Last reviewed · How we verify
Levocetirizine (drug)
Levocetirizine is a selective H1-receptor antagonist that blocks histamine binding to H1 receptors on mast cells and basophils, preventing allergic cascade activation.
Levocetirizine is a selective H1-receptor antagonist that blocks histamine signaling to reduce allergic symptoms. Used for Allergic rhinitis (seasonal and perennial), Chronic urticaria.
At a glance
| Generic name | Levocetirizine (drug) |
|---|---|
| Sponsor | UCB Pharma |
| Drug class | H1-receptor antagonist (second-generation antihistamine) |
| Target | H1-receptor |
| Modality | Small molecule |
| Therapeutic area | Allergy/Immunology |
| Phase | FDA-approved |
Mechanism of action
As the active R-enantiomer of cetirizine, levocetirizine competitively inhibits H1 receptors with high selectivity and minimal off-target effects. This blocks histamine-mediated allergic responses including vasodilation, increased vascular permeability, and smooth muscle contraction. The drug is non-sedating due to poor blood-brain barrier penetration.
Approved indications
- Allergic rhinitis (seasonal and perennial)
- Chronic urticaria
- Allergic conjunctivitis
Common side effects
- Somnolence
- Headache
- Fatigue
- Dry mouth
Key clinical trials
- Intravenous Immunoglobulin for the Treatment of Acute Exacerbations of Idiopathic Pulmonary Fibrosis (PHASE3)
- Steroid Use in Treatment of Allergic Reactions to Food (PHASE4)
- Efficacy of Bilastine Up-dosing (40 mg ) Versus Combination of Bilastine (20 mg )With Levocitirizine (5 mg) in the Treatment of Chronic Spontaneous Urticaria (NA)
- Parallel, Double-dummy, Superiority Study Levocetirizine/Pseudoephedrine x Zina for Allergic Rhinitis in Brazil (PHASE3)
- COrticosteroids in acUte uRticAria in emerGency dEpartment (PHASE3)
- A Histamine Pharmacodynamic Biomarker to Guide Treatment in Pediatric Asthma (HAS3) (PHASE3)
- A Trial of Camrelizumab Plus Nab-paclitaxel and Levocetirizine in Metastatic or Recurrent TNBC (PHASE2)
- Treatment Options for Chronic Urticaria (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Levocetirizine (drug) CI brief — competitive landscape report
- Levocetirizine (drug) updates RSS · CI watch RSS
- UCB Pharma portfolio CI