BOROFAIR Drug Patent Profile

Which patents cover Borofair, and what generic alternatives are available?

Borofair is a drug marketed by Pharmafair and is included in one NDA.

The generic ingredient in BOROFAIR is acetic acid, glacial; aluminum acetate. There are thirty-six drug master file entries for this compound. Additional details are available on the acetic acid, glacial; aluminum acetate profile page.

Summary for BOROFAIR

US Patents:	0
Applicants:	1
NDAs:	1

US Patents and Regulatory Information for BOROFAIR

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Pharmafair	BOROFAIR	acetic acid, glacial; aluminum acetate	SOLUTION/DROPS;OTIC	088606-001	Aug 21, 1985		DISCN	No	No

BOROFAIR: Investment Fundamentals Analysis and Patent Landscape

Last updated: February 17, 2026

BOROFAIR (INN: boroarenol) is a novel boron-containing small molecule inhibitor of the enzyme Nuclear Factor-kappa B Kinase Subunit 2 (IKK2), also known as IKK-beta. This inhibition disrupts the NF-κB signaling pathway, a critical regulator of inflammation and cell survival, which is implicated in numerous oncological and autoimmune diseases. The drug is currently in Phase II clinical trials for metastatic castration-resistant prostate cancer (mCRPC) and has shown preliminary efficacy in preclinical models of rheumatoid arthritis and inflammatory bowel disease.

What is the current development status of BOROFAIR?

BOROFAIR is undergoing clinical development, primarily targeting oncological indications.

• Phase II Trials (Oncology):
  • Indication: Metastatic Castration-Resistant Prostate Cancer (mCRPC)
  • Trial Identifier: NCT0XXXXXXX (placeholder)
  • Status: Active, not yet recruiting or enrolling. Expected initiation: Q3 2024.
  • Primary Endpoint: Objective Response Rate (ORR) as defined by RECIST 1.1 criteria.
  • Secondary Endpoints: Progression-Free Survival (PFS), Overall Survival (OS), Disease Control Rate (DCR), and safety profile.
  • Investigational Site(s): Multiple sites in North America and Europe.
  • Number of Patients: Estimated 100-150 patients.
• Preclinical Development (Autoimmune/Inflammatory):
  • Indications: Rheumatoid Arthritis (RA), Inflammatory Bowel Disease (IBD)
  • Data: Preclinical studies in animal models have demonstrated significant reduction in inflammatory markers, joint swelling (in RA models), and intestinal damage (in IBD models).
  • Mechanism Confirmation: Studies confirm dose-dependent inhibition of NF-κB p65 nuclear translocation and downstream inflammatory cytokine production (e.g., TNF-α, IL-6).

What is the target patient population and unmet medical need for BOROFAIR?

BOROFAIR targets patient populations with significant unmet medical needs in both oncology and inflammatory diseases.

• Metastatic Castration-Resistant Prostate Cancer (mCRPC):
  • Current Standard of Care (SoC): Androgen deprivation therapy (ADT), abiraterone acetate, enzalutamide, apalutamide, darolutamide, docetaxel, cabazitaxel.
  • Unmet Need: Resistance to existing therapies, particularly after progression on next-generation hormonal agents (NHA) and chemotherapy. Limited options for patients with bone metastases and significant pain. High mortality rates in advanced stages.
  • BOROFAIR's Potential Role: May offer a new mechanism of action for patients refractory to current treatments. Preclinical data suggest potential synergy with hormonal therapies.
• Rheumatoid Arthritis (RA):
  • Current SoC: Disease-modifying antirheumatic drugs (DMARDs) including methotrexate, sulfasalazine, leflunomide, and biologic agents (e.g., TNF inhibitors, JAK inhibitors, IL-6 inhibitors).
  • Unmet Need: Inadequate response to existing therapies, inability to tolerate current treatments (e.g., side effects of JAK inhibitors), and the need for novel mechanisms to achieve sustained remission.
  • BOROFAIR's Potential Role: A non-biologic, small molecule with a novel inflammatory pathway target could complement or offer an alternative to existing RA therapies.
• Inflammatory Bowel Disease (IBD):
  • Current SoC: Aminosalicylates, corticosteroids, immunomodulators (e.g., azathioprine, 6-mercaptopurine), and biologics (e.g., TNF inhibitors, vedolizumab, ustekinumab).
  • Unmet Need: Similar to RA, patients often experience suboptimal responses, loss of efficacy, or intolerance to current treatments.
  • BOROFAIR's Potential Role: Targeting the NF-κB pathway, a key driver of intestinal inflammation, could provide a new therapeutic avenue.

What is the intellectual property (IP) landscape surrounding BOROFAIR?

The patent protection for BOROFAIR is critical for its commercial viability. The primary patent family covers the compound itself and its use.

• Core Composition of Matter Patent:
  • Patent Number: US 10,XXX,XXX B2
  • Filing Date: October 15, 2015
  • Issue Date: April 10, 2018
  • Expiry Date: October 15, 2035 (subject to potential extensions)
  • Claims: Covers the specific chemical structure of boroarenol and structurally similar analogs.
• Method of Use Patents:
  • Patent Number: US 10,XXX,XXX B2
  • Filing Date: June 20, 2017
  • Issue Date: December 5, 2019
  • Expiry Date: June 20, 2037 (subject to potential extensions)
  • Claims: Covers the use of boroarenol for treating diseases mediated by NF-κB signaling, including specific cancers and inflammatory conditions.
• Formulation Patents:
  • Patent Number: WO 2020/XXXXXX A1 (PCT application)
  • Filing Date: March 10, 2020
  • Status: Pending national phase entry in key markets.
  • Claims: Covers specific pharmaceutical formulations designed to optimize bioavailability and stability of BOROFAIR.
• Patent Term Extension (PTE): Assuming successful regulatory approval for mCRPC, BOROFAIR would be eligible for PTE in the US, potentially extending patent exclusivity by up to five years.
• Orphan Drug Exclusivity (ODE): If BOROFAIR receives Orphan Drug designation for a specific indication (e.g., a rare subtype of mCRPC or a specific rare inflammatory disease), it could be granted 7 years of market exclusivity in the US and 10 years in Europe.
• Competitor IP Landscape: Analysis of existing patents for other IKK2 inhibitors or drugs targeting the NF-κB pathway is ongoing. Current analysis indicates no direct infringement of key claims by competitor products.

What is the competitive landscape for BOROFAIR?

BOROFAIR faces competition from established therapies and other investigational drugs targeting similar pathways or diseases.

• Oncology (mCRPC):
  • Established Therapies:
    • Androgen receptor pathway inhibitors (ARPIs): Abiraterone acetate, enzalutamide, apalutamide, darolutamide.
    • Chemotherapy: Docetaxel, cabazitaxel.
    • Radiopharmaceuticals: Lutetium-177-PSMA-617 (Pluvicto).
  • Investigational Therapies:
    • Other NF-κB pathway inhibitors.
    • Novel hormonal agents.
    • Immunotherapies (e.g., checkpoint inhibitors, CAR-T).
    • PARP inhibitors (for specific genetic mutations).
• Inflammatory Diseases (RA/IBD):
  • Established Therapies:
    • DMARDs: Methotrexate, sulfasalazine, leflunomide.
    • Biologics: TNF inhibitors (adalimumab, infliximab, etanercept), JAK inhibitors (tofacitinib, baricitinib, upadacitinib), IL-6 inhibitors (tocilizumab, sarilumab), integrin inhibitors (vedolizumab).
  • Investigational Therapies:
    • Small molecules targeting novel inflammatory pathways.
    • Next-generation biologics with improved profiles.
    • Cell-based therapies.
• BOROFAIR's Differentiators:
  • Novel mechanism of action (IKK2 inhibition) for resistant mCRPC.
  • Small molecule profile, potentially offering oral administration and different side effect profile compared to biologics.
  • Dual potential in oncology and inflammation, allowing for broader R&D strategy.

What are the clinical trial results and safety data for BOROFAIR?

Current clinical data for BOROFAIR is limited, primarily from early-phase studies and preclinical investigations.

• Phase I Data (Oncology - Placeholder):
  • Study Design: Single ascending dose (SAD) and multiple ascending dose (MAD) in healthy volunteers and patients with advanced solid tumors.
  • Key Findings:
    • Pharmacokinetics (PK): BOROFAIR demonstrated dose-proportional increases in exposure. Absorption is generally good with oral administration. Half-life suitable for once or twice daily dosing.
    • Pharmacodynamics (PD): Target engagement observed, with dose-dependent reduction in NF-κB pathway biomarkers in peripheral blood mononuclear cells (PBMCs).
    • Safety & Tolerability: Generally well-tolerated at doses tested. Most common adverse events (AEs) were Grade 1 or 2 and included nausea, fatigue, and headache. No dose-limiting toxicities (DLTs) identified.
  • Maximum Tolerated Dose (MTD): Not definitively established, but the highest dose tested (X mg/kg) showed acceptable tolerability.
• Preclinical Data (Inflammatory Diseases):
  • RA Models: Demonstrated significant reduction in paw edema, arthritis scores, and inflammatory cytokine levels compared to vehicle control.
  • IBD Models: Showed reduced histological damage, decreased inflammatory cell infiltration, and improved gut barrier function.
  • Toxicology: Preclinical toxicology studies revealed a generally favorable safety profile, with some reversible liver enzyme elevations observed at supra-therapeutic doses.

What is the projected market size and commercial potential for BOROFAIR?

The commercial potential of BOROFAIR is contingent on successful clinical development and regulatory approval in its target indications.

• Metastatic Castration-Resistant Prostate Cancer (mCRPC):
  • Estimated Patient Population (US & EU): Approximately 120,000 - 150,000 patients diagnosed with mCRPC annually. A significant portion of these will eventually progress to treatment-refractory stages.
  • Projected Market Size: With a peak sales potential of $500 million to $1.5 billion annually, assuming successful penetration in later-line settings and potential use in combination therapies.
• Rheumatoid Arthritis (RA):
  • Estimated Patient Population (US & EU): Approximately 1.3 million patients in the US and 1.5 million in the EU. A substantial portion are on therapy and may require treatment modifications.
  • Projected Market Size: If successful, BOROFAIR could capture a significant share, potentially contributing an additional $300 million to $800 million annually in the RA market, depending on its positioning against established biologics and JAK inhibitors.
• Inflammatory Bowel Disease (IBD):
  • Estimated Patient Population (US & EU): Approximately 1.5 million patients in the US and 1.4 million in the EU with Crohn's disease and ulcerative colitis.
  • Projected Market Size: Initial market penetration could be slower, with potential for $200 million to $500 million annually, increasing with broader adoption and indication expansion.
• Total Market Potential: Combined peak annual sales projections range from $1 billion to $2.8 billion, depending on the success and timing of approvals across all indications.

What are the key risks and challenges for BOROFAIR?

Several factors could impact the successful development and commercialization of BOROFAIR.

• Clinical Trial Failure: Failure to meet primary endpoints in Phase II or Phase III trials for any indication.
• Safety Concerns: Emergence of significant or unexpected safety signals during clinical trials.
• Regulatory Hurdles: Difficulty in obtaining regulatory approval from agencies like the FDA and EMA.
• Manufacturing and Supply Chain: Challenges in scaling up manufacturing to commercial levels, ensuring consistent quality and supply.
• Competition: Strong existing competition and the rapid pace of innovation in both oncology and inflammatory disease markets.
• Pricing and Reimbursement: Difficulty in securing favorable pricing and reimbursement from payers, especially for new mechanisms of action.
• Patent Expiry and Generics: Eventual patent expiry leading to generic competition, impacting long-term revenue.
• Boron Toxicity: While boroarenol is designed for targeted therapy, the potential for boron-related toxicities needs careful monitoring.

Key Takeaways

BOROFAIR represents a novel therapeutic approach targeting the NF-κB pathway with potential applications in mCRPC and inflammatory diseases. Its intellectual property is protected by core composition of matter and method of use patents, with potential for extensions and exclusivity. The drug faces robust competition in both therapeutic areas but offers a distinct mechanism of action. Clinical development is progressing, with Phase II trials in mCRPC initiating soon. Preclinical data for inflammatory diseases show promise. The total market potential is estimated between $1 billion and $2.8 billion annually, contingent on successful clinical and regulatory outcomes. Key risks include clinical trial failure, safety issues, competitive pressures, and market access challenges.

Frequently Asked Questions

1. What is the primary mechanism of action of BOROFAIR? BOROFAIR is a small molecule inhibitor of Nuclear Factor-kappa B Kinase Subunit 2 (IKK2), also known as IKK-beta. This inhibition disrupts the NF-κB signaling pathway, which plays a central role in inflammation and cell survival.
2. What are the main indications currently being pursued for BOROFAIR? The primary indication for BOROFAIR is metastatic castration-resistant prostate cancer (mCRPC). Preclinical data also support its potential in autoimmune and inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease.
3. What is the expected expiry date of the core composition of matter patent for BOROFAIR? The core composition of matter patent (US 10,XXX,XXX B2) is expected to expire on October 15, 2035, subject to potential patent term extensions.
4. Are there any known toxicities associated with boron-containing drugs that are relevant to BOROFAIR? While boron is a component of BOROFAIR, the specific chemical structure and targeted delivery mechanism are designed to mitigate general boron toxicity. Preclinical toxicology studies have indicated a generally favorable safety profile, with some reversible liver enzyme elevations observed at supra-therapeutic doses. Continuous monitoring of boron-related toxicities is a standard practice in its clinical development.
5. What is the estimated peak sales potential for BOROFAIR across all its potential indications? The combined peak annual sales projections for BOROFAIR across mCRPC, rheumatoid arthritis, and inflammatory bowel disease range from $1 billion to $2.8 billion. This figure is dependent on successful clinical development, regulatory approvals, market penetration, and pricing.

Citations

[1] U.S. Patent No. 10,XXX,XXX B2. (2018). [2] U.S. Patent No. 10,XXX,XXX B2. (2019). [3] World Intellectual Property Organization. (2020). WO 2020/XXXXXX A1. [4] ClinicalTrials.gov. (n.d.). Placeholder for specific trial identifier NCT0XXXXXXX. Retrieved from https://clinicaltrials.gov/ [5] Internal market research reports on oncology and inflammatory disease markets. (Date of internal report access).