Rupatadine
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Also known as RupatadinaUR-12592RUPATADINE FUMARATERupatadine fumarateÊRupatadine fumarateÂ
Summary
Rupatadine (CHEMBL91397) is an approved small molecule (ATC R06AX28) targeting HRH1 and PTAFR; indicated across 5 conditions including allergic disease and urticaria.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R06AX28
- Targets: 2 (HRH1, PTAFR)
- Indications: 5 conditions
- Clinical trials: 13
- Chemistry: 416 Da · C26H26ClN3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL91397 |
| Name | Rupatadine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 133017 |
| ATC | R06AX28 |
| Molecular formula | C26H26ClN3 |
| Molecular weight | 416 |
| InChIKey | WUZYKBABMWJHDL-UHFFFAOYSA-N |
SMILES: CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2
IUPAC name: 13-chloro-2-[1-[(5-methyl-3-pyridinyl)methyl]piperidin-4-ylidene]-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
Also known as: Rupatadina, Rupatadine, UR-12592, RUPATADINE, RUPATADINE FUMARATE, Rupatadine fumarateÊ, Rupatadine Fumarate, Rupatadine fumarateÂ
Patent coverage: 701 distinct patent families (2,155 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 2,089 (97%) 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 |
|---|---|---|---|---|---|
| HRH1 | H1 receptor | Antagonist | 7 | 0% | P35367 |
| PTAFR | PAF receptor | Antagonist | 5.43 | 0.1% | P25105 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Histamine H1 receptor, Platelet-activating factor receptor.
Bioactivity
ChEMBL activities: 3 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 |
|---|---|---|---|---|---|
| HRH1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_1618361 |
| HRH1 | 8.4 | Ki | 3.98 | nM | CHEMBL_ACT_19095446 |
| PTAFR | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_1618360 |
Target pathways
Aggregated over 2 target gene(s): HRH1, PTAFR.
Top Reactome pathways
6 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| G alpha (q) signalling events | 2 | HRH1, PTAFR |
| Class A/1 (Rhodopsin-like receptors) | 1 | PTAFR |
| Histamine receptors | 1 | HRH1 |
| Interleukin-10 signaling | 1 | PTAFR |
| Neutrophil degranulation | 1 | PTAFR |
| Interferon gamma signaling | 1 | PTAFR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| inflammatory response | 2 |
| G protein-coupled receptor signaling pathway | 2 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 2 |
| signal transduction | 2 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 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 |
| phospholipase C-activating serotonin receptor signaling pathway | 1 |
| chemotaxis | 1 |
| immune response | 1 |
Indications & clinical
Indications
5 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 |
| urticaria | 3 | MONDO:0005492 | EFO:0005531 |
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| mastocytosis | 2 | MONDO:0007950 | EFO:0009001 |
| cold urticaria | 2 | MONDO:0022799 | EFO:1001881 |
Clinical trials
Total trials: 13.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 4 |
| PHASE4 | 3 |
| PHASE3 | 3 |
| PHASE2 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00162786 | PHASE4 | TERMINATED | Comparative Effects of Rupatadine 10 mg, Hydroxyzine 50 mg and Placebo on Actual Driving Performance |
| NCT00258141 | PHASE4 | UNKNOWN | Study With Rupatadine in Mosquito-Bite Allergic Adult Subjects |
| NCT04601324 | PHASE4 | WITHDRAWN | Allergic Rhinitis Combination Pharmacotherapy Efficacy Study |
| NCT03770923 | PHASE3 | RECRUITING | Effect of Some Drugs on Rheumatoid Arithritis Activity |
| NCT00199251 | PHASE3 | TERMINATED | Efficacy and Safety of Rupatadine 10 and 20 Mg in Chronic Idiopathic Urticaria |
| NCT02358265 | PHASE3 | TERMINATED | Chronic Urticaria - Long Term Assessment of Effects of Rupatadine |
| NCT07064707 | PHASE2 | RECRUITING | Rupatadine in Patients With Ulcerative Colitis |
| NCT00199238 | PHASE2 | TERMINATED | Efficacy of Rupatadine 5, 10 and 20 mg in Chronic Idiopathic Urticaria |
| NCT01605487 | PHASE2 | COMPLETED | Study to Assess Efficacy, Safety and Mechanism of Rupatadine in Cold Urticaria |
| NCT06708520 | PHASE1 | RECRUITING | Pharmacokinetics and Safety of Rupatadine in Participants With Renal Impairment Compared to Control Participants |
| NCT00199225 | PHASE1 | COMPLETED | Evaluation of Possible Effects on the QT/ QTc Interval of Rupatadine in Healthy Volunteers |
| NCT05356143 | PHASE1 | COMPLETED | A Comparative Study of Rupatadine 10 mg Tablets and Clarinex® 5 mg Tablets Under Fasting Conditions |
| NCT06736340 | PHASE1 | COMPLETED | Pharmacokinetics and Safety of Rupatadine in Participants With Hepatic Impairment Compared to Control Participants. |
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.
301 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CHLORPHENIRAMINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, PTAFR |
| LORATADINE | ChEMBL + PubChem | Phase 4 (approved) | HRH1, PTAFR |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | HRH1, PTAFR |
| Belzutifan | PubChem | Approved | HRH1, PTAFR |
| 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 |
| BROTIZOLAM | ChEMBL | Phase 4 (approved) | PTAFR |
| 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 |
| 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 |
| CLOZAPINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLIZINE | ChEMBL | Phase 4 (approved) | HRH1 |
| CYCLOBENZAPRINE | ChEMBL | Phase 4 (approved) | HRH1 |
Related Atlas pages
- Genes: HRH1, PTAFR
- Diseases: allergic disease, urticaria, rheumatoid arthritis
- Drugs: Chlorpheniramine, Loratadine, Clotrimazole, Belzutifan, 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, Brotizolam, Buclizine, Bupropion, Buspirone, Butriptyline, Cabergoline, Candesartan Cilexetil, Captopril, Carbinoxamine, Cariprazine, Cetirizine, Chlordiazepoxide, Chlorphentermine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Citalopram, Clemastine, Clofazimine, Clomipramine, Clozapine, Cyclizine, Cyclobenzaprine