NLRP3 Protein Inhibitors - Pipeline Insight, 2024

This “NLRP3 Protein Inhibitors- Pipeline Insight, 2024” report provides comprehensive insights about 20+ companies and 25+ pipeline drugs in NLRP3 Protein Inhibitors pipeline landscape. It covers the pipeline drug profiles, including clinical and nonclinical stage products. It also covers the therapeutics assessment by product type, stage, route of administration, and molecule type. It further highlights the inactive pipeline products in this space.

Geography Covered

• Global coverage

NLRP3 Protein Inhibitors: Understanding

NLRP3 Protein Inhibitors: Overview

NLRP3 inhibitors are a promising class of drugs targeting the NLRP3 inflammasome, a critical regulator of the innate immune system involved in inflammation. By blocking the activation of the NLRP3 inflammasome, these inhibitors help reduce excessive or chronic inflammation, which is implicated in various diseases. The NLRP3 (NOD-, LRR-, and pyrin domain-containing protein 3) inflammasome is a multi-protein complex that, when activated, leads to the production of pro-inflammatory cytokines like IL-1β and IL-18.

NLRP3 is a sensor protein in the NLR family, consisting of three key domains: the Pyrin domain (PYD), which interacts with other proteins like ASC to form the inflammasome complex; the NACHT domain, responsible for oligomerization and ATP binding, critical for NLRP3 activation; and the Leucine-rich repeat (LRR) domain, involved in sensing cellular changes and maintaining the protein's inactive state until activation. When the NLRP3 inflammasome is activated, the protein undergoes a conformational change, leading to oligomerization and recruitment of ASC and caspase-1, triggering downstream inflammatory responses.

The NLRP3 inflammasome is a multiprotein complex crucial for the innate immune response, detecting danger signals and activating caspase-1, which processes pro-inflammatory cytokines IL-1β and IL-18. It is triggered by a wide range of signals, including PAMPs, DAMPs, and environmental stressors. Overactivation of the NLRP3 in Therapeutic Implications flammasome is linked to numerous diseases, such as autoimmune, neurodegenerative, metabolic, and cardiovascular disorders. Inhibitors like MCC950 are being explored as potential therapies to reduce chronic inflammation by blocking inflammasome activation and pyroptosis.

The NLRP3 inflammasome plays a key role in detecting danger signals and triggering inflammation through the release of cytokines IL-1β and IL-18. Dysregulation of NLRP3 is implicated in various diseases. In autoimmune diseases like rheumatoid arthritis and lupus, it promotes chronic inflammation and tissue damage. In metabolic disorders such as type 2 diabetes, obesity, and gout, NLRP3 activation drives insulin resistance and joint inflammation. It also contributes to neurodegenerative diseases like Alzheimer’s and Parkinson’s, as well as cardiovascular diseases like atherosclerosis and heart damage post-myocardial infarction.

Additionally, genetic mutations in NLRP3 cause autoinflammatory syndromes like CAPS, leading to excessive inflammation. Targeting the NLRP3 inflammasome in these diseases offers a novel therapeutic strategy. Inhibitors like MCC950 and dapansutrile aim to reduce IL-1β and IL-18 production, mitigating the inflammatory response and preventing disease progression.In summary, the NLRP3 inflammasome contributes to the pathophysiology of various inflammatory diseases by amplifying immune responses, making it a key target for developing anti-inflammatory therapies.

"NLRP3 Protein Inhibitors- Pipeline Insight, 2024" report outlays comprehensive insights of present scenario and growth prospects across the indication. A detailed picture of the NLRP3 Protein Inhibitors pipeline landscape is provided which includes the disease overview and NLRP3 Protein Inhibitors treatment guidelines. The assessment part of the report embraces, in depth NLRP3 Protein Inhibitors commercial assessment and clinical assessment of the pipeline products under development. In the report, detailed description of the drug is given which includes mechanism of action of the drug, clinical studies, NDA approvals (if any), and product development activities comprising the technology, NLRP3 Protein Inhibitors collaborations, licensing, mergers and acquisition, funding, designations and other product related details.

Report Highlights

The companies and academics are working to assess challenges and seek opportunities that could influence NLRP3 Protein Inhibitors R&D. The therapies under development are focused on novel approaches to treat/improve NLRP3 Protein Inhibitors.

NLRP3 Protein Inhibitors Emerging Drugs Chapters

This segment of the NLRP3 Protein Inhibitors report encloses its detailed analysis of various drugs in different stages of clinical development, including phase III, II, II/III I, preclinical and Discovery. It also helps to understand clinical trial details, expressive pharmacological action, agreements and collaborations, and the latest news and press releases.

NLRP3 Protein Inhibitors Emerging Drugs

Diacerein: Castle Creek Pharmaceuticals

Diacerein is a slow-acting, small molecular weight compound of the class anthraquinone with potent anti-inflammatory properties. Diacerein and its active metabolite rhein have been shown to inhibit the in vitro and in vivo production and activity of IL-1β and other pro-inflammatory cytokines. CCP-020 is a formulation of diacerein, 1% ointment developed for topical application.

Diacerein in the formulation is hydrolyzed to rhein in the epidermis and dermis following administration and is believed to block an inflammatory signaling pathway associated with EBS resulting in strengthening epidermal tissue and healing of skin blisters. Currently, the drug is in the Phase III stage of its development for the treatment of Epidermolysis bullosa.

HT6184: Halia Therapeutics

HT-6184 represents an innovative approach as it is the first drug candidate to target the protein NEK7 through an allosteric mechanism. NEK7 is an essential component of the NLRP3 inflammasome and is critical for its assembly and the maintenance of NLRP3 activity. In preclinical models, Halia has shown that inhibiting the ability of NEK7 to bind to NLRP3 leads to a disruption in the formation of the NLRP3 inflammasome complex, thereby inhibiting the signaling from the inflammasome and reducing the inflammatory response. Preclinical models also showed that in addition to disrupting the formation of the NLRP3 inflammasome, HT-6184 promotes the disassembly of the inflammasome once activated (Halia unpublished data). Currently, the drug is in the Phase II stage of its development for the treatment of Inflammatory Pain.

VENT 02: Ventus Therapeutics

VENT-02, is the most advanced wholly-owned program, is a highly potent and selective brain-penetrant NLRP3 inhibitor. The Phase I clinical trial of VENT-02 has been completed. The trial evaluated the pharmacodynamics, pharmacokinetics, safety, and tolerability of VENT-02 across a broad range of single and multiple ascending doses. In this Phase I clinical trial, VENT-02 was well-tolerated, with no dose-limiting toxicities or serious adverse events reported. VENT-02 demonstrated full target engagement through 100% inhibition of IL-1β in the blood in an ex vivo whole blood challenge assay, significant drug levels in the CSF for 24 hours, and robust reduction of inflammatory biomarkers such as hsCRP. In addition, VENT-02 demonstrated potential for once-daily dosing.

NLRP3 Protein Inhibitors: Therapeutic Assessment

This segment of the report provides insights about the different NLRP3 Protein Inhibitors drugs segregated based on following parameters that define the scope of the report, such as:

Major Players in NLRP3 Protein Inhibitors

There are approx. 20+ key companies which are developing the therapies for NLRP3 Protein Inhibitors. The companies which have their NLRP3 Protein Inhibitors drug candidates in the most advanced stage, i.e. Phase III include, Castle Creek Pharmaceuticals.

Phases

The report covers around 25+ products under different phases of clinical development like

• Late stage products (Phase III)
• Mid-stage products (Phase II)
• Early-stage product (Phase I) along with the details of
• Pre-clinical and Discovery stage candidates
• Discontinued & Inactive candidates

Route of Administration

NLRP3 Protein Inhibitors pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration. Products have been categorized under various ROAs such as

• Intravenous
• Subcutaneous
• Oral
• Intramuscular
• Molecule Type

Products have been categorized under various Molecule types such as

• Monoclonal antibody
• Small molecule
• Peptide
• Product Type

Drugs have been categorized under various product types like Mono, Combination and Mono/Combination.

NLRP3 Protein Inhibitors: Pipeline Development Activities

The report provides insights into different therapeutic candidates in phase II, I, preclinical and discovery stage. It also analyses NLRP3 Protein Inhibitors therapeutic drugs key players involved in developing key drugs.

Pipeline Development Activities

The report covers the detailed information of collaborations, acquisition and merger, licensing along with a thorough therapeutic assessment of emerging NLRP3 Protein Inhibitors drugs.

NLRP3 Protein Inhibitors Report Insights

• NLRP3 Protein Inhibitors Pipeline Analysis
• Therapeutic Assessment
• Unmet Needs
• Impact of Drugs

NLRP3 Protein Inhibitors Report Assessment

• Pipeline Product Profiles
• Therapeutic Assessment
• Pipeline Assessment
• Inactive drugs assessment
• Unmet Needs

Key Questions

Current Treatment Scenario and Emerging Therapies:

• How many companies are developing NLRP3 Protein Inhibitors drugs?
• How many NLRP3 Protein Inhibitors drugs are developed by each company?
• How many emerging drugs are in mid-stage, and late-stage of development for the treatment of NLRP3 Protein Inhibitors?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the NLRP3 Protein Inhibitors therapeutics?
• What are the recent trends, drug types and novel technologies developed to overcome the limitation of existing therapies?
• What are the clinical studies going on for NLRP3 Protein Inhibitors and their status?
• What are the key designations that have been granted to the emerging drugs?

Key Players

• Castle Creek Pharmaceuticals
• Halia Therapeutics
• Ventus Therapeutics
• EpicentRx
• Zydus Lifesciences Limited
• Monte Rosa Therapeutics
• Inflammasome Therapeutics
• Ventyx Biosciences
• Biolexis Therapeutics/Halia Therapeutics
• Olatec Therapeutics
• Ryvu Therapeutics

Key Products

• Diacerein
• HT6184
• VENT 02
• Nibrozetone
• ZYIL1
• MRT-8102
• Kamuvudine-9
• VTX 3232
• NLRP3 inflammasome inhibitor
• Dapansutrile
• NT 0796

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