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Cetirizine (Zyrtec)
Cetirizine is a selective H1-receptor antagonist that blocks histamine binding to H1 receptors on cells, preventing allergic symptoms.
Cetirizine is a selective H1-receptor antagonist that blocks histamine binding to H1 receptors on cells, preventing allergic symptoms. Used for Allergic rhinitis (seasonal and perennial), Chronic urticaria, Allergic conjunctivitis.
At a glance
| Generic name | Cetirizine (Zyrtec) |
|---|---|
| Also known as | Zyrtec®, Zyrtec |
| Sponsor | Organon and Co |
| Drug class | H1-receptor antagonist (second-generation antihistamine) |
| Target | H1 receptor |
| Modality | Small molecule |
| Therapeutic area | Immunology / Allergy |
| Phase | FDA-approved |
Mechanism of action
Cetirizine competitively inhibits histamine at H1 receptors, which are responsible for allergic responses including itching, sneezing, and urticaria. As a second-generation antihistamine, it is highly selective for H1 receptors and has minimal central nervous system penetration due to its hydrophilic nature and poor blood-brain barrier crossing, resulting in reduced sedation compared to first-generation antihistamines.
Approved indications
- Allergic rhinitis (seasonal and perennial)
- Chronic urticaria
- Allergic conjunctivitis
- Allergic dermatitis
Common side effects
- Headache
- Somnolence
- Fatigue
- Dry mouth
- Pharyngitis
Key clinical trials
- IMPOWER-QoL: IMPact Of Discontinuing Premedication for WEekly Paclitaxel on bReast Cancer Patient's Quality Of Life (NA)
- Alternate Pre-med in Anti-Cluster of Differentiation 20 (CD20) Pilot Project (PHASE3)
- An Open-Label, Single-Arm, Dose-Escalation Phase I Study Evaluating the Safety, Tolerability, and Preliminary Efficacy of EDB-102 in Patients With EGFR L858R-Mutant, Third-Generation TKI-Resistant Advanced Non-Small Cell Lung Cancer With Liver Metastases (PHASE1)
- Rash & Diarrhea Prophylaxis With Capivasertib (PHASE2)
- Alpelisib/iNOS Inhibitor/Nab-paclitaxel in Patients With HER2 Negative Metaplastic Breast Cancer (MpBC) (PHASE2)
- A Multi-dose Study of ARC-520 in Patients With Hepatitis B 'e' Antigen (HBeAg) Negative, Chronic Hepatitis B Virus (HBV) Infection (PHASE2)
- Extension Study of the Safety and Efficacy of Multi-dose Intravenous ARC-520 in Patients With Chronic Hepatitis B (HBV) Infection (PHASE2)
- Study of ARC-520 With or Without Other Drugs Used in the Treatment of Chronic Chronic Hepatitis B Virus (HBV) (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:
- Cetirizine (Zyrtec) CI brief — competitive landscape report
- Cetirizine (Zyrtec) updates RSS · CI watch RSS
- Organon and Co portfolio CI