Allergic rhinitis

Disease ID:1190
Name:Allergic rhinitis
Associated with:0 target
13 immuno-relevant ligands
Synonyms
atopic rhinitis | hay fever | Non-seasonal allergic rhinitis | Perenial allergic rhinitis | pollenosis | seasonal allergic rhinitis
Description
A rhinitis that is an allergic inflammation and irritation of the nasal airways involving sneezing, runny nose, nasal congestion, itching and tearing of the eyes caused by exposure to an allergen such as pollen, dust, mold, animal dander and droppings of cockroaches or house dust mites.(DOID)
Database Links
Disease Ontology: DOID:4481

Targets

No target related data available for Allergic rhinitis

Ligands

Key to terms and symbols Click ligand name to view ligand summary Click column headers to sort
Ligand References Clinical comments
GSK2245035 3
Immuno Disease Comments: Phase 2 clinical candidate for allergic rhinitis- administered intranasally.
Clinical Use: GSK2245035 has completed Phase 2 clinical trials in patients with asthma and allergic rhinitis. Results from early clinical evaluation in trials for allergic rhinitis, NCT01480271 (Phase 1) and NCT01607372 (Phase 2), are reported in [6], and results from NCT02446613 reported in [3]. | View clinical data
Bioactivity Comments: In vivo findings disclosed in WO2010018133 report that GSK2245035 (Example 22) induces IFNα production, with mean serum levels reaching 21029 pg/ml (none detected in control mice) [2]. Early clinical trial results show clear target engagement at a dose of 20ng (as detected by local and peripheral increase of IFN-gamma-inducible protein-10) and an accceptable safety profile doses acheiving a local TLR7-mediated immune response [6]. Doses above 100ng were associated with undesireable cytokine release syndrome-related symptoms.

Direct binding assays have not been performed for this compound, rather its engagement with TLR7 has been assessed in functional assays measuring ligand-induced increases in downstream cytokine production/release [1]. An EC50 of ~4.5nM for IFNα production in PBMCs is reported [1]. | View biological activity
fexofenadine
Immuno Disease Comments: Antihistamine approved for the treatment of the symptoms of seasonal allergies.
Clinical Use: Fexofenadine is used to treat the symptoms of seasonal allergies and other histamine-dependent conditions. | View clinical data
clemastine
Immuno Disease Comments: A sedating antihistamine used to treat the symptoms of allergic rhinitis.
Clinical Use: Used to treat hay fever, rhinitis, allergic skin conditions, and pruritus | View clinical data
fluticasone propionate
Immuno Disease Comments: A glucocorticoid (corticosteroid) drug that can be used to manage the symptoms of allergic rhinitis.
Clinical Use: Fluticasone propionate is used for long-term prevention of bronchospasm in asthmatic patients and also is also contained in creams and nasal sprays to control allergy symptoms. In the US, fluticasone propionate is available over-the-counter, as Flonase Allergy Relief®. | View clinical data
azatadine
Immuno Disease Comments: Approved drug for allergic rhinitis.
Clinical Use: Used to reduce symptoms of allergies (such as sneezing, itching, runny nose and watery eyes, rashes). | View clinical data
Bioactivity Comments: We have been unable to find publicly available affinity data for this drug at its proposed molecular target to substantiate its MMOA, and have therefore not tagged a primary drug target. | View biological activity
desloratadine
Immuno Disease Comments: Antihistamine approved for many allergic conditions.
Clinical Use: Desloratadine is used to treat the symptoms (eg rhinitis and urticaria) of many allergic conditions. In some countries this drug is available without prescription. | View clinical data
diphenylpyraline
Immuno Disease Comments: Approved antihistamine for allergic rhinitis, hay fever, and allergic skin disorders.
Clinical Use: Diphenylpyraline is an antihistamine used to treat allergic rhinitis, hay fever, and allergic skin disorders. There is no information regarding approval for clinical use of this drug on the US FDA website. Other national approval agencies may have granted marketing authorisation. | View clinical data
Bioactivity Comments: We have been unable to find publicly available affinity data for this drug at its proposed molecular target to substantiate its MMOA, and have therefore not tagged a primary drug target. | View biological activity
loratadine
Immuno Disease Comments: Antihistamine approved for allergic rhinitis.
Clinical Use: Loratidine is used to relieve the symptoms of allergic rhinitis and chronic idiopathic urticaria. | View clinical data
tripelennamine
Immuno Disease Comments: Antihistamine approved for allergic rhinitis.
Clinical Use: Used as an antipruritic and antihistamine in the treatment of asthma, hay fever, rhinitus and urticaria. All formulations of this drug appear to have been discontinued by the US FDA, although other national approval agencies may continue to grant marketing authorisation. | View clinical data
dectrekumab
Immuno Disease Comments: Phase 2 trial NCT00584584 in allergic rhinitis has been completed.
Clinical Use: Dectrekumab (QBX258) reached Phase II clinical trial as a potential biologic therapy for several immune conditions, including idiopathic pulmonary fibrosis (IPF), asthma, eosinophilic esophagitis [5] (proof of principle study NCT01022970), Crohn's disease, keloids and allergic rhinitis. As of May 2017, there are no active dectrekumab studies. | View clinical data
QAV680
Immuno Disease Comments: Completed Phase 2 trial in allergic rhinitis (see NCT01103050).
Clinical Use: QAV680 reached Phase II clinical trial in asthma and allergic rhinitis. As of May 2017, there are no active clinical trials evaluating this compound. | View clinical data
mometasone
Immuno Disease Comments: A corticosteroid drug used in the management of allergic rhinitis and nasal polyposis.
Clinical Use: Mometasone is used intranasally in the management of asthma, allergic rhinitis and nasal polyposis, and topically for allergic skin disorders. Prescribed formulations contain mometasone furoate (PubChem CID 441336). | View clinical data
timapiprant
Immuno Disease Comments: Phase 2 clinical candidate for allergic rhinitis.
Clinical Use: OC000459 is being evaluated in several Phase 2 clinical trials in various inflammatory and allergic conditions including asthma, allergic rhinitis and atopic dermatitis. Click here to link to a list of Phase 2 OC000459 trials registered with ClinicalTrials.gov. | View clinical data
Bioactivity Comments: OC000459 inhibits mast cell-dependent activation of human Th2 lymphocytes and eosinophils [4]. It does not antagonise ligand binding at any of the other prostanoid receptors [4]. | View biological activity

References

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1. Biggadike K, Ahmed M, Ball DI, Coe DM, Dalmas Wilk DA, Edwards CD, Gibbon BH, Hardy CJ, Hermitage SA, Hessey JO et al.. (2016) Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma. J. Med. Chem., 59 (5): 1711-26. [PMID:26861551]

2. Biggadike K, Coe DM, Lewell XQ, Mitchell CJ, Smith SA, Trivedi N. (2010) Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases. Patent number: WO2010018133. Assignee: Smithkline Beecham Corporation. Priority date: 11/08/2008. Publication date: 18/02/2010.

3. Ellis AK, Tsitoura DC, Quint D, Powley W, Lee LA. (2017) Safety and pharmacodynamics of intranasal GSK2245035, a TLR7 agonist for allergic rhinitis: A randomized trial. Clin. Exp. Allergy, 47 (9): 1193-1203. [PMID:28681506]

4. Pettipher R, Vinall SL, Xue L, Speight G, Townsend ER, Gazi L, Whelan CJ, Armer RE, Payton MA, Hunter MG. (2012) Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J. Pharmacol. Exp. Ther., 340 (2): 473-82. [PMID:22106101]

5. Rothenberg ME, Wen T, Greenberg A, Alpan O, Enav B, Hirano I, Nadeau K, Kaiser S, Peters T, Perez A et al.. (2015) Intravenous anti-IL-13 mAb QAX576 for the treatment of eosinophilic esophagitis. J. Allergy Clin. Immunol., 135 (2): 500-7. [PMID:25226850]

6. Tsitoura D, Ambery C, Price M, Powley W, Garthside S, Biggadike K, Quint D. (2015) Early clinical evaluation of the intranasal TLR7 agonist GSK2245035: Use of translational biomarkers to guide dosing and confirm target engagement. Clin. Pharmacol. Ther., 98 (4): 369-80. [PMID:26044169]