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Comparator: cetirizine
Cetirizine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without significant central nervous system penetration.
Cetirizine is a selective H1-receptor antagonist that blocks histamine-mediated allergic responses without significant central nervous system penetration. Used for Allergic rhinitis (seasonal and perennial), Chronic urticaria, Allergic conjunctivitis.
At a glance
| Generic name | Comparator: cetirizine |
|---|---|
| Sponsor | Organon and Co |
| Drug class | Selective H1-receptor antagonist (second-generation antihistamine) |
| Target | H1 histamine receptor |
| Modality | Small molecule |
| Therapeutic area | Immunology / Allergy |
| Phase | Phase 3 |
Mechanism of action
Cetirizine competitively binds to peripheral H1 histamine receptors on mast cells, basophils, and other immune cells, preventing histamine from triggering allergic cascade reactions. Due to its hydrophilic nature and low lipophilicity, it has minimal blood-brain barrier penetration, resulting in reduced sedation compared to first-generation antihistamines. This mechanism provides symptomatic relief of allergic rhinitis, urticaria, and other histamine-mediated allergic conditions.
Approved indications
- Allergic rhinitis (seasonal and perennial)
- Chronic urticaria
- Allergic conjunctivitis
Common side effects
- Headache
- Somnolence
- Fatigue
- Dry mouth
- Pharyngitis
Key clinical trials
- A Multi-dose Study of ARC-520 in Patients With Hepatitis B 'e' Antigen (HBeAg) Positive, Chronic Hepatitis B Virus Infection (PHASE2)
- Comparing Risk and Severity of IRRs in Patients Premedicated With Cetirizine vs. Diphenhydramine Prior to Ocrelizumab (PHASE3)
- Montelukast in Perennial Allergic Rhinitis - 2001-2002 Study (0476-246) (PHASE3)
- Ofatumumab in Children With Drug Resistant Idiopathic Nephrotic Syndrome (PHASE2)
- A Comparator Study of Fluticasone Propionate Nasal Spray Verses (vs) Cetirizine in the Treatment of Seasonal Allergic Rhinitis (PHASE4)
- Combination Study Of S-555739/Cetirizine HCl In Adult Patients With Seasonal Allergic Rhinitis (PHASE2)
- 723/726 Proof of Concept Study in Allergen Challenge Chamber in Hannover (PHASE2)
- Allergen Challenge Chamber Study With Single Dose Oral GSK835726 Compared With Placebo (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |