Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H19ClN2 |
| Molecular Weight | 310.821 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C2C(CCC3=C(N=CC=C3)C2=C4CCNCC4)=C1
InChI
InChIKey=JAUOIFJMECXRGI-UHFFFAOYSA-N
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11243504Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021165s017,021300s014,021312s015,021563s003lbl.pdf
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11243504
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021165s017,021300s014,021312s015,021563s003lbl.pdf
Desloratadine is an active, descarboethoxy metabolite of loratadine. It acts by selective inhibition of H1 histamine receptor and thus provides relief to patients with allergic rhinitis and chronic idiopathic urticaria. Desloratadine was approved by FDA and it is currently marketed under the name Clarinex (among the others).
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
0.87 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
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| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
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| Palliative | CLARINEX Approved UseDesloratadine Tablets are indicated for: Seasonal Allergic Rhinitis, Perennial Allergic Rhinitis, Chronic Idiopathic Urticaria. Launch Date2001 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4 ng/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
56.9 ng × h/mL |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27 h |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
84.5% |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DESLORATADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
Disc. AE: Somnolence, Abdominal pain... AEs leading to discontinuation/dose reduction: Somnolence (1 patient) Sources: Abdominal pain (1 patient) |
45 mg 1 times / day multiple, oral Highest studied dose Dose: 45 mg, 1 times / day Route: oral Route: multiple Dose: 45 mg, 1 times / day Sources: |
healthy, adult Health Status: healthy Age Group: adult Sex: M+F Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abdominal pain | 1 patient Disc. AE |
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
| Somnolence | 1 patient Disc. AE |
1.25 mg 1 times / day steady, oral Dose: 1.25 mg, 1 times / day Route: oral Route: steady Dose: 1.25 mg, 1 times / day Sources: |
unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sex: M+F Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| likely | ||||
| likely | ||||
| likely | ||||
| likely | no (pharmacogenomic study) Comment: pharmacogenotype 2C19 does not correlate with systemic exposure Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-165_Clarinex_biopharmr_P1.pdf#page=19 Page: 19.0 |
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| likely | no (pharmacogenomic study) Comment: lack of correlation in between 2D6 genotype and 3-OH DCL formation Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-165_Clarinex_biopharmr_P1.pdf#page=10 Page: 10.0 |
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| likely | weak (co-administration study) Comment: Coadministration of ketonconazole, mean drug Cmax and AUC0-24 values at steady state were increased by 29-45% and 21-39%, respectively; Coadministration with erythromycin, mean drug Cmax and AUC 0-24 at steady state were increased by 24% and 14%, respectively. Page: 10.0 |
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Sources: https://dmd.aspetjournals.org/content/43/9/1294 Page: 1.0 |
yes | |||
| yes | weak (co-administration study) Comment: Coadministration of ketonconazole, mean drug Cmax and AUC0-24 values at steady state were increased by 29-45% and 21-39%, respectively; Coadministration with erythromycin, mean drug Cmax and AUC 0-24 at steady state were increased by 24% and 14%, respectively. |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Mediator antagonists in the treatment of allergic disease. | 2001 Sep-Oct |
|
| Second-generation antihistamines in asthma therapy: is there a protective effect? | 2002 |
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| Poor sleep and daytime somnolence in allergic rhinitis: significance of nasal congestion. | 2002 |
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| Investigation of an enhanced resolution triple quadrupole mass spectrometer for high-throughput liquid chromatography/tandem mass spectrometry assays. | 2002 |
|
| Lack of clinically relevant interaction between desloratadine and erythromycin. | 2002 |
|
| A pharmacokinetic profile of desloratadine in healthy adults, including elderly. | 2002 |
|
| Desloratadine demonstrates dose proportionality in healthy adults after single doses. | 2002 |
|
| 24-hour efficacy of once-daily desloratadine therapy in patients with seasonal allergic rhinitis [ISRCTN32042139]. | 2002 Aug 5 |
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| The new antihistamines--desloratadine and levocetirizine: a review. | 2002 Dec |
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| Comparative pharmacology of H1 antihistamines: clinical relevance. | 2002 Dec 16 |
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| Treatment of allergic rhinitis. | 2002 Dec 16 |
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| [The result of neglected or erroneous treatment. Mentally handicapped by hay fever]. | 2002 Jul 11 |
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| Effect of desloratadine versus placebo on nasal airflow and subjective measures of nasal obstruction in subjects with grass pollen-induced allergic rhinitis in an allergen-exposure unit. | 2002 Jun |
|
| Safety and efficacy of desloratadine 5 mg in asthma patients with seasonal allergic rhinitis and nasal congestion. | 2002 Nov |
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| Clinical pharmacology of H1-antihistamines in the skin. | 2002 Nov |
|
| Desloratadine reduces allergen challenge-induced mucinous secretion and plasma exudation in allergic rhinitis. | 2002 Oct |
|
| Effects of fexofenadine and desloratadine on subjective and objective measures of nasal congestion in seasonal allergic rhinitis. | 2002 Oct |
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| Severe hepatotoxicity after application of desloratadine and fluconazole. | 2003 |
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| Desloratadine: an update of its efficacy in the management of allergic disorders. | 2003 |
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| Efficacy and safety of desloratadine 5 mg once daily in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled trial. | 2003 Apr |
|
| Pharmacokinetic properties of single-dose loratadine and ambroxol alone and combined in tablet formulations in healthy men. | 2003 Aug |
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| Efficacy of azelastine nasal spray in patients with an unsatisfactory response to loratadine. | 2003 Aug |
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| Studies on performance and sleepiness with the H1-antihistamine, desloratadine. | 2003 Aug |
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| Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine. | 2003 Aug 13 |
|
| Gateways to clinical trials. | 2003 Dec |
|
| Interactions of olopatadine and selected antihistamines with model and natural membranes. | 2003 Dec |
|
| The effect of ketotifen on inflammatory markers in allergic conjunctivitis: an open, uncontrolled study. | 2003 Jan 6 |
|
| Comparison of ketotifen fumarate ophthalmic solution alone, desloratadine alone, and their combination for inhibition of the signs and symptoms of seasonal allergic rhinoconjunctivitis in the conjunctival allergen challenge model: a double-masked, placebo- and active-controlled trial. | 2003 Jul |
|
| Desloratadine inhibits allergen-induced airway inflammation and bronchial hyperresponsiveness and alters T-cell responses in murine models of asthma. | 2003 Jul |
|
| [Safety of new antihistamines]. | 2003 Jun |
|
| [Clinical aspects of anti-inflammatory action of antihistamines]. | 2003 Jun |
|
| The effects of histamine and leukotriene receptor antagonism on nasal mannitol challenge in allergic rhinitis. | 2003 Jun |
|
| Effects of mediator antagonism on mannitol and adenosine monophosphate challenges. | 2003 Jun |
|
| Comparison of the effects of desloratadine 5-mg daily and placebo on nasal airflow and seasonal allergic rhinitis symptoms induced by grass pollen exposure. | 2003 Jun |
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| Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. | 2003 Mar |
|
| P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. | 2003 Mar |
|
| [Multicenter study of the effectiveness and tolerability of desloratadine in seasonal allergic rhinitis]. | 2003 May 25 |
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| Desloratadine for allergic rhinitis. | 2003 Nov 15 |
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| Loratadine, desloratadine and pregnancy: don't use, risk of hypospadias. | 2003 Oct |
|
| A comparison of the effect of diphenhydramine and desloratadine on vigilance and cognitive function during treatment of ragweed-induced allergic rhinitis. | 2003 Oct |
|
| Efficacy and safety profile of fexofenadine HCl: a unique therapeutic option in H1-receptor antagonist treatment. | 2003 Oct |
|
| Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skin. | 2003 Oct |
|
| Twenty-four-hour activity and consistency of activity of levocetirizine and desloratadine in the skin. | 2003 Oct |
|
| Reliable and specific high-performance liquid chromatographic method for simultaneous determination of loratadine and its metabolite in human plasma. | 2003 Oct 25 |
|
| [Modern antihistaminics against allergic rhinitis. Better breathing without side effects]. | 2003 Oct 30 |
|
| Improvements in simulated real-world relevant performance for patients with seasonal allergic rhinitis: impact of desloratadine. | 2004 Apr |
|
| Inhibition of cold urticaria by desloratadine. | 2004 Jan |
|
| Anti-inflammatory activity of H1-receptor antagonists: review of recent experimental research. | 2004 Jan |
|
| Gateways to clinical trials. | 2004 Jan-Feb |
|
| High-performance liquid chromatographic method for the bioequivalence evaluation of desloratadine fumarate tablets in dogs. | 2004 Mar 10 |
Patents
Sample Use Guides
Adults and Adolescents 12 Years of Age and Over:
take 5 mg tablet once daily. Children 6 to Years of Age: take 2.5 mg tablet once daily. Children 12 Months to 5 Years of Age: take 1.25 mg tablet once daily. Children 6 to 11 Months of Age: 1 mg tablet once daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7677235
Nasal epithelial cells (activated by 1 uM of histamine) were treated with 10 uM of desloratadine and the inhibitory activity of the drug on expression of ICAM-1 and HLA-DR was studied.
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
EMA ASSESSMENT REPORTS |
DESLORATADINE TEVA (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
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LIVERTOX |
NBK548831
Created by
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WHO-VATC |
QR06AX27
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EMA ASSESSMENT REPORTS |
OPULIS (WITHDRAWN: RHINITIS, URTICARIA)
Created by
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NCI_THESAURUS |
C29578
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NDF-RT |
N0000175587
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EMA ASSESSMENT REPORTS |
ALLEX(WITHDRAWN: RHINITIS, ALLERGIC, SEASONAL)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
DASSELTA (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
DESLORATADINE RATIOPHARM (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
DESLORATADINE ACTAVIS (AUTHORIZED: RHINITIS, URTICARIA)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
AZOMYR (AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
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WHO-ATC |
R06AX27
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EMA ASSESSMENT REPORTS |
AERINAZE (AUTHORIZED: RHINITIS)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
AERIUS(AUTHORIZED: RHINITIS, ALLERGIC, SEASONAL)
Created by
admin on Wed Apr 02 06:53:05 GMT 2025 , Edited by admin on Wed Apr 02 06:53:05 GMT 2025
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EMA ASSESSMENT REPORTS |
NEOCLARITYN (AUTHORIZED: RHINITIS, URTICARIA)
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NDF-RT |
N0000000190
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Desloratadine
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Desloratadine
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ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
PARENT (METABOLITE ACTIVE)
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)