Mechanism of Action: Neurokinin 1 Antagonists

Drugs with Mechanism of Action: Neurokinin 1 Antagonists

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	8,623,826
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	10,676,440		Y	Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	9,271,975
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	10,961,195		Y	Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	9,186,357
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	10,233,154			Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	10,828,297

Neurokinin 1 Antagonists Market Analysis and Financial Projection

The market for Neurokinin-1 (NK1) receptor antagonists has evolved significantly since the approval of aprepitant in 2003, driven by their role in managing chemotherapy-induced nausea/vomiting (CINV) and emerging applications in oncology and beyond. Below is a detailed analysis of the market dynamics and patent landscape:

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Market Dynamics

Global Valuation & Growth:

• The NK1 antagonists market reached $XX million in 2024, with a projected CAGR of X% through 2031[9][15]. Growth is fueled by rising cancer prevalence (demanding CINV treatments) and expanding applications in psychiatric disorders, pain management, and vasomotor symptoms[9][13].
• North America dominates (X% market share) due to advanced oncology care, while Asia-Pacific shows rapid growth (CAGR >X%) from increasing healthcare spending[9][15].

Key Players & Competition:

• Merck & Co. leads with approved drugs (aprepitant, fosaprepitant)[2][17], followed by Helsinn Healthcare and Heron Therapeutics (CINVANTI®)[4][16].
• Generics are gaining traction post-patent expirations[11]. For example, Heron’s injectable aprepitant formulations face competition from stable emulsion patents[4][16].
• Over 98 NK1 drugs are in development globally, with 615 clinical trials underway[2].

Segmentation:

• By Type: NK1 antagonists (75% market share) dominate over NK3-focused drugs[9][15].
• By Application: CINV accounts for 60% of use, with vasomotor symptoms (e.g., menopausal hot flashes) as a growth area[9][13].

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Patent Landscape

Innovation & Key Patents:

• Formulation Patents: Heron’s patents cover stable aprepitant emulsions with specific egg yolk lecithin ratios (e.g., US’794 and ’465 patents)[4].
• Diagnostic Tools: Radiolabeled NK1 antagonists (e.g., F-18 tracers) enable PET imaging to study receptor occupancy and drug efficacy[6].
• Combination Therapies: Patents like US7049320B2 cover NK1 antagonists paired with 5-HT3 inhibitors for enhanced antiemetic effects[8].

Expired Patents & Generics:

• Aprepitant’s patent expiration led to generic entries, reducing prices by ~30% in some markets[11][16].
• Over 84 organizations are active in NK1 R&D, with China accelerating generic manufacturing[2][13].

Litigation:

• Heron’s 2022 lawsuit against Fresenius (for patent infringement on emulsion stability) underscores the high stakes in protecting formulation IP[4].

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Future Trends

1. Drug Repurposing: Aprepitant’s antitumor potential (via SP/NK1R axis inhibition) is under study for overcoming chemotherapy resistance[1][17].
2. Regional Expansion: Emerging markets like India and Brazil are prioritizing cost-effective generics[11][13].
3. Next-Gen Antagonists: Companies are developing:
   • Long-acting formulations (e.g., rolapitant)[5][16].
   • Dual NK1/NK3 inhibitors for broader indications[9][15].
4. Personalized Medicine: Biomarker-driven dosing using PET tracers could optimize therapy[6][17].

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Challenges

• Safety Concerns: Aprepitant-linked cardiac issues (e.g., tachycardia) and injection-site reactions require ongoing monitoring[12].
• Regulatory Hurdles: Regional discrepancies in pricing policies (e.g., EU vs. U.S. HTAs) complicate market strategies[11][16].

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Key Takeaways

• NK1 antagonists remain critical in oncology supportive care, with a $XX billion market potential by 2031.
• Patent wars and generics are reshaping competition, while R&D focuses on novel formulations and expanded indications.
• Asia-Pacific’s growth and diagnostic advancements (e.g., PET imaging) will define the next decade of NK1 therapeutics.

> "The SP/NK1R axis is a promising target not just for CINV but also for overcoming tumor resistance pathways." – PMC Study[1]

References

1. https://pmc.ncbi.nlm.nih.gov/articles/PMC9102068/
2. https://synapse.patsnap.com/blog/analysis-on-the-research-progress-of-neurokinin-1-receptor-antagonist
3. https://synapse.patsnap.com/blog/understanding-nk1-antagonists-and-methods-to-keep-abreast-of-their-recent-developments
4. https://www.ded.uscourts.gov/sites/ded/files/opinions/22-985.pdf
5. https://biotarget.amegroups.org/article/view/3703/html
6. https://patents.google.com/patent/US6241964
7. https://touchoncology.com/supportive-cancer-care/journal-articles/current-trends-and-future-directions-in-the-management-of-delayed-nausea-and-vomiting/
8. https://patents.google.com/patent/US7049320B2/en
9. https://www.qyresearch.com/reports/4666860/neurokinin-receptor-antagonists
10. https://citeseerx.ist.psu.edu/document?repid=rep1&type=pdf&doi=480c1c891f59a33315a0af72ec066e36155ea0f7
11. https://www.cofece.mx/cofece/ingles/attachments/article/38/Studies-drug%20markets_vF-Baja.pdf
12. https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2024.1413709/full
13. https://www.qyresearch.com/reports/4666851/neurokinin-receptor-antagonists-api
14. https://patents.google.com/patent/US20110098468A1/en
15. https://www.qyresearch.com/reports/4661358/neurokinin-receptor-antagonists
16. https://pmarketresearch.com/hc/aprepitant-capsules-market/
17. https://pubmed.ncbi.nlm.nih.gov/20533894/