Desloratadine

Summary

Desloratadine (CHEMBL1172) is an approved small-molecule H1-receptor antagonist (ATC R06AX27) targeting HRH1; indicated across 14 conditions including allergic rhinitis and urticaria.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AX27
• Targets: 1 (HRH1)
• Indications: 14 conditions
• Clinical trials: 67
• Chemistry: 310.8 Da · C19H19ClN2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1172
Name	Desloratadine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	124087
ChEBI	CHEBI:291342
ATC	R06AX27
Molecular formula	C19H19ClN2
Molecular weight	310.8
InChIKey	JAUOIFJMECXRGI-UHFFFAOYSA-N

SMILES: C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4

IUPAC name: 13-chloro-2-piperidin-4-ylidene-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene

ChEBI definition: Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.

Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent, cholinergic antagonist.

Other ChEBI roles (chemical / environmental): drug metabolite.

Also known as: Aerius, Allex, Azomyr, Clarinex, Dasselta, Denosin, Descarboethoxyloratadine, Desloratadina, Desloratadine, Desloratadine actavis, Desloratadine component of clarinex-d, Desloratadine ratiopharm

Patent coverage: 5,187 distinct patent families (19,720 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 19,652 (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
HRH1	H1 receptor	Antagonist	9.01	0%	P35367

Broader ChEMBL bioactivity targets: 38 (assay-derived). Sample: Prelamin-A/C, Inositol monophosphatase 1, Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Beta-lactamase, Muscarinic acetylcholine receptor M5.

Bioactivity

ChEMBL activities: 75 potent at pChembl ≥ 5 of 93 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HRH1	9.19	IC50	0.64	nM	CHEMBL_ACT_25873921
HRH1	9.08	IC50	0.83	nM	CHEMBL_ACT_25874074
HRH1	9.01	Ki	0.97	nM	CHEMBL_ACT_1455414
HRH1	8.94	Ki	1.16	nM	CHEMBL_ACT_7700271
HRH1	8.8	Ki	1.58	nM	CHEMBL_ACT_19095447
HRH1	8.73	IC50	1.84	nM	CHEMBL_ACT_19288737
HRH2	8.48	AC50	3.3	nM	CHEMBL_ACT_25114581
HTR2A	8.03	Ki	9.45	nM	CHEMBL_ACT_7702370
HRH1	8	IC50	9.98	nM	CHEMBL_ACT_7700270
HRH1	7.89	AC50	13	nM	CHEMBL_ACT_25213149
HTR2C	7.8	Ki	16	nM	CHEMBL_ACT_7702374
HRH1	7.62	Kd	24	nM	CHEMBL_ACT_20714589
HTR2B	7.55	Ki	28	nM	CHEMBL_ACT_7702372
HTR2C	7.52	IC50	30	nM	CHEMBL_ACT_7702373
HTR2B	7.49	AC50	32.7	nM	CHEMBL_ACT_25164268
HTR2A	7.48	IC50	33	nM	CHEMBL_ACT_7702369
CHRM2	7.43	AC50	37.5	nM	CHEMBL_ACT_25196304
CHRM2	7.42	Ki	38	nM	CHEMBL_ACT_7700301
HTR2A	7.4	AC50	40.2	nM	CHEMBL_ACT_25173822
HTR2B	7.37	IC50	43	nM	CHEMBL_ACT_7702371
CHRM4	7.33	Ki	47	nM	CHEMBL_ACT_7700305
CHRM1	7.19	Ki	64	nM	CHEMBL_ACT_7700299
CHRM2	7.12	AC50	75.3	nM	CHEMBL_ACT_25195409
CHRM3	7.02	Ki	95	nM	CHEMBL_ACT_7700303
CHRM2	6.97	IC50	107	nM	CHEMBL_ACT_7700300
SLC6A4	6.91	Ki	122	nM	CHEMBL_ACT_7702382
HTR2B	6.82	AC50	150	nM	CHEMBL_ACT_25228122
CHRM5	6.68	Ki	210	nM	CHEMBL_ACT_7700307
SLC6A4	6.64	IC50	230	nM	CHEMBL_ACT_7702381
CHRM1	6.62	AC50	239.1	nM	CHEMBL_ACT_25210704

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

14 indications (5 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 rhinitis	4	MONDO:0011786	EFO:0005854
urticaria	4	MONDO:0005492	EFO:0005531
seasonal allergic rhinitis	4	MONDO:0005324	EFO:0003956
perennial allergic rhinitis	4	MONDO:0024332	EFO:1001417
allergic disease	4	MONDO:0005271	MONDO:0005271
atopic conjunctivitis	3	MONDO:0005642	EFO:0007141
common cold	3	MONDO:0005709	EFO:0007214
dermatitis	3	MONDO:0002406	MONDO:0002406
primary progressive multiple sclerosis	3	MONDO:0000451	EFO:0008520
multiple sclerosis	3	MONDO:0005301	MONDO:0005301
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 67.

Phase distribution

Phase	Trials
PHASE3	25
PHASE4	24
PHASE1	6
Not specified	6
PHASE2	5
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00264303	PHASE4	COMPLETED	CUTE (Chronic Urticaria Treatment Evaluation)
NCT00311844	PHASE4	COMPLETED	A Study of the Effects of Desloratadine on Conjunctival Allergen Challenge-induced Ocular Signs and Symptoms (Study P04209)
NCT00359138	PHASE4	COMPLETED	The Duration of the Suppressive Effects of Desloratadine on Allergen Prick Tests After Discontinuation (P04441)
NCT00536380	PHASE4	COMPLETED	Study for the Treatment of Chronic Idiopathic Urticaria With High Doses of AERIUS (Desloratadine) (Study P04849)
NCT00600847	PHASE4	COMPLETED	A Study to Assess and Compare the Effects of 5 mg vs. 20 mg Desloratadine on the Development of Cold Urticaria Lesions
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)
NCT00779116	PHASE4	COMPLETED	Multi-center, Pediatric, Open-label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec 5.0 mg Chewable Tablet Medications (Study P04574)(COMPLETED)
NCT00779636	PHASE4	COMPLETED	Effectiveness and Safety of Desloratadine in Patients With Allergic Airway Disease During the Pollen Season (Study P03284)
NCT00780403	PHASE4	COMPLETED	Multi-Center, Pediatric, Open-Label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec ® 5.0 mg Chewable Tablet Medications (Study P04573) (Completed)
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)
NCT00783354	PHASE4	COMPLETED	A Comparison of Aerius Continuous Treatment Versus Aerius PRN for Chronic Idiopathic Urticaria (Study P03147)
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)
NCT00795522	PHASE4	COMPLETED	An Open-Label Study of the Effects of Desloratadine (Aerius.) Treatment on the Quality of Life of Patients With Chronic Idiopathic Urticaria (Study P02540)
NCT00805584	PHASE4	COMPLETED	Study of Nasal Symptom Relief and Side Effects in Hayfever Patients Treated With Aerius (Desloratadine)(P03442)
NCT00867191	PHASE4	COMPLETED	Comparison of the Effects of Desloratadine and Placebo in the Relief of Nasal Symptom Scores in Subjects With Seasonal Allergic Rhinitis to Cypress Pollen (Study P02836)
NCT01444196	PHASE4	COMPLETED	Desloratadine 5, 10 and 20mg in Patients With Cold Urticaria
NCT01940393	PHASE4	COMPLETED	Evaluation of the Inhibitory Effect of 5 Anti-Histamines in Urticaria
NCT01985789	PHASE4	COMPLETED	Anti-histamines and Methacholine Challenges.
NCT02507635	PHASE4	COMPLETED	Anti-inflammatory H1 Antihistamines Allergic Rhinitis
NCT06217367	PHASE4	UNKNOWN	Over-the-Counter Antihistamines & Heat Stress
NCT06272409	PHASE3	NOT_YET_RECRUITING	Efficacy and Safety of DEP114 in the Treatment of Moderate to Severe Persistent Allergic Rhinitis in Children.
NCT06916884	PHASE3	RECRUITING	Confirmatory Study on the Efficacy and Safety of the Fixed-dose Combination of Desloratadine/Betamethasone Versus Desloratadine
NCT07486583	PHASE3	NOT_YET_RECRUITING	Autologous Whole Blood Therapy in Chronic Idiopathic Urticaria Patients.
NCT00405964	PHASE3	COMPLETED	Study for the Treatment of Persistent Allergic Rhinitis With Desloratadine (Study P04684)
NCT00406783	PHASE3	COMPLETED	Study for the Treatment of Intermittent Allergic Rhinitis With Desloratadine (Study P04683)
NCT00598611	PHASE3	COMPLETED	Effects of 5 mg vs. 20 mg Desloratadine on Skin Lesions in Patients With Chronic Urticaria (CU)
NCT00633919	PHASE2/PHASE3	COMPLETED	Efficacy of SLITone in House Dust Mite Allergic Patients
NCT00757562	PHASE3	COMPLETED	Safety of Desloratadine in Children With Allergy Sensitivity and Chronic Hives, Who Are Poor Metabolizers of Desloratadine (Study P02994)
NCT00789152	PHASE3	COMPLETED	The Effect of Desloratadine and Levocetirizine on Nasal Obstruction (Study P03609)
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)
NCT00795158	PHASE3	COMPLETED	How Desloratadine (Clarinex, Aerius) Affects Quality of Life in Patients With Chronic Idiopathic Urticaria (Have Had Hives for 6 Weeks or Longer)(Study P02988)
NCT00805324	PHASE3	COMPLETED	Study of the Effectiveness and Safety of Desloratadine (Aerius) Syrup in Children With Hayfever With or Without Asthma (P03472)
NCT00817076	PHASE3	COMPLETED	Study of the Effectiveness and Safety of Desloratadine (Aerius) Syrup in Children With Allergic Skin Inflammation (P03475)
NCT01108783	PHASE3	COMPLETED	A Phase III Efficacy Study of the Symptomatic Treatment of Seasonal Allergic Rhinitis With Bilastine
NCT01400828	PHASE3	COMPLETED	Investigate the Safety/Tolerability and Efficacy of Bilastine 20mg in Korean Patients With Seasonal Allergic Rhinitis

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 7 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
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
DEXBROMPHENIRAMINE	ChEMBL	Phase 4 (approved)	HRH1