Mechanism of Action: Adrenergic beta1-Antagonists

Drugs with Mechanism of Action: Adrenergic beta1-Antagonists

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-001	Oct 20, 2006		DISCN	Yes	No					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-002	Oct 20, 2006		DISCN	Yes	No					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-003	Oct 20, 2006		DISCN	Yes	No					Y
Waylis Therap	COREG CR	carvedilol phosphate	CAPSULE, EXTENDED RELEASE;ORAL	022012-004	Oct 20, 2006		DISCN	Yes	No					Y
Waylis Therap	COREG	carvedilol	TABLET;ORAL	020297-004	May 29, 1997	AB	RX	Yes	No

Adrenergic beta1-Antagonists Market Analysis and Financial Projection

The global market for adrenergic β1-antagonists (beta1-blockers) is experiencing steady growth driven by rising cardiovascular disease prevalence and expanding therapeutic applications. Simultaneously, the patent landscape reflects ongoing innovation in drug formulations and combination therapies, alongside strategic legal battles over intellectual property. Here's a detailed analysis of both sectors:

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Market Dynamics

Growth Drivers

• Cardiovascular Disease Burden: Over 1.13 billion people globally suffer from hypertension, a primary indication for beta1-blockers like metoprolol and nebivolol[17].
• Aging Population: Increased incidence of heart failure and arrhythmias in the elderly supports demand, with North America dominating >65% of market share[7][9].
• Therapeutic Expansion: Beta1-blockers are now used for migraines, anxiety, and glaucoma, broadening their clinical utility[18][14].

Market Projections

• The market is projected to grow from $9.58B in 2023 to $15.08B by 2030, with a 5.2% CAGR[2][13].
• Key segments include angina pectoris (fastest-growing) and hypertension (largest application)[7][9].

Competitive Landscape

• Top Players: AstraZeneca, Novartis, Pfizer, and Teva lead R&D efforts, focusing on combination therapies and extended-release formulations[5][9].
• Regional Trends: Asia-Pacific shows the highest growth potential due to aging demographics and improving healthcare access[6][9].

Challenges

• Side Effects: Fatigue, dizziness, and contraindications in asthma patients limit adoption[13][10].
• Generic Competition: Patent expirations (e.g., metoprolol) have intensified price pressures[11][15].

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Patent Landscape

Key Innovations

1. Formulation Advances:

   • Nebivolol hydrochloride patents cover improved salt stability and dissolution properties without wetting agents[12][19].
   • Controlled-release combinations (e.g., tesofensine + metoprolol) target obesity and diabetes[4].

2. Therapeutic Expansion:

   • US Patent 8,338,489B2 protects β-blockers for treating infantile hemangiomas, a novel application[14].

3. Selectivity Enhancements:

   • Research highlights poor β1/β2 selectivity in existing drugs, prompting development of next-gen agents like CGP 20712A (501-fold β1-selective)[10].

Patent Litigation

• Metoprolol Succinate: AstraZeneca’s ‘154 patent was invalidated due to "obviousness-type double patenting" over an earlier composition patent, allowing generic competition[11][15].

Strategic R&D Trends

• Personalized Medicine: Companies like Saniona are exploring tailored delivery systems to minimize side effects[4][13].
• Geographical Filing: Over 70% of β1-blocker patents target high-burden regions, though grant status varies[3][8].

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Strategic Insights

• Opportunities: Developing β1-selective antagonists and combination therapies could capture $13.68B by 2030[2][10].
• Risks: Patent cliffs and litigation (e.g., metoprolol) necessitate robust lifecycle management strategies[15][8].

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"The shift toward personalized medicine and advanced formulations is reshaping the β1-blocker market, offering avenues for differentiation in a crowded field." [13]

This dynamic interplay of market growth and intellectual property innovation underscores the critical role of strategic R&D and legal agility in sustaining competitiveness.

References

1. https://www.newschannelnebraska.com/story/52447250/beta-blocker-market-2025-2032-global-industry-analysis-revenue-growth-business-prospects
2. https://www.databridgemarketresearch.com/reports/global-beta-blockers-market
3. https://unitaid.org/uploads/TMC_207_Patent_Landscape.pdf
4. https://pubchem.ncbi.nlm.nih.gov/patent/US-10828278-B2
5. https://synapse.patsnap.com/blog/an-in-depth-analysis-of-nebivolol-hydrochlorides-randd-progress
6. https://www.cognitivemarketresearch.com/beta-blockers-market-report
7. https://www.techsciresearch.com/report/beta-blockers-market/22234.html
8. https://crsreports.congress.gov/product/pdf/R/R46679
9. https://www.transparencymarketresearch.com/beta-blockers-market.html
10. https://pmc.ncbi.nlm.nih.gov/articles/PMC1576008/
11. https://casetext.com/analysis/in-re-metoprolol-succinate-patent-litigation-astrzeneca-ab-et-al-v-kv-pharmaceutical-company-et-al
12. https://pubchem.ncbi.nlm.nih.gov/patent/EP-1737847-B1
13. https://www.researchandmarkets.com/report/beta-blocker
14. https://patents.google.com/patent/US8338489B2/en
15. https://go.gale.com/ps/i.do?id=GALE%7CA173374848&sid=googleScholar&v=2.1&it=r&linkaccess=abs&issn=17411343&p=AONE&sw=w
16. https://patents.google.com/patent/WO2006103101A2/en
17. https://www.verifiedmarketreports.com/product/beta-blockers-market/
18. https://www.openpr.com/news/3907457/beta-blockers-market-growth-forecast-insights-trends
19. https://patents.google.com/patent/US20100137424A1/en