Histamine-1 Receptor Antagonist Drug Class List

Drugs in Drug Class: Histamine-1 Receptor Antagonist

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Haleon Us Holdings	ADVIL ALLERGY AND CONGESTION RELIEF	chlorpheniramine maleate; ibuprofen; phenylephrine hydrochloride	TABLET;ORAL	022113-001	Dec 21, 2011		OTC	Yes	Yes
Haleon Us Holdings	ADVIL ALLERGY SINUS	chlorpheniramine maleate; ibuprofen; pseudoephedrine hydrochloride	TABLET;ORAL	021441-001	Dec 19, 2002		OTC	Yes	Yes			Y
Haleon Us Holdings	ADVIL MULTI-SYMPTOM COLD & FLU	chlorpheniramine maleate; ibuprofen; phenylephrine hydrochloride	TABLET;ORAL	022113-002	Apr 28, 2017		OTC	Yes	Yes
Haleon Us Holdings	ADVIL PM	diphenhydramine hydrochloride; ibuprofen	CAPSULE;ORAL	021393-001	Dec 21, 2005		OTC	Yes	Yes

Histamine-1 Receptor Antagonist Market Analysis and Financial Projection

The Histamine-1 (H1) Receptor Antagonist drug class is a cornerstone of allergy treatment, with a dynamic market influenced by evolving therapeutic needs, patent expirations, and innovation in drug development. Below is a detailed analysis of the market dynamics and patent landscape:

---

Market Dynamics

Market Size and Growth

• The global antihistamines market was valued at $282.7 billion in 2023, projected to reach $616 billion by 2033, growing at a CAGR of 8.1% [7].
• H1 blockers dominate the product segment, holding 58.3% market share in 2023, driven by their efficacy in treating allergies, urticaria, and pruritus [7].

Key Drivers

1. Shift to Non-Sedating Antihistamines: Demand for formulations minimizing drowsiness (e.g., cetirizine, fexofenadine) is rising, especially among professionals and drivers requiring alertness [1].
2. OTC Expansion: Retail pharmacies account for 41.7% of distribution, fueled by self-medication trends and accessibility of OTC antihistamines [1][7].
3. Allergy Epidemic: Allergies represent 42.3% of antihistamine use, linked to increasing pollen exposure and urbanization [7].

Regional Insights

• North America leads with 35.82% market share ($105.4B in 2023), driven by high allergy prevalence and healthcare spending [7].
• Asia-Pacific and Africa are emerging markets, with expanding healthcare access and rising disposable incomes [1].

Competitive Landscape

• Top Players: GSK, Sanofi, and Bayer AG lead H1 antagonist R&D, focusing on small-molecule drugs [6].
• Strategic Moves: Companies are diversifying into biologics and combination therapies to offset generic competition [6][9].

---

Patent Landscape

Key Patents and Expirations

1. Wakix (Pitolisant):
   • Protected by 5 U.S. patents, with critical expiries in 2026 and 2030. Estimated generic entry by 2031 [11].
   • Represents a shift toward H3 receptor antagonists for CNS disorders like narcolepsy [8][9].
2. Pollinex Quattro: Allergy Therapeutics’ adjuvant-based allergy vaccine patent (expiring 2038) highlights innovation in immunotherapy [5].
3. Diphenhydramine: A first-generation H1 antagonist with expired patents, now widely genericized [14].

Innovation Trends

• Multi-Target Antagonists: Dual H1/H3 and H1/H4 receptor antagonists are in development for enhanced efficacy in allergies and CNS disorders [2][10].
• Combination Therapies: Patents like US6420560B1 cover H1/H4 antagonist combinations to address inflammation and immune responses [10].

Challenges and Opportunities

• Patent Cliffs: Major drugs like Keytruda (2028) and Eliquis will face biosimilar/generic competition, pressuring revenue but improving affordability [4].
• R&D Focus: Over 270 H1 receptor drugs are in development globally, with China leading in trials (e.g., ebastine for allergic rhinitis) [6][9].

---

Future Outlook

• Emerging Markets: Asia-Pacific’s healthcare expansion and allergy prevalence will drive growth, with oral antihistamines remaining preferred (73.2% market share) [1][7].
• Regulatory and Clinical Shifts: Increased focus on non-sedative formulations and pediatric applications (e.g., Altamira’s intranasal betahistine for dizziness) [12].
• Multi-Indication Expansion: H1 antagonists are being tested for autism, Prader-Willi syndrome, and fatigue, broadening therapeutic scope [9].

---

"The development of multiple-activity H1 antihistamines in allergy has met with limited success due to a competitive commercial environment" [2].

While generics and biosimilars will challenge incumbents, innovation in targeted therapies and geographic expansion will sustain market growth. Companies must balance patent lifecycle management with R&D investments to remain competitive.

References

1. https://sites.google.com/view/insightpulsepro/market-intelligence-insight/h1-receptor-antagonist-market-by-application
2. https://pubmed.ncbi.nlm.nih.gov/20716024/
3. https://www.360iresearch.com/library/intelligence/antihistamine-drugs
4. https://www.pharmanow.live/knowledge-hub/market-trends/pharmaceutical-drugs-losing-patent-exclusivity
5. https://www.biospace.com/allergy-therapeutics-plc-key-technology-patent-for-pollinex-r-quattro-in-japan-granted
6. https://synapse.patsnap.com/blog/exploringebastines-revolutionary-randd-successes
7. https://market.us/report/antihistamines-market/
8. https://pmc.ncbi.nlm.nih.gov/articles/PMC4485016/
9. https://pubmed.ncbi.nlm.nih.gov/39757430/
10. https://patents.google.com/patent/AP2002002401A0/en
11. https://pharsight.greyb.com/drug/wakix-patent-expiration
12. https://ir.altamiratherapeutics.com/news-releases/news-release-details/altamira-therapeutics-announces-european-patent-office-decision
13. https://patents.google.com/patent/US6420560B1/en
14. https://www.drugpatentwatch.com/p/generic-api/diphenhydramine+hydrochloride