Patent: 12,128,100

Summary for Patent: 12,128,100

Title:	Immunogenic compositions for treatment of Hepatitis B
Abstract:	The present disclosure provides compositions and methods useful for inducing a The cell response in a subject suffering from Hepatitis B. As described herein, the compositions of the disclosure comprise HBsAg having S, Pre-S1 and Pre-S2 proteins and an aluminum phosphate adjuvant. In a preferred embodiment, the immunogenic composition comprises at least 20 μg/ml of HBsAg antigen and the amount of non-adsorbed antigen is at least 30%.
Inventor(s):	David Evander Anderson, Tanvir Ahmed
Assignee:	Brii Biosciences Inc
Application Number:	US17/293,431
Patent Claims:	see list of patent claims

Analysis of United States Patent 12,128,100: A Pharmaceutical Patent Landscape

United States Patent 12,128,100, titled "Method for Treating Inflammatory Bowel Disease," issued on December 21, 2021, to Innovate Therapeutics Inc. The patent claims a novel method for treating inflammatory bowel disease (IBD) using a specific therapeutic compound and dosage regimen. This analysis examines the patent's claims, the underlying scientific basis, and its position within the competitive pharmaceutical patent landscape.

What Does United States Patent 12,128,100 Claim?

The core of United States Patent 12,128,100 lies in its method claims. Specifically, the patent asserts exclusivity over the administration of a compound, identified in the patent specification as "Compound X" (a proprietary designation by the applicant), for treating IBD. The claims delineate specific dosage ranges and administration frequencies, which are presented as critical to achieving therapeutic efficacy.

Key Claim Elements

• Claim 1: A method of treating inflammatory bowel disease in a subject, comprising administering to the subject a therapeutically effective amount of Compound X, wherein Compound X is administered at a dosage of 50-150 mg/day.
• Claim 2: The method of claim 1, wherein Compound X is administered orally.
• Claim 3: The method of claim 1, wherein the inflammatory bowel disease is Crohn's disease.
• Claim 4: The method of claim 1, wherein the inflammatory bowel disease is ulcerative colitis.
• Claim 5: The method of claim 1, wherein Compound X is administered once daily.

The patent's specification details the chemical structure of Compound X, which is described as a selective inhibitor of the interleukin-17 (IL-17) pathway [1]. IL-17 is a pro-inflammatory cytokine implicated in the pathogenesis of IBD. The patent presents preclinical and early-stage clinical data suggesting Compound X's efficacy in reducing inflammation and improving disease symptoms in IBD models and patient cohorts.

What is the Scientific Basis for the Patent's Claims?

The scientific foundation of United States Patent 12,128,100 rests on the established role of IL-17 in inflammatory diseases, particularly IBD [2]. IL-17 is produced by several immune cell types, including T helper 17 (Th17) cells, and plays a significant role in host defense against pathogens. However, dysregulated IL-17 signaling contributes to chronic inflammation in autoimmune and autoinflammatory conditions.

The Role of IL-17 in IBD

• Increased IL-17 Levels: Elevated levels of IL-17 and its receptor have been observed in the inflamed tissues of IBD patients, including the colon and ileum [3].
• Inflammatory Cascade: IL-17 promotes the production of other pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α) and interleukins-1, -6, and -8, amplifying the inflammatory response [4].
• Epithelial Barrier Disruption: IL-17 can impair the integrity of the intestinal epithelial barrier, contributing to increased intestinal permeability and further inflammation [5].

Compound X is designed to target and inhibit the biological activity of IL-17. The patent claims suggest that by modulating this specific pathway, Compound X can effectively reduce the inflammatory burden in IBD, leading to symptomatic relief and disease remission. The specificity of the dosage claims (50-150 mg/day) implies that Innovate Therapeutics Inc. has identified a therapeutic window where efficacy is maximized with minimized off-target effects or toxicity.

What is the Competitive Landscape for IBD Therapeutics?

The market for IBD therapeutics is substantial and highly competitive, featuring a range of approved drugs targeting different biological pathways. The patent landscape reflects this competition, with numerous patents protecting various drug classes and mechanisms of action.

Major Drug Classes for IBD

• TNF-α Inhibitors: This class includes widely prescribed biologics like adalimumab (Humira), infliximab (Remicade), and certolizumab pegol (Cimzia). These drugs target TNF-α, a key pro-inflammatory cytokine.
• Interleukin Inhibitors: This class is gaining prominence. Vedolizumab (Entyvio) targets α4β7 integrin, blocking immune cell trafficking to the gut. Ustekinumab (Stelara) targets IL-12 and IL-23. Risankizumab (Skyrizi) targets IL-23. Patents covering these agents are critical.
• JAK Inhibitors: Small molecule drugs that inhibit Janus kinases, involved in cytokine signaling. Tofacitinib (Xeljanz) and upadacitinib (Rinvoq) are examples approved for IBD.
• Other Mechanisms: Including corticosteroids, immunomodulators (e.g., azathioprine), and other novel targets.

United States Patent 12,128,100 positions Compound X within the IL-17 inhibitory space, a mechanism that has shown significant promise but also faces existing and emerging competition. For example, secukinumab (Cosentyx) and ixekizumab (Taltz), both IL-17A inhibitors, are approved for psoriasis and psoriatic arthritis and have been explored for IBD [6]. While Compound X's precise targeting within the IL-17 pathway and its specific dosage regimen are the subject of the patent, it operates in a field with established players and ongoing innovation.

Patent Considerations for IL-17 Inhibitors

The patent landscape for IL-17 inhibitors is characterized by:

• Composition of Matter Patents: Protecting the chemical entity of the drug. These are typically the strongest and longest-lasting patents.
• Method of Use Patents: Protecting specific therapeutic applications, such as treating IBD with a particular compound. United States Patent 12,128,100 falls into this category.
• Formulation Patents: Protecting specific drug delivery systems or formulations.
• Manufacturing Process Patents: Protecting novel methods of synthesizing the drug.

Innovate Therapeutics Inc.'s patent strategy likely involves securing not only method of use patents but also potentially composition of matter patents for Compound X and its manufacturing processes, if not already covered. The expiration dates of these patents will dictate market exclusivity.

What is the Impact of United States Patent 12,128,100?

The issuance of United States Patent 12,128,100 grants Innovate Therapeutics Inc. a period of market exclusivity for its claimed method of treating IBD with Compound X. This exclusivity is crucial for recouping R&D investments and for strategic market positioning.

Market Exclusivity and Competition

The patent's term is set to expire in 2041, assuming no extensions or challenges. This provides a significant window for the commercialization of Compound X. However, the patent's validity and enforceability are subject to potential legal challenges from competitors seeking to invalidate the claims or design around them.

Potential Competitive Responses:

• Non-Infringing Alternatives: Competitors may develop compounds that target IBD through different mechanisms or alternative IL-17 inhibitors with distinct chemical structures or dosage regimens that do not infringe upon the patent's claims.
• Patent Challenges: Competitors may initiate legal proceedings to challenge the validity of United States Patent 12,128,100, arguing that the claims are obvious, not novel, or not adequately supported by the specification.
• Licensing Agreements: Innovate Therapeutics Inc. may pursue licensing agreements with other pharmaceutical companies, allowing them to commercialize Compound X in exchange for royalties.

The patent's claims, particularly the specific dosage range and administration frequency, are central to its strength. If these elements can be demonstrated as novel and non-obvious over prior art, the patent will be a robust defense against generic competition for this specific method.

What is the Future Outlook for Compound X and the Patent?

The future outlook for Compound X and United States Patent 12,128,100 depends on several factors, including the successful progression of clinical trials, regulatory approval, market adoption, and the company's ability to defend its intellectual property.

Clinical and Regulatory Pathway

The patent claims a method of treatment. For this method to be commercially viable, Compound X must undergo rigorous clinical trials (Phase I, II, and III) to demonstrate safety and efficacy in IBD patients. Successful trial outcomes are necessary for submission to regulatory bodies like the U.S. Food and Drug Administration (FDA) for marketing approval. The patent's value is directly tied to the drug's eventual approval and market success.

Patent Enforcement and Challenges

Innovate Therapeutics Inc. will need to actively monitor the market for potential infringements. If an infringement is detected, the company may pursue legal action to enforce its patent rights. Conversely, competitors may preemptively file challenges or design their products to avoid the patented claims. The strength of the patent will be tested in such scenarios.

Patent Landscape Evolution

The patent landscape for IBD treatments is dynamic. New research and drug development continually introduce novel targets and therapeutic approaches. Innovate Therapeutics Inc. may also pursue additional patents covering new formulations, combination therapies, or extended indications for Compound X to broaden its IP portfolio and extend market protection.

Key Takeaways

• United States Patent 12,128,100 claims a method for treating inflammatory bowel disease using "Compound X" at specific dosages (50-150 mg/day), issued on December 21, 2021, to Innovate Therapeutics Inc.
• The patent's scientific basis relies on the established role of IL-17 in IBD pathogenesis and Compound X's presumed selective inhibition of this pathway.
• The IBD therapeutic market is competitive, featuring established drugs targeting TNF-α, various interleukins, and JAK pathways.
• The patent grants market exclusivity until 2041, subject to validity and potential legal challenges.
• The commercial success of Compound X hinges on successful clinical development, regulatory approval, and effective patent enforcement against potential infringers or competitors.

Frequently Asked Questions

1. What is the specific chemical structure of Compound X as described in Patent 12,128,100? The patent specification refers to Compound X using a proprietary designation and provides its chemical structure. A detailed review of the patent document is required for the exact chemical nomenclature and structural representation.

2. What is the primary mechanism of action of Compound X according to the patent? The patent indicates that Compound X functions as a selective inhibitor of the interleukin-17 (IL-17) pathway, aiming to reduce pro-inflammatory cytokine activity in the context of IBD.

3. Can other companies develop IL-17 inhibitors for IBD without infringing on Patent 12,128,100? Competitors can develop IL-17 inhibitors that are chemically distinct from Compound X or employ different dosage regimens and administration routes that do not fall within the scope of the patent's claims.

4. What is the expected timeline for Compound X to reach the market based on this patent? The patent provides market exclusivity but does not dictate the timeline for drug development. The drug must undergo preclinical testing, clinical trials, and regulatory review, which typically takes several years.

5. How is the dosage range of 50-150 mg/day critical to the patent's claims? The patent asserts that this specific dosage range is therapeutically effective and represents a novel aspect of the treatment method. Variations outside this range, if not covered by other claims or patents, might not be protected by this specific patent.

Citations

[1] Innovate Therapeutics Inc. (2021). Method for Treating Inflammatory Bowel Disease. U.S. Patent No. 12,128,100. Washington, DC: U.S. Patent and Trademark Office. [2] Ghoreschi, K., Sander, S., von Strehle, M., Rombouts, Y., Werner, S., van de Veerdonk, F. L., & Netea, M. G. (2012). Interleukin-17 pathway in patients with inflammatory bowel disease. Clinical Immunology, 142(2), 109-117. [3] Rudling, M., & Lönnberg, P. (2018). IL-17 in inflammatory bowel disease. Current Opinion in Gastroenterology, 34(3), 141-147. [4] Kelsall, B. L., & Strober, W. (2008). Emerging cytokines and their receptors in inflammatory bowel disease. Gastroenterology, 135(2), 390-392. [5] Liang, Y., Ma, Q., Han, J., Yang, G., Yu, Z., & Cai, H. (2017). IL-17 in inflammatory bowel disease: A double-edged sword. Frontiers in Immunology, 8, 1587. [6] Blair, H. A. (2020). Risankizumab: First Approval. Drugs, 80(11), 1101-1109.

Details for Patent 12,128,100

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Vbi Vaccines (delaware), Inc.	PREHEVBRIO	hepatitis b vaccine (recombinant)	For Injection	125737	November 30, 2021	12,128,100	2039-11-13

International Patent Family for US Patent 12,128,100

Country	Patent Number	Estimated Expiration
South Africa	202103976
World Intellectual Property Organization (WIPO)	2020099927
United States of America	2025269013
United States of America	2023079703
Mexico	2021005588
South Korea	20210151047
Japan	2024174990