NLS Pharmaceutics Announces Publication of New Patent Application for Next-Gen Dual Non-Sulfonamide Orexin Receptor Agonists (DOXA)

Rhea-AI Summary

NLS Pharmaceutics, a clinical-stage biopharmaceutical company, has announced a new patent application for dual orexin receptor agonists (DOXA), developed with Aexon Labs, targeting narcolepsy and neurodegenerative diseases like Parkinson's. These non-sulfonamide compounds are designed to reduce side effects and improve patient safety. The molecules enhance neurotransmitter release and protect neuronal health by modulating orexin receptors and inhibiting cathepsin H (CTSH), offering potential therapeutic benefits for sleep regulation and neurodegeneration. This patent represents a significant advancement in addressing unmet medical needs in both narcolepsy and neurodegenerative diseases.

Positive

• New patent application for dual orexin receptor agonists (DOXA) targeting narcolepsy and neurodegenerative diseases.
• Non-sulfonamide compounds reduce side effects and improve patient safety.
• Potential therapeutic benefits for sleep regulation and neurodegeneration.
• Enhances neurotransmitter release and protects neuronal health by modulating orexin receptors.
• Inhibits cathepsin H (CTSH) to protect neuronal cells and improve therapeutic outcomes.
• Multitarget molecules show promise in treating conditions like Parkinson's disease.
• Better long-term outcomes suggested by preventing receptor desensitization and high-affinity binding issues.

Negative

• No clinical trial data provided to substantiate in vitro efficacy claims.
• Potential delays or regulatory hurdles in obtaining patent approval and subsequent commercialization.
• Uncertainty around the effectiveness of new compounds in human trials.
• Existing financial and operational risks associated with development-stage biopharmaceutical companies.
• Possible competition from other companies developing similar treatments.

Insights

Medical Research Analyst

The announcement of NLS Pharmaceutics' new patent application for dual orexin receptor agonists represents a significant development in the therapeutic landscape for narcolepsy and neurodegenerative diseases like Parkinson's. This novel approach targets both orexin receptors (OX1R and OX2R), which are important for regulating sleep and wakefulness. The non-sulfonamide nature of these compounds could reduce side effects, making them safer for long-term use. The inclusion of CTSH inhibition adds an extra layer of neuroprotection by tackling inflammation and autoimmune responses, which are pivotal in these conditions.

For investors, the potential of these compounds to address substantial unmet medical needs could translate into a strong market position for NLS. However, clinical trials are necessary to validate in-vitro findings and prove efficacy and safety in humans.

Tech Expert

This patent highlights the technological advancements in the biopharmaceutical sector, leveraging dual-targeting mechanisms to enhance therapeutic outcomes. The combination of orexin receptor agonism with CTSH inhibition represents a sophisticated approach to tackling complex disorders. This multifaceted strategy not only focuses on symptom management but also aims to slow disease progression, which could be a game-changer in the treatment of neurodegenerative diseases.

From a technical standpoint, the shift away from sulfonamide derivatives addresses a critical need for safer medication profiles. Investors should note that this innovation could set a new standard in the industry, potentially disrupting current treatment paradigms and opening new revenue streams for NLS Pharmaceutics.

ZURICH, SWITZERLAND / ACCESSWIRE / June 11, 2024 / NLS Pharmaceutics Ltd. (NASDAQ:NLSP)(NASDAQ:NLSPW) ("NLS" or the "Company"), a Swiss clinical-stage biopharmaceutical company dedicated to pioneering therapies for rare and complex central nervous system disorders, today announced the publication of the latest patent application (PCT/WO2024115797) by Aexon Labs with the World Intellectual Property Organization (WIPO). The patent will be used by NLS pursuant to its existing and previously announced license agreement with Aexon Labs.

"This new patent application covers groundbreaking advancements in a novel series of dual orexin receptor agonists targeting narcolepsy as the primary indication and neurodegenerative conditions such as Parkinson's disease as secondary indications," said Eric Konofal, MD, PhD, Chief Scientific Officer of NLS Pharmaceutics, President of Aexon Labs, and inventor of the Dual Orexin Receptor Agonist platform (DOXA). "This application highlights the continued commitment from NLS to pioneer therapeutic approaches to address significant unmet medical needs."

Key Highlights :

• Innovative Dual Orexin Receptor Agonists: The patent application introduces a completely new series of molecules, licensed to NLS from Aexon Labs, acting primarily as dual orexin receptor agonists (OX1R and OX2R). These multitarget compounds have demonstrated efficacy in vitro, showing potential to not only mitigate narcolepsy symptoms, but also to slow the progression of neurodegenerative diseases.
• Non-Sulfonamide Compounds: Unlike many current treatments acting as orexin receptor agonists, these innovative non-sulfonamide derivatives have the potential to reduce the risk of side effects and adverse reactions associated with traditional sulfonamide medications. This characteristic may both broaden their potential use and improve patient safety.
• Mechanism of Action: The new molecules enhance neurotransmitter release and protect neuronal health by modulating orexin receptors (OX1R/OX2R) and integrating neuroinflammation protection through cathepsin H (CTSH) inhibition. This combined action targets both sleep regulation and neurodegeneration, offering the potential for significant therapeutic benefits for patients.
• Therapeutic Implications: CTSH is involved in proteolytic degradation and antigen presentation, influencing autoimmune responses in narcolepsy. Inhibiting CTSH could protect neuronal cells by disrupting the proteolytic pathway. When combined with dual orexin receptor agonist action, this approach could significantly enhance orexin signaling stability and mitigate symptoms. Neuroprotective strategies focusing on reducing neuroinflammation and modulating immune responses could further improve therapeutic outcomes.
• Focus on Narcolepsy: These compounds are designed primarily to treat narcolepsy by activating orexin pathways, which are crucial for maintaining wakefulness and regulating sleep patterns. By addressing the core pathology of narcolepsy, these dual orexin receptor agonists provide a novel and effective treatment approach.
• Application in Neurodegenerative Diseases: Beyond narcolepsy, these multitarget molecules show promise for treating conditions like Parkinson's disease by targeting neurodegenerative processes such as OX1R and a-synuclein. This represents a significant advancement in developing treatments that could improve quality of life and disease outcomes for patients.

Recent Advances and Presentations from NLS Pharmaceutics and Aexon Labs:

At Sleep 2024 (Houston, June 1-5), data on selective OX2R agonists highlighted their limitations, including receptor desensitization and reduced efficacy at higher doses. In contrast, a new generation of compounds from Aexon Labs, presented at the 2024 ASCP Annual Meeting (Miami, May 27-31), targets both OX1R and OX2R while also preventing the destruction of orexin cells through an inhibitory effect on CTSH. These multitarget compounds, with their broader affinity, show fewer issues related to high-affinity binding and efficacy loss, suggesting a more stable pharmacological profile and better long-term outcomes.

About Narcolepsy

Narcolepsy is a lifelong sleep disorder caused by the autoimmune-mediated loss of 70,000-90,000 orexin-producing neurons in the hypothalamus. It is characterized by excessive daytime sleepiness, cataplexy, and rapid eye movement (REM) sleep abnormalities, and is tightly associated with the human leukocyte antigen HLA-DQB1*06:02. Other predisposing factors for narcolepsy include associations with polymorphisms in the T-cell receptor alpha and beta genes, whose products recognize antigens presented by HLA molecules, and the CTSH gene.

About NLS Pharmaceutics Ltd.

NLS is a global development-stage biopharmaceutical company, working with a network of world-class partners and internationally recognized scientists, focused on the discovery and development of innovative therapies for patients with rare and complex central nervous system disorders who have unmet medical needs. Headquartered in Switzerland and founded in 2015, NLS is led by an experienced management team with a track record of developing and commercializing product candidates. For more information, please visit www.nlspharma.com.

About Aexon Labs, Inc.

Aexon Labs is conducting leading edge research on new compounds to address unmet needs in neurodegenerative disorders, defined by the breakdown of neurons over time. Alzheimer's, Parkinson's, Huntington's, Narcolepsy and Amyotrophic Lateral Sclerosis are just a few examples of brain disorders that have no cure. Current treatments do not address the root cause of each disorder and often lack therapeutical effectiveness and safety for these neurological disorders. Eric Konofal, MD, PhD, Chief Scientific Officer of NLS Pharmaceutics, is also the president and founder of Aexon Labs. Both Dr. Konofal and Alex Zwyer, CEO of NLS Pharmaceutics are shareholders of Aexon Labs.

Safe Harbor Statement

This press release contains expressed or implied forward-looking statements pursuant to U.S. Federal securities laws. For example, NLS is using forward-looking statements when it discusses the potential benefits of NLS' and Aexon Labs' products and the new patent. These forward-looking statements and their implications are based on the current expectations of the management of NLS only and are subject to a number of factors and uncertainties that could cause actual results to differ materially from those described in the forward-looking statements. The following factors, among others, could cause actual results to differ materially from those described in the forward-looking statements: changes in technology and market requirements; NLS may encounter delays or obstacles in launching and/or successfully completing its clinical trials; NLS' products may not be approved by regulatory agencies, NLS' technology may not be validated as it progresses further and its methods may not be accepted by the scientific community; NLS may be unable to retain or attract key employees whose knowledge is essential to the development of its products; unforeseen scientific difficulties may develop with NLS' process; NLS' products may wind up being more expensive than it anticipates; results in the laboratory may not translate to equally good results in real clinical settings; results of preclinical studies may not correlate with the results of human clinical trials; NLS' patents may not be sufficient; NLS' products may harm recipients; changes in legislation may adversely impact NLS; inability to timely develop and introduce new technologies, products and applications; and loss of market share and pressure on pricing resulting from competition, which could cause the actual results or performance of NLS to differ materially from those contemplated in such forward-looking statements. Except as otherwise required by law, NLS undertakes no obligation to publicly release any revisions to these forward-looking statements to reflect events or circumstances after the date hereof or to reflect the occurrence of unanticipated events. More detailed information about the risks and uncertainties affecting NLS is contained under the heading "Risk Factors" in NLS' annual report on Form 20-F for the year ended December 31, 2023 filed with the Securities and Exchange Commission (SEC), which is available on the SEC's website, www.sec.gov, and in subsequent filings made by NLS with the SEC.

Contact:

Investor Relations Contact
InvestorRelations@nls-pharma.com
www.nlspharmaceutics.com

SOURCE: NLS Pharmaceutics AG

View the original press release on accesswire.com

FAQ

What did NLS Pharmaceutics announce on June 11, 2024?

NLS Pharmaceutics announced a new patent application for dual orexin receptor agonists (DOXA) targeting narcolepsy and neurodegenerative diseases.

What conditions are targeted by the new patent application NLSP announced?

The patent targets narcolepsy as the primary indication and neurodegenerative diseases such as Parkinson's disease.

What are dual orexin receptor agonists?

Dual orexin receptor agonists are compounds that modulate orexin receptors (OX1R and OX2R) to enhance wakefulness and combat neurodegeneration.

What are the benefits of non-sulfonamide compounds mentioned in NLSP's patent?

Non-sulfonamide compounds reduce the risk of side effects and adverse reactions associated with traditional sulfonamide medications.

How do the new compounds in NLSP's patent help in treating neurodegenerative diseases?

These compounds enhance neurotransmitter release, protect neuronal health, and inhibit cathepsin H (CTSH), potentially slowing neurodegeneration.

What recent advances were presented by NLS Pharmaceutics and Aexon Labs?

At recent conferences, data indicated that the new compounds avoid issues like receptor desensitization and high-affinity binding, suggesting better long-term outcomes.