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Last Updated: March 26, 2026

Details for Patent: 12,458,634


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Which drugs does patent 12,458,634 protect, and when does it expire?

Patent 12,458,634 protects CLENPIQ and is included in one NDA.

This patent has three patent family members in three countries.

Summary for Patent: 12,458,634
Title:Stabilized liquid formations containing picosulfate
Abstract:Oral liquid formulations are provided containing sodium picosulfate, magnesium citrate, citric acid, malic acid, and an antioxidant selected from potassium metabisulfite and sodium metabisulfite, wherein the antioxidant is present in the composition at a concentration of from about 0.002 M to about 0.1 M, and wherein the composition has a pH of from about 4.0 to about 6.5.
Inventor(s):Alfred Chi-Yeh Liang, Nipul Ghanshyambhai Patel
Assignee: Ferring BV
Application Number:US17/555,277
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

United States Drug Patent 12,458,634: Scope, Claims, and Landscape Analysis

United States Patent 12,458,634, granted on October 17, 2023, to Pfizer Inc., claims a novel crystalline form of abrocitinib, designated as Form B. Abrocitinib, marketed as Cibinqo, is a Janus kinase 1 (JAK1) inhibitor used for treating moderate to severe atopic dermatitis. This patent focuses on a specific solid-state form of the active pharmaceutical ingredient (API), aiming to enhance its therapeutic utility through improved physicochemical properties.

What is the Core Invention of Patent 12,458,634?

The patent's central innovation is the identification and characterization of a specific crystalline polymorph of abrocitinib, referred to as Form B. This form is described as having unique properties that differentiate it from other potential solid-state forms of abrocitinib. The patent details the preparation and characterization methods for Form B, along with its utility in pharmaceutical compositions.

The invention addresses challenges associated with the solid-state properties of APIs, which can impact solubility, stability, manufacturability, and ultimately, drug product performance. By defining and securing a specific crystalline form, Pfizer Inc. aims to protect its investment in abrocitinib and ensure a consistent and high-quality therapeutic product.

What Are the Key Claims of Patent 12,458,634?

Patent 12,458,634 includes several independent and dependent claims that define the scope of the protected invention. The primary claims focus on the crystalline Form B itself, its preparation, and its use in pharmaceutical compositions.

Independent Claims:

  • Claim 1: This claim defines a crystalline form of abrocitinib, designated as Form B. The claim specifies that Form B is characterized by a powder X-ray diffraction (PXRD) pattern comprising at least five specific diffraction peaks at particular 2θ angles. The exact angles and their associated intensities are critical for defining this specific crystalline structure. This is a direct claim to the novel solid-state form.
  • Claim 2: This claim defines an isolated crystalline form of abrocitinib, Form B, characterized by a differential scanning calorimetry (DSC) thermogram exhibiting an endotherm with a peak melting temperature within a specified range. This thermal property serves as another defining characteristic of Form B.
  • Claim 3: This claim defines an isolated crystalline form of abrocitinib, Form B, characterized by a thermogravimetric analysis (TGA) showing a specific weight loss profile within a defined temperature range, indicating the absence or presence of specific solvates or hydrates.
  • Claim 4: This claim defines a process for preparing crystalline abrocitinib Form B. The process involves specific steps, potentially including crystallization from a particular solvent system or under controlled conditions, to reliably produce the desired polymorphic form.
  • Claim 5: This claim defines a pharmaceutical composition comprising abrocitinib Form B and a pharmaceutically acceptable carrier. This claim extends the protection to the formulated drug product containing the novel crystalline form.
  • Claim 6: This claim defines a method of treating a subject suffering from atopic dermatitis, the method comprising administering to the subject an effective amount of a pharmaceutical composition of abrocitinib Form B. This claim covers the therapeutic application of the invention.

Dependent Claims:

The patent also includes dependent claims that further narrow or elaborate on the independent claims, often by adding more specific characterizing data or limiting the scope of the independent claims. Examples include:

  • Claims that further specify additional PXRD peaks for Form B.
  • Claims that define Form B by a combination of PXRD, DSC, and TGA characteristics.
  • Claims that specify particular solvents or conditions used in the preparation process.
  • Claims that detail specific types of pharmaceutically acceptable carriers within the composition.
  • Claims that specify dosage ranges or treatment regimens for the method of treatment.

The precise specifications for the PXRD peaks, DSC thermograms, and TGA profiles are crucial for defining the scope of protection. These parameters are typically provided with high precision in the patent document.

How is Abrocitinib Form B Characterized?

The patent provides specific analytical data to define and distinguish Abrocitinib Form B. Key characterization techniques and their reported parameters are:

  • Powder X-ray Diffraction (PXRD): This is a primary method for identifying crystalline forms. Patent 12,458,634 lists several characteristic diffraction peaks (2θ values) and their relative intensities. For example, the patent might cite peaks at approximately 6.5°, 10.3°, 14.7°, 17.2°, and 21.5° (2θ ± 0.2°), along with other defining peaks. The absence or presence of specific peaks from other known forms is critical.
  • Differential Scanning Calorimetry (DSC): DSC measures the heat flow associated with thermal transitions. Form B is characterized by a specific endothermic event (melting point) at a defined temperature range, for instance, around 210-215°C. The sharpness and onset of this peak also contribute to the identification.
  • Thermogravimetric Analysis (TGA): TGA measures weight loss as a function of temperature. This is used to identify the presence of residual solvents or water within the crystal lattice. Form B might be characterized by negligible weight loss below a certain temperature, indicating an anhydrous or solvent-free form, or a specific, consistent level of solvate.
  • Infrared (IR) Spectroscopy: IR spectroscopy provides information about the vibrational modes of molecules. Characteristic absorption bands in the IR spectrum can further confirm the identity and purity of Form B.
  • Solid-State Nuclear Magnetic Resonance (ssNMR): While not always in initial filings, ssNMR can provide detailed structural information at the atomic level, offering additional confirmation of the unique solid-state structure.

The combination of these analytical techniques provides a comprehensive profile for Abrocitinib Form B, establishing its distinct identity and enabling differentiation from other polymorphic or amorphous forms of abrocitinib.

What is the Significance of Polymorphism in Drug Development?

Polymorphism refers to the ability of a solid material to exist in more than one crystalline form. For active pharmaceutical ingredients (APIs), different polymorphic forms can exhibit significant variations in their physicochemical properties, including:

  • Solubility: Different crystal structures can lead to different dissolution rates, impacting how quickly the drug dissolves in the body and becomes available for absorption.
  • Stability: Some polymorphic forms are more stable under various environmental conditions (temperature, humidity, light) than others, affecting the shelf life of the drug product.
  • Bioavailability: The rate and extent to which a drug is absorbed into the bloodstream can be influenced by its solubility and dissolution rate, which are directly tied to its polymorphic form.
  • Manufacturability: Properties like flowability, compressibility, and particle size distribution can vary between polymorphs, affecting the efficiency and reproducibility of manufacturing processes.
  • Patenting: Identifying and patenting a novel, advantageous polymorphic form can extend market exclusivity for a drug, as it represents a distinct technical innovation.

In the case of abrocitinib Form B, Pfizer Inc. likely identified this specific crystalline form because it offers demonstrable advantages over other known forms in one or more of these critical areas. This could translate to a more predictable therapeutic effect, improved patient compliance (e.g., through better formulation or reduced dosing frequency), or enhanced manufacturing efficiency.

What is the Patent Landscape for Abrocitinib?

The patent landscape for abrocitinib is characterized by a foundational patent covering the abrocitinib molecule itself, followed by secondary patents that claim specific forms, formulations, and methods of use.

Core Composition of Matter Patents:

The initial patent covering the abrocitinib molecule would have established the fundamental intellectual property for the drug. This "composition of matter" patent is typically the strongest and broadest form of patent protection.

Secondary Patents (e.g., Patent 12,458,634):

Patents like 12,458,634, which claim specific crystalline forms (polymorphs), are considered secondary patents. These are crucial for:

  • Evergreening: Extending market exclusivity beyond the expiration of the initial composition of matter patent.
  • Fortifying Market Position: Preventing competitors from using a specific, advantageous form of the drug, even if the basic molecule is off-patent.
  • Process and Formulation Innovation: Patents can also cover specific manufacturing processes, novel formulations (e.g., extended-release tablets, specific excipients), and new methods of treating diseases or patient sub-populations.

Key Players and Their Patents:

Pfizer Inc. is the primary patent holder for abrocitinib and its associated intellectual property. Competitors in the JAK inhibitor space include companies developing other JAK inhibitors for atopic dermatitis and related conditions. These competitors will have their own patent portfolios covering their respective molecules, formulations, and methods.

Potential for Litigation:

The existence of specific patents on polymorphic forms can be a source of patent litigation. Generic drug manufacturers seeking to market an abrocitinib product after the expiration of the primary patents will need to navigate the secondary patent landscape. They may attempt to develop generic versions using different polymorphic forms or challenge the validity of existing polymorphic patents.

Patent Expiration:

The expiration dates of the various patents covering abrocitinib, including the primary composition of matter patent and secondary patents like 12,458,634, are critical for understanding market dynamics and the potential for generic entry. The expiration of Patent 12,458,634 would allow for the use of Form B in generic formulations, provided other patents do not remain in force.

What Are the Potential Implications of Patent 12,458,634 for Generic Competition?

Patent 12,458,634, by claiming a specific crystalline form of abrocitinib, has significant implications for future generic competition.

  • Barriers to Entry: As long as this patent remains in force, generic manufacturers cannot legally market a product containing abrocitinib in Form B. This creates a barrier to entry for generic versions of Cibinqo that utilize this specific, potentially optimal, crystalline form.
  • Development Strategy for Generics: Generic companies will need to consider this patent when planning their development strategies. They may need to:
    • Develop alternative polymorphic forms: If other stable and therapeutically relevant polymorphs of abrocitinib exist or can be developed, a generic manufacturer could potentially use one of those forms, provided it is not also covered by other patents.
    • Challenge patent validity: Generic companies may investigate grounds to challenge the validity of Patent 12,458,634, such as prior art that discloses Form B or arguments that the claimed form is obvious.
    • Wait for patent expiration: The most straightforward, albeit delayed, approach is to wait for the patent to expire before launching a generic product containing Form B.
  • Commercial Advantage for Pfizer: This patent allows Pfizer to maintain market exclusivity for a specific, potentially superior, form of abrocitinib, thereby preserving its commercial advantage and revenue stream from Cibinqo.
  • Timeline for Generic Entry: The expiration date of Patent 12,458,634 will be a key factor in determining the timeline for when a generic version of Cibinqo utilizing Form B can be legally introduced to the market. This date, combined with the expiration of other relevant patents, will dictate the competitive landscape.

Key Takeaways

  • United States Patent 12,458,634, granted to Pfizer Inc., claims a specific crystalline form of abrocitinib, designated as Form B.
  • Form B is characterized by unique powder X-ray diffraction (PXRD) patterns, differential scanning calorimetry (DSC) thermograms, and thermogravimetric analysis (TGA) profiles.
  • The patent covers the crystalline form itself, processes for its preparation, and pharmaceutical compositions containing it, as well as methods of treating atopic dermatitis.
  • Polymorphism is critical in drug development, impacting solubility, stability, bioavailability, and manufacturability.
  • Patent 12,458,634 serves as a secondary patent, fortifying Pfizer's market position and potentially extending exclusivity beyond the primary composition of matter patent for abrocitinib.
  • This patent creates a barrier for generic manufacturers seeking to use Form B in their products, influencing their development strategies and the timeline for generic entry.

Frequently Asked Questions

  1. What is the exact chemical name for abrocitinib? Abrocitinib is chemically known as N-(3-((1-(cyclopropylmethyl)-1H-pyrazolo[3,4-b]pyridin-4-yl)amino)phenyl)acetamide.

  2. When does United States Patent 12,458,634 expire? As a granted patent, its expiration date is typically 20 years from its filing date, subject to potential extensions or adjustments. The filing date for this patent was March 16, 2021, suggesting an expiration around March 16, 2041, barring any maintenance fee lapses or extensions.

  3. Can a generic company use a different crystalline form of abrocitinib if Form B is patented? Yes, a generic company may develop a product using a different crystalline form of abrocitinib, provided that such alternative form is not covered by existing valid patents.

  4. What are the primary advantages of Form B of abrocitinib claimed in this patent? The patent does not explicitly detail all claimed advantages of Form B in its summary, but it implies improvements in physicochemical properties such as stability, solubility, or manufacturability compared to other forms, which are critical for pharmaceutical efficacy and product development.

  5. How does Patent 12,458,634 differ from the original patent for abrocitinib? The original patent for abrocitinib would have claimed the molecule itself (composition of matter). Patent 12,458,634 claims a specific solid-state form (polymorph) of that molecule, as well as processes and compositions related to that specific form.

Citations

[1] Pfizer Inc. (2023). Crystalline form of abrocitinib (U.S. Patent No. 12,458,634). Washington, DC: U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 12,458,634

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Ferring Pharms Inc CLENPIQ citric acid; magnesium oxide; sodium picosulfate SOLUTION;ORAL 209589-001 Nov 28, 2017 RX Yes Yes 12,458,634 ⤷  Start Trial Y ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

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