Mechanism of Action: Sigma-1 Receptor Agonists

Drugs with Mechanism of Action: Sigma-1 Receptor Agonists

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
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes
Axsome	AUVELITY	bupropion hydrochloride; dextromethorphan hydrobromide	TABLET, EXTENDED RELEASE;ORAL	215430-001	Aug 18, 2022		RX	Yes	Yes

Sigma-1 Receptor Agonists Market Analysis and Financial Projection

The market dynamics and patent landscape for Sigma-1 receptor agonists reveal a rapidly evolving therapeutic sector with significant growth potential, driven by expanding clinical applications and strategic intellectual property (IP) developments.

Market Dynamics

• Growth Projections: The global blarcamesine (a Sigma-1 agonist) market is projected to grow from $822.9 million in 2025 to $1.08 billion by 2032, reflecting a 4.0% CAGR[9]. This growth is fueled by Sigma-1 agonists’ neuroprotective properties, particularly in treating Parkinson’s disease and Rett syndrome.

• Key Drivers:

  • Neurodegenerative and Psychiatric Disorders: Sigma-1 agonists like blarcamesine (ANAVEX2-73) show promise in preclinical models for rescuing neuronal damage in Parkinson’s and improving cognitive function in Alzheimer’s and Rett syndrome [9][16].
  • Pain Management: Drugs such as E-52862 (Esteve) have demonstrated efficacy in Phase II clinical trials for neuropathic pain (NP) [7].
  • Depression: Sigma-1 receptors modulate neurotransmitter systems linked to depression, with antagonists like sertraline repurposed for their rapid antidepressant effects [8].

• Regional Insights:

  • North America dominates due to advanced healthcare infrastructure and prevalence of neurological disorders[9].
  • Asia-Pacific is the fastest-growing region, driven by unmet clinical needs and expanding healthcare access[1][9].

Patent Landscape

• Therapeutic Applications:

  • Neurodegeneration: Patents cover blarcamesine for Rett syndrome (valid until 2037)[16] and pridopidine (Prilenia Therapeutics) for Huntington’s disease[12].
  • Cancer: US8349898B2 describes Sigma-1 ligands for inhibiting tumor growth, particularly in prostate, breast, and CNS cancers[14].
  • Fibrosis: WO2015118365A1 details Sigma-1 agonists for treating organ fibrosis[6].

• Strategic IP Activity:

  • Pipeline Dominance: Over 50 Sigma-1 receptor agonists are in clinical development, with companies like Anavex Life Sciences and Esteve Pharmaceuticals leading in neurodegenerative and pain indications[12][13].
  • Combination Therapies: Patents highlight synergies with opioids (e.g., S1RA enhances loperamide’s antinociceptive effects)[7] and chemotherapy agents for cancer[14].
  • White Space Opportunities: Emerging areas include retinal degeneration and COVID-19-related mental health disorders[7][13].

Competitive Landscape

• Key Players:	Company	Drug/Candidate	Indication	Development Stage
  Anavex Life Sciences	Blarcamesine	Rett syndrome, Parkinson’s	Phase III
  Esteve Pharmaceuticals	E-52862 (S1RA)	Neuropathic pain	Phase II
  Prilenia Therapeutics	Pridopidine	Huntington’s disease	Phase III

• Challenges:

  • Manufacturing bottlenecks and supply chain limitations (e.g., GLP-1 agonist shortages highlight scalability risks)[5].
  • Generic competition in related markets (e.g., Parkinson’s drugs) pressures pricing[10].

Future Outlook

• Market Expansion: Sigma-1 agonists could address $125 billion+ metabolic and neurological markets by 2033, mirroring GLP-1 agonist growth trajectories[5][9].
• Innovation Trends:
  • Dual-targeting drugs: Viking Therapeutics’ VK-2735 (GLP-1/GIP agonist) and Amgen’s MariTide signal interest in multi-receptor approaches[5].
  • AI-driven IP strategies: Patent landscape analysis tools are critical for navigating crowded fields (e.g., AI patents grew 1,800% in a decade)[15].

"The hope that modulation of Sigma-1 receptors could be a therapeutic strategy drives the research community."
— Frontiers in Pharmacology (2020)[13]

In summary, Sigma-1 receptor agonists are poised for transformative growth across neurology, oncology, and psychiatry, supported by robust patent portfolios and a deepening understanding of receptor biology. Strategic collaborations and IP management will be pivotal in capturing market share amid rising competition.

References

1. https://www.grandviewresearch.com/press-release/global-glp-1-receptor-agonist-market
2. https://colab.ws/articles/10.4155%2Fppa-2020-0007
3. https://legacy.www.sbir.gov/node/1196907
4. https://pmc.ncbi.nlm.nih.gov/articles/PMC2785038/
5. https://www.biospace.com/glp-1-receptor-agonist-market-to-reach-125b-by-2033-globaldata
6. https://patents.google.com/patent/WO2015118365A1/en
7. https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2020.590519/full
8. https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2022.925879/full
9. https://www.coherentmarketinsights.com/industry-reports/global-blarcamesine-market
10. https://www.oncotarget.com/article/8104/text/
11. https://www.epo.org/en/boards-of-appeal/decisions/t061642eu1
12. https://www.researchandmarkets.com/reports/5504276/sigma-1-receptor-agonists-pipeline-insight-2024
13. https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2019.00564/full
14. https://patents.google.com/patent/US8349898B2/en
15. https://caldwelllaw.com/news/how-patent-landscape-analysis-drives-business-growth/
16. https://rettsyndromenews.com/news/anavex-2-73-treatment-rett-syndrome-other-neurodevelopmental-disorders-to-receive-new-us-patent/