Uncompetitive N-methyl-D-aspartate Receptor Antagonist Drug Class List

Drugs in Drug Class: Uncompetitive N-methyl-D-aspartate Receptor Antagonist

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	12,146,889
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	11,357,744
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	9,238,032
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	10,799,497
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	9,198,905
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes	10,894,046

Uncompetitive N-methyl-D-aspartate Receptor Antagonist Market Analysis and Financial Projection

The market for uncompetitive NMDA receptor antagonists is expanding significantly due to their therapeutic potential in neurological and psychiatric disorders, though development challenges persist. Here's an analysis of the market dynamics and patent landscape:

Market Dynamics

• Growth Projections:
  The US NMDA receptor antagonist market was valued at $900 million in 2022, with projections to reach $1.6 billion by 2030 (CAGR: 8%)[4]. Globally, the glutamate antagonist market, driven by NMDA-targeted therapies, is expected to grow at >8% CAGR, with North America leading and Asia-Pacific emerging as a key growth region[12].

• Key Drivers:

  • Rising prevalence of Alzheimer’s disease, depression, and chronic pain[4][12].
  • Demand for neuroprotective agents with reduced side effects compared to older NMDA blockers (e.g., ketamine)[6][11].
  • Investments in subunit-selective modulators (e.g., GluN2B-targeted drugs) to improve safety[6].

• Major Players:
  Leading companies include Relmada Therapeutics (dextromethadone), Adamas Pharmaceuticals (memantine combinations), Astellas Pharma, and UCB[4][13].

• Challenges:

  • Drug-induced hyperglycemia exacerbating stroke outcomes in preclinical models[10].
  • Balancing efficacy with side effects (e.g., hallucinations, agitation)[1][6].

---

Patent Landscape

• Key Patents and Innovations:	Company/Inventor	Patent Focus	Key Claims
  Relmada Therapeutics	d-Methadone (REL-1017)	Broad coverage for depression, anxiety, and mood disorders in the US and China[3][8][14].
  Adamas Pharmaceuticals	Memantine combinations	Methods for administering memantine with donepezil (NAMZARIC®) for Alzheimer’s[13].
  Astellas Pharma	Aminoindan derivatives	Therapies for Parkinson’s, Alzheimer’s, and ischemic apoplexy[2].
  NeurOp Inc. & Others	GluN2B-selective antagonists	Improved bioavailability and reduced side effects (e.g., phenanthroic acid derivatives)[6].

• Emerging Trends:

  • Subunit selectivity: Patents focus on GluN2B or GluN2A/C/D subunits to minimize off-target effects[6].
  • Combination therapies: Memantine paired with acetylcholinesterase inhibitors to enhance Alzheimer’s treatment[13].
  • Novel chemical scaffolds: 1-aminoalkylcyclohexane derivatives with rapid action and moderate affinity[7].

• Clinical Development:

  • Relmada’s Phase 2a trial for dextromethadone in major depressive disorder (2018)[3][14].
  • Astellas’ compounds showing anti-seizure activity (ED₅₀: 4.2 mg/kg in mice)[2].

---

Competitive and Regulatory Factors

• IP Strategies: Companies prioritize territorial expansion (e.g., Relmada’s patents in China)[3] and pediatric exclusivity extensions (e.g., NAMZARIC®)[13].
• Regulatory Hurdles: Conflicting preclinical-clinical results and poorly defined NMDA receptor subtypes complicate approval[6].
• Market Risks: Hyperglycemia-linked failures in stroke trials highlight the need for patient stratification[10].

---

Future Outlook

• Opportunities:
  • Repurposing: NMDA antagonists like ketamine for treatment-resistant depression[2][12].
  • Precision delivery: Nanoparticle systems to enhance brain targeting[12].
• Threats:
  • Generic competition for older drugs (e.g., memantine)[5].
  • High R&D costs for subunit-selective agents[6].

In summary, the uncompetitive NMDA receptor antagonist market is buoyed by innovation in subunit selectivity and combination therapies, though developers must navigate clinical and regulatory challenges to capitalize on growth opportunities.

References

1. https://en.wikipedia.org/wiki/NMDA_receptor
2. https://pmc.ncbi.nlm.nih.gov/articles/PMC4860953/
3. https://www.relmada.com/for-investors/news/detail/186/relmada-therapeutics-allowed-patent-application-in-china
4. https://sites.google.com/view/wavemakersresearch/research/us-nmda-receptor-antagonist-market-by-type
5. https://www.fdli.org/wp-content/uploads/2022/08/7-Darrow-and-Mai.pdf
6. https://pmc.ncbi.nlm.nih.gov/articles/PMC11124131/
7. https://patentimages.storage.googleapis.com/fc/b4/e8/470ec1568985c0/US6034134.pdf
8. https://www.relmada.com/for-investors/news/detail/167/relmada-therapeutics-announces-issuance-of-key-u-s-patent
9. https://www.globenewswire.com/news-release/2025/02/06/3022127/0/en/Opioid-Use-Disorder-Market-Size-Projected-to-Hit-USD-9-02-Billion-by-2032-SNS-Insider.html
10. https://www.eneuro.org/content/8/6/ENEURO.0346-21.2021
11. https://pmc.ncbi.nlm.nih.gov/articles/PMC5002349/
12. https://pmarketresearch.com/product/worldwide-carbon-footprint-audit-market-research-2024-by-type-application-participants-and-countries-forecast-to-2030/worldwide-glutamate-antagonist-market-research-2024-by-type-application-participants-and-countries-forecast-to-2030
13. https://www.drugpatentwatch.com/p/patent/8173708
14. https://www.relmada.com/for-investors/news/detail/183/relmada-therapeutics-acquires-global-rights-to-develop-and