Substance P/Neurokinin-1 Receptor Antagonist Drug Class List

Drugs in Drug Class: Substance P/Neurokinin-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
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	12,042,494		Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	9,951,016		Y	Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	9,943,515
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes	8,951,969		Y
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

Substance P/Neurokinin-1 Receptor Antagonist Market Analysis and Financial Projection

The Substance P/Neurokinin-1 (NK1) receptor antagonist drug class has emerged as a critical component in managing conditions like chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. Below is an analysis of its market dynamics and patent landscape.

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Market Dynamics

Current Market Size and Growth

• The Aprepitant market, a leading NK1 antagonist, was valued at USD 1.2 billion in 2023, with projections to reach USD 1.9 billion by 2031 at a 5.5% CAGR[3].
• The broader chemotherapy-induced nausea and vomiting drugs market is expected to grow to USD 3.2 billion by 2027, driven by rising cancer therapies and demand for antiemetic drugs[6][8].
• Neurokinin receptor antagonists hold a significant share, with the NK1 segment anticipated to grow at 5.8% CAGR through 2027[6].

Key Drivers

1. Expanding Applications: Approved for CINV and postoperative nausea, NK1 antagonists like aprepitant are now explored for pain, inflammation, and CNS disorders[1][12].
2. Cancer Prevalence: Rising chemotherapy use fuels demand for effective antiemetics, with aprepitant reducing acute and delayed vomiting[1][3].
3. Geographic Expansion: North America leads (USD 1.1 billion in 2023), but Asia-Pacific is the fastest-growing region due to healthcare modernization[9][13].

Competitive Landscape

• Merck & Co. dominates with two approved drugs:
  • Aprepitant (2003, U.S.) and Fosaprepitant dimeglumine (2008)[8].
• Other players include Helsinn Healthcare, Bayer, and Heron Therapeutics, with 21 companies producing generic fosaprepitant[5][9].

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Patent Landscape

Key Patents and Innovations

1. Early Developments:

   • WO1983001252A1 (1981): Early Substance P antagonist modifying amino acids to inhibit inflammation[2].
   • US7902366B2 (NY): Covers NK1 antagonists with small-molecule structures[4].

2. Commercial Breakthroughs:

   • Merck’s Aprepitant: First approved in 2003, protected by patents expiring in 2025–2030[1][5].
   • Fosaprepitant Dimeglumine: Merck’s injectable form faces Paragraph IV challenges from generics but retains patents in the EU and China[5].

3. Global Activity: Over 300 patents filed in 20 years, with China emerging as a key developer of NK1 drugs[1][7][12].

Challenges and Generic Competition

• Patent Litigation: Fosaprepitant has faced 4 Paragraph IV challenges in the U.S., with generics entering post-2025[5].
• Pipeline Diversity: Companies like Novartis and Pfizer explore novel scaffolds (e.g., pyrrolidine derivatives) to improve efficacy[7].

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Future Opportunities

• New Indications: Potential use in neuropathic pain, depression, and cancer progression via NK1 receptor modulation[12].
• Regional Growth: China’s healthcare investment and approvals for drugs like aprepitant signal untapped markets[1][10].
• Technological Advances: Radioligands targeting NK1 receptors for tumor imaging and therapy[12].

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Challenges

• Side Effects: Headaches, constipation, and drug interactions may limit patient compliance[13].
• Generic Erosion: Post-2030, loss of exclusivity may reduce brand revenue by 20–30%[5].

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“The NK1 receptor research has led to the clinical introduction of aprepitant in 2003 and fosaprepitant in 2008, revolutionizing antiemetic therapy.” [8]

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Key Takeaways

• NK1 antagonists are critical in oncology support, with steady market growth driven by innovation and rising cancer rates.
• Patent expiries and generic competition will reshape the landscape post-2030, while new therapeutic applications offer long-term opportunities.
• Asia-Pacific’s expanding healthcare infrastructure positions it as a future growth hub.

References

1. https://synapse.patsnap.com/blog/analysis-on-the-research-progress-of-neurokinin-1-receptor-antagonist
2. https://patents.google.com/patent/WO1983001252A1
3. https://www.marketresearchintellect.com/product/global-aprepitant-market-size-and-forecast/
4. https://patents.google.com/patent/US7902366B2/en
5. https://www.drugpatentwatch.com/p/generic/fosaprepitant+dimeglumine
6. https://citeseerx.ist.psu.edu/document?repid=rep1&type=pdf&doi=480c1c891f59a33315a0af72ec066e36155ea0f7
7. https://www.businesswire.com/news/home/20210517005514/en/Global-Chemotherapy-induced-Nausea-and-Vomiting-Drugs-Market-Report-2021-Serotonin-Receptor-Antagonist-is-Projected-to-Account-for-$1.2-Billion-of-the-Total-$3.2-Billion-Market-by-2027---ResearchAndMarkets.com
8. https://pubmed.ncbi.nlm.nih.gov/20533894/
9. https://www.qyresearch.com/reports/4661358/neurokinin-receptor-antagonists
10. https://synapse.patsnap.com/blog/understanding-nk1-antagonists-and-methods-to-keep-abreast-of-their-recent-developments
11. https://www.qyresearch.com/reports/4666860/neurokinin-receptor-antagonists
12. https://pmc.ncbi.nlm.nih.gov/articles/PMC6781293/
13. https://market.us/report/radiotherapy-induced-nausea-and-vomiting-treatment-market/