Cetirizine
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Also known as AC-170CetidermCetirizinacetirizinSID174007233C0165008CETERIZINE/ZYRTECCETERIZINECETIRIZINE HYDROCHLORIDE
Summary
Cetirizine (CHEMBL1000) is an approved small-molecule anti-allergic agent (ATC R06AE07) targeting HRH1; indicated across 18 conditions including eye allergy and allergic disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AE07 (+1 more)
- Targets: 1 (HRH1)
- Indications: 18 conditions
- Clinical trials: 77
- Chemistry: 388.9 Da · C21H25ClN2O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1000 |
| Name | Cetirizine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 2678 |
| ChEBI | CHEBI:3561 |
| ATC | R06AE07, S01GX12 |
| Molecular formula | C21H25ClN2O3 |
| Molecular weight | 388.9 |
| InChIKey | ZKLPARSLTMPFCP-UHFFFAOYSA-N |
SMILES: C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl
IUPAC name: 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid
ChEBI definition: A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.
Pharmacological roles (ChEBI): anti-allergic agent, H1-receptor antagonist.
Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.
Also known as: AC-170, Cetiderm, Cetirizina, Cetirizine, cetirizine, cetirizin, CETIRIZINE, SID174007233, C0165008, CETERIZINE/ZYRTEC, CETERIZINE, CETIRIZINE HYDROCHLORIDE
Parent form; salt/anhydrous children: CHEMBL1201113, CHEMBL1607273
Patent coverage: 7,389 distinct patent families (26,030 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 | 8.2 | 0% | P35367 |
Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Histamine H2 receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, Sodium-dependent serotonin transporter, Histamine H1 receptor, D(3) dopamine receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, Angiopoietin-1 receptor.
Bioactivity
ChEMBL activities: 17 potent at pChembl ≥ 5 of 24 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HRH1 | 8.23 | Ki | 5.89 | nM | CHEMBL_ACT_1420594 |
| HRH1 | 7.85 | Ki | 14 | nM | CHEMBL_ACT_1455410 |
| HRH1 | 7.85 | Ki | 14 | nM | CHEMBL_ACT_1618035 |
| HRH1 | 7.85 | Ki | 14 | nM | CHEMBL_ACT_934456 |
| HRH1 | 7.5 | Ki | 31.62 | nM | CHEMBL_ACT_3418281 |
| HRH1 | 7.5 | Ki | 31.62 | nM | CHEMBL_ACT_3418282 |
| HRH1 | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_3418279 |
| HRH1 | 7.3 | Ki | 50.12 | nM | CHEMBL_ACT_3418280 |
| HRH1 | 7.2 | Ki | 63.1 | nM | CHEMBL_ACT_3418284 |
| HRH1 | 7.2 | Ki | 63.1 | nM | CHEMBL_ACT_3418285 |
| HRH1 | 7.11 | AC50 | 78 | nM | CHEMBL_ACT_25212099 |
| HRH1 | 7.1 | Ki | 79.43 | nM | CHEMBL_ACT_3418283 |
| HRH2 | 5.73 | AC50 | 1851 | nM | CHEMBL_ACT_25114347 |
| HTR2A | 5.67 | AC50 | 2118 | nM | CHEMBL_ACT_25173473 |
| HTR2B | 5.05 | AC50 | 8927 | nM | CHEMBL_ACT_25164004 |
| SLC6A3 | 5.04 | AC50 | 9181 | nM | CHEMBL_ACT_25124761 |
| SLC6A4 | 5.03 | AC50 | 9313 | nM | CHEMBL_ACT_25151129 |
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
18 indications (2 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 |
|---|---|---|---|
| eye allergy | 4 | MONDO:0005551 | EFO:0005751 |
| allergic disease | 4 | MONDO:0005271 | MONDO:0005271 |
| seasonal allergic rhinitis | 3 | MONDO:0005324 | EFO:0003956 |
| allergic rhinitis | 3 | MONDO:0011786 | EFO:0005854 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
| atopic conjunctivitis | 3 | MONDO:0005642 | EFO:0007141 |
| dermatitis | 3 | MONDO:0002406 | MONDO:0002406 |
| pemphigus | 3 | MONDO:0006594 | EFO:1000749 |
| multiple sclerosis | 3 | MONDO:0005301 | MONDO:0005301 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| rhinitis | 2 | MONDO:0003014 | EFO:0008521 |
| androgenetic alopecia | 2 | MONDO:0005339 | EFO:0004191 |
| neuromyelitis optica | 1 | MONDO:0019100 | EFO:0004256 |
| migraine disorder | 1 | MONDO:0005277 | MONDO:0005277 |
| glycogen storage disease III | 1 | MONDO:0009291 | MONDO:0009291 |
| burn | 1 | MONDO:0043519 | EFO:0009516 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 77.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 22 |
| PHASE3 | 20 |
| PHASE1 | 13 |
| PHASE2 | 10 |
| Not specified | 7 |
| PHASE2/PHASE3 | 2 |
| PHASE1/PHASE2 | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00488176 | PHASE4 | UNKNOWN | Comparison of the Effect of Montelukast and Cetirizine on Allergic Inflammation in Children With Allergic Rhinitis |
| NCT00561717 | PHASE4 | COMPLETED | A Randomized, Placebo Controlled Study to Determine the Efficacy and Speed of a Nasal Spray in Allergen Induced Seasonal Allergic Rhinitis |
| NCT00751166 | PHASE4 | TERMINATED | A Comparative Double-blind, Double-dummy Study of Desloratadine (DL) 5 mg Once Daily, Cetirizine 10 mg Once Daily, and Placebo Once Daily in Patients With Chronic Idiopathic Urticaria (Study P03736) |
| NCT00751218 | PHASE4 | COMPLETED | A Comparative Double-Blind, Double- Dummy Study of Desloratadine (DL) 5 MG Once Daily, Cetirizine 10 MG Once Daily, and Placebo Once Daily in Patients With Chronic Idiopathic Urticaria (Study P03735) |
| NCT00794495 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03181) |
| NCT00794599 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03182) |
| NCT00794846 | PHASE4 | COMPLETED | Preference for Clarinex Tablets vs. Zyrtec Tablets in Patients With Allergies (P03180) |
| NCT00826943 | PHASE4 | COMPLETED | Is Levocetirizine Less Sedating Than Cetirizine? |
| NCT01781507 | PHASE4 | COMPLETED | Study of Bronchodilation Effects of Cetirizine |
| NCT01825655 | PHASE4 | TERMINATED | Study of Using Long Acting Antihistamine to Treat Opioid Induced Itching |
| NCT01916226 | PHASE4 | COMPLETED | A Comparator Study of Fluticasone Propionate Nasal Spray Verses (vs) Cetirizine in the Treatment of Seasonal Allergic Rhinitis |
| NCT01940393 | PHASE4 | COMPLETED | Evaluation of the Inhibitory Effect of 5 Anti-Histamines in Urticaria |
| NCT01985789 | PHASE4 | COMPLETED | Anti-histamines and Methacholine Challenges. |
| NCT02205489 | PHASE4 | COMPLETED | Management Of The Infusion-Associated Reactions In RRMS Patients Treated With LEMTRADA |
| NCT02543346 | PHASE4 | COMPLETED | Comparability and Standardization of Controlled Allergen Challenge Facilities |
| NCT02932774 | PHASE4 | COMPLETED | Randomized, Double Blind, Parallel Group, Placebo Controlled, Multi-Center Study of the Efficacy and Safety of Cetirizine HCl Syrup vs. Loratadine Syrup vs. Placebo in Treatment of Children With Seasonal Allergic Rhinitis (SAR) |
| NCT03047278 | PHASE4 | COMPLETED | Transporters for Organic Cations and Glycemic Control in Patients With Neuropathic Pain. |
| NCT03192488 | PHASE4 | COMPLETED | Effect of an H1 Receptor Antagonist on Exercise Performance in Hypoxia |
| NCT03340740 | PHASE4 | COMPLETED | The Effect of Cetirizine on Bronchoconstriction |
| NCT04293822 | PHASE4 | UNKNOWN | Topical Cetirizine 1% vs Minoxidil 5% Gel in Treatment of Androgenetic Alopecia |
| NCT04836806 | PHASE4 | WITHDRAWN | Cetirizine and Famotidine for COVID-19 |
| NCT06019728 | PHASE4 | COMPLETED | A Prospective Study to Investigate Safety and Tolerability of Shorter Infusion of Fabrazyme |
| NCT06819774 | PHASE3 | RECRUITING | Phase III Clinical Study of Cetirizine Hydrochloride Injection in Treatment of Acute Urticaria |
| NCT07472413 | PHASE3 | NOT_YET_RECRUITING | Alternate Pre-med in Anti-Cluster of Differentiation 20 (CD20) Pilot Project |
| 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 |
| NCT00490204 | PHASE3 | COMPLETED | Cetirizine Placebo Controlled Study For Perennial Allergic Rhinitis |
| NCT00504933 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Seasonal Allergic Rhinitis |
| NCT00639587 | PHASE3 | COMPLETED | Efficacy and Safety of Cetirizine Tablets Versus Ketotifen Dry Syrup in Children With Perennial Allergic Rhinitis |
| NCT00794378 | PHASE3 | COMPLETED | Taste Test Between Desloratadine and Cetirizine Syrup in Children (Study P03829)(COMPLETED) |
| NCT00794794 | PHASE3 | COMPLETED | Taste Test Between Desloratadine and Cetirizine Syrup in Children (Study P03826) |
| NCT00974571 | PHASE3 | COMPLETED | Montelukast in Perennial Allergic Rhinitis - 2001-2002 Study (0476-246) |
| NCT01127620 | PHASE3 | COMPLETED | Efficacy Study for the Symptomatic Treatment of Perennial Allergic Rhinitis With a 1 Year Safety Extension |
| NCT01332188 | PHASE2/PHASE3 | COMPLETED | Efficacy of AC-170 for the Treatment of Allergic Conjunctivitis in the Conjunctival Allergen Challenge (CAC) Model |
| NCT01484119 | PHASE3 | COMPLETED | Efficacy, Safety, and Tolerability Study of ACT-129968 in Patients With Seasonal Allergic Rhinitis |
| NCT01551056 | PHASE3 | COMPLETED | A Multi-Center Study Evaluating the Onset and Duration of Action of AC-170 0.24% Compared to Vehicle in the Conjunctival Allergen Challenge (CAC) |
| NCT01685242 | PHASE3 | COMPLETED | A Single-Center,Evaluation of the Onset and Duration of Action of AC-170 0.24% Compared to Vehicle |
| NCT01881113 | PHASE3 | COMPLETED | A Multi-Center, Evaluation of the Onset and Duration of Action of AC-170 0.24% Compared to Vehicle |
| NCT02132169 | PHASE3 | COMPLETED | A Multi-Center Study Evaluating the Safety of AC-170 0.24% |
| NCT02756624 | PHASE3 | COMPLETED | A Multi-Center, Vehicle-Controlled, Parallel-Group Study Evaluating the Safety of AC-170 Ophthalmic Solution |
| NCT03368664 | PHASE3 | TERMINATED | A Study to Evaluate Efficacy, Safety, and Tolerability of Alemtuzumab in Pediatric Patients With RRMS With Disease Activity on Prior DMT |
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.
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 |
| 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 |
| DEXBROMPHENIRAMINE | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1
- Diseases: eye allergy, allergic disease, seasonal allergic rhinitis, allergic rhinitis, perennial allergic rhinitis, atopic conjunctivitis, dermatitis, pemphigus, multiple sclerosis, severe acute respiratory syndrome
- 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, Dexbrompheniramine