| NCT01563081 | PHASE3 | COMPLETED | Safety Study of Levocetirizine Oral Solution for Japanese Pediatrics |
| NCT01640535 | PHASE3 | COMPLETED | Efficacy and Safety of Concomitant Montelukast Sodium and Levocetirizine Dihydrochloride in Perennial Allergic Rhinitis (PAR) Patients |
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.
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, allergic rhinitis, urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, vasomotor rhinitis, rhinitis, dermatitis, 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, Chlordiazepoxide, Chlorpheniramine, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clotrimazole, Clozapine, Cyclizine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine