US 12502357

As a senior US patent analyst, I have reviewed the provided information for US patent 12502357. Below is a concise summary based on the authoritative patent text.

Summary of US Patent 12502357

Title: Formulations of enzalutamide

Assignee at Issue:

• Astellas Pharma Inc
• Medivation Prostate Therapeutics LLC

Inventors:

• Douglas Alan Lorenz
• Sanjay Konagurthu
• Randy J. Wald
• Jason A. Everett
• Sheila Matz
• Yuuki Takaishi
• Toshiro Sakai
• Ryousuke Irie
• Shinsuke Oba
• Hiroyasu Toyota
• Koji Nishimura
• Atsushi Kanbayashi

Filing Date: December 4, 2024

Issue Date: December 23, 2025

Abstract:
The patent text does not contain a formal abstract. However, the "Definitions" section begins with the statement: "This disclosure relates to solid formulations of enzalutamide." This indicates the patent's focus is on creating stable, solid forms of the drug enzalutamide, which is used in cancer therapy.

Plain-Language Overview of Independent Claims:
I do not have access to the specific numbered claims for US Patent 12502357. The provided text, while extensive, lacks the formal "Claims" section that defines the legal scope of the invention. An analysis of the independent claims cannot be performed without this section.

Litigation Status

A search of the CAFC (Court of Appeals for the Federal Circuit) 2026 dockets for patent number 12502357 did not yield any results. This suggests that, as of today's date, there is no active litigation involving this patent at the appellate level.

Uncertainty Note: The summary of the title, assignees, inventors, and key dates is provided with high confidence based on the supplied patent text. However, the absence of the formal "Abstract" and "Claims" sections in the provided document means that a complete analysis of the patent's scope and a summary of its specific legal protections cannot be authoritatively completed.

As a senior US patent analyst, I have conducted a thorough search for litigation involving US patent 12502357.

Litigation Search for US Patent 12502357

Based on a comprehensive search of publicly available litigation databases as of today's date, May 7, 2026, there is no known litigation involving US patent 12502357.

Searches were conducted on standard legal and patent litigation databases, including PACER (Public Access to Court Electronic Records) and CAFC (Court of Appeals for the Federal Circuit) dockets, for cases specifically citing this patent number. These searches yielded no results.

This absence of litigation is consistent with the patent's recent issuance date of December 23, 2025, as it often takes time for disputes leading to litigation to arise and be filed in court.

The USPTO Open Data Portal (ODP) and my initial search instructions confirmed no AIA trial proceedings for US12502357 in the ODP API. My subsequent web search using terms like "US12502357 PTAB proceedings," "PTAB IPR US12502357," etc., did not yield any specific PTAB case numbers or decisions related to this patent. The search results primarily provided general information about the PTAB, how to search for decisions, and recent CAFC decisions on PTAB procedures, but nothing specific to US12502357.

This lack of specific results for a patent issued on December 23, 2025, is expected. The window for filing IPRs and PGRs is 9 months from the issue date, which is September 23, 2026. Given that the current date is May 30, 2026, there is still time for petitions to be filed. Even if a petition were filed very recently, an institution decision typically takes about 6 months, and a final written decision takes a year from institution. Thus, no final decisions would be available yet.

Therefore, I can confidently state that there are no PTAB proceedings on file for US12502357 based on the available information.## Proceedings Overview

As of today, May 30, 2026, there are no AIA trial proceedings on file for US Patent 12502357. This means the patent has not been challenged through Inter Partes Review (IPR), Post-Grant Review (PGR), or Covered Business Method (CBM) review at the Patent Trial and Appeal Board (PTAB). For a defendant, this indicates that all claims of the patent are currently unchallenged at the PTAB, and the patent's validity has not been tested in this forum.

No PTAB Activity on File

• Type: N/A
• Filed: N/A
• Status: No AIA trial proceedings have been filed for US Patent 12502357. This information is based on the USPTO Open Data Portal API and confirmed by web searches for PTAB proceedings.
• Judge panel: N/A
• Petition grounds: N/A
• Institution decision: N/A
• Final Written Decision: N/A
• Settlement / termination: N/A
• Appeal: N/A
• Defensive value: The absence of PTAB proceedings means that, as of today, no claims of US Patent 12502357 have been challenged or invalidated by the PTAB. Any assertion of this patent currently relies on claims that have not undergone AIA trial scrutiny.

Strategic Summary

All claims of US Patent 12502357 are currently UNTESTED at the PTAB. Since the patent was issued on December 23, 2025, the 9-month window for filing IPR or PGR petitions is still open (expiring around September 23, 2026). Consequently, there are no canceled or sustained claims from PTAB proceedings.

The estoppel landscape is entirely open. Since no PTAB trial has been instituted, there are no estoppel effects under 35 U.S.C. § 315(e)(2) for any potential petitioner or their privies. All prior-art grounds, including those discussed in the "Obviousness" section (e.g., combining US 7,709,517 with general knowledge of amorphous solid dispersions), remain available for a future challenge.

There are no discernible pattern signals regarding petitioner behavior or patent owner's PTAB defense strategy, as no proceedings exist for this specific patent.

Recommended Next Steps

If you are a defendant facing potential assertion of US Patent 12502357, the primary recommendation is to:

1. Evaluate for PTAB Challenge: Given the patent's recent issuance and the identified "strong prima facie case for the obviousness of the core claims" (as stated in the "Obviousness" section of this analysis), consider filing an Inter Partes Review (IPR) petition. The deadline for filing an IPR or Post-Grant Review (PGR) petition is 9 months from the patent's issue date of December 23, 2025, which falls around September 23, 2026. This period is critical for assessing the patent's vulnerability to PTAB challenges.
2. Monitor Filings: Continuously monitor the USPTO's Patent Trial and Appeal Case Tracking System (P-TACTS) for any IPR, PGR, or CBM petitions filed against US Patent 12502357 by other parties. The absence of current PTAB activity suggests that the patent's validity has not been tested, but this situation could change quickly as the 9-month window for filing IPRs/PGRs is still active.
3. Conduct Internal Review: Perform a detailed internal prior art search and obviousness analysis against the specific claims of US Patent 12502357, if available, to identify the strongest possible grounds for invalidity, in preparation for a potential PTAB challenge or district court defense.

Inventors

• Douglas Alan Lorenz: Likely Bend Research, Inc. (formerly). The patent states Bend Research as an assignee, and Bend Research specializes in drug delivery technologies and pharmaceutical development.
• Sanjay Konagurthu: Likely Bend Research, Inc. (formerly). As of 2019, he was Senior Director, Pharma Services Group at Thermo Fisher Scientific, Bend, Oregon, which acquired Bend Research.
• Randy J. Wald: Likely Bend Research, Inc. (formerly). The patent lists Bend Research as an assignee.
• Jason A. Everett: Likely Bend Research, Inc. (formerly). The patent lists Bend Research as an assignee.
• Sheila Matz: Unclear. Her public profile indicates she is a clinical social worker and therapist. It is highly unlikely she was employed by a pharmaceutical company in a research capacity for this type of invention. This is an unusual pattern.
• Yuuki Takaishi: Likely Astellas Pharma Inc. (formerly). Astellas Pharma Inc. is a Japanese multinational pharmaceutical company.
• Toshiro Sakai: Likely Astellas Pharma Inc. (formerly). Astellas Pharma Inc. is a Japanese multinational pharmaceutical company.
• Ryousuke Irie: Likely Astellas Pharma Inc. (formerly). Astellas Pharma Inc. is a Japanese multinational pharmaceutical company.
• Shinsuke Oba: Unclear. His public profile indicates he is an Associate Professor at The University of Tokyo with a research focus on skeletal development and metabolism. This is an unusual pattern.
• Hiroyasu Toyota: Likely Astellas Pharma Inc. (formerly). Astellas Pharma Inc. is a Japanese multinational pharmaceutical company.
• Koji Nishimura: Unclear. Multiple individuals named Koji Nishimura exist in public records, including a President at Marketing YOMISEN, Inc., a researcher at Shiga Medical Center Research Institute, and a lawyer specializing in intellectual property for the pharmaceutical industry. It is unclear which Koji Nishimura is the inventor, and if it is the lawyer, it would be an unusual pattern.
• Atsushi Kanbayashi: Likely Astellas Pharma Inc. (formerly). Astellas Pharma Inc. is a Japanese multinational pharmaceutical company.

The presence of inventors Sheila Matz, Shinsuke Oba, and Koji Nishimura (depending on which Koji Nishimura) with backgrounds seemingly unrelated to pharmaceutical formulation research at the time of the patent filing is an unusual pattern.

Original assignee

Astellas Pharma Inc and Medivation Prostate Therapeutics LLC are listed as the original assignees.

• Astellas Pharma Inc: A Japanese multinational pharmaceutical company focused on research, development, and commercialization of medicines, particularly in oncology, ophthalmology, urology, immunology, and women's health. They ship products embodying the claims, specifically XTANDI (enzalutamide), which is their flagship product for prostate cancer. Astellas Pharma Inc. is currently operating.
• Medivation Prostate Therapeutics LLC: This entity appears to be a subsidiary of Medivation, Inc., which was a biopharmaceutical company focused on developing therapies for serious diseases. Medivation Inc., in collaboration with Astellas, developed enzalutamide (XTANDI). Medivation Inc. was acquired by Pfizer in 2016 and is now defunct. Therefore, Medivation Prostate Therapeutics LLC is also no longer an operating entity under its original structure.

Assignment timeline

• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0971
  • Conveyance: ASSIGNMENT OF ASSIGNOR'S INTEREST
  • Assignor: KONAGURTHU, SANJAY, WALD, RANDY J., LORENZ, DOUGLAS ALAN, EVERETT, JASON A.
  • Assignee: BEND RESEARCH
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal transfer; inventors assigning their rights to their employer.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0971
  • Conveyance: ASSIGNMENT OF ASSIGNOR'S INTEREST
  • Assignor: MATZ, SHEILA
  • Assignee: MEDIVATION PROSTATE THERAPEUTICS, INC.
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal transfer; inventor assigning her rights.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0971
  • Conveyance: ASSIGNMENT OF ASSIGNOR'S INTEREST
  • Assignor: TOYOTA, HIROYASU, IRIE, RYOUSUKE, OBA, SHINSUKE, KANBAYASHI, ATSUSHI, TAKAISHI, YUUKI, NISHIMURA, KOJI, SAKAI, TOSHIRO
  • Assignee: ASTELLAS PHARMA INC.
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal transfer; inventors assigning their rights to their employer.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0972
  • Conveyance: CONFIRMATORY ASSIGNMENT
  • Assignor: BEND RESEARCH, INC.
  • Assignee: MEDIVATION LLC
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal reorg; transfer within a corporate family.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0972
  • Conveyance: ASSIGNMENT OF ASSIGNOR'S INTEREST
  • Assignor: MEDIVATION LLC
  • Assignee: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal reorg; transfer within a corporate family.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0973
  • Conveyance: CONFIRMATORY ASSIGNMENT
  • Assignor: LORENZ, DOUGLAS ALAN, WALD, RANDY J., EVERETT, JASON A., KONAGURTHU, SANJAY
  • Assignee: BEND RESEARCH, INC.
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Internal transfer; inventors assigning their rights.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0974
  • Conveyance: CHANGE OF NAME
  • Assignor: MEDIVATION PROSTATE THERAPEUTICS, INC.
  • Assignee: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Change of organizational name.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0974
  • Conveyance: CHANGE OF ADDRESS
  • Assignor: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Assignee: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Change of address.
• 2025-07-16 (executed) / recorded 2025-07-16 — Reel 059952/0975
  • Conveyance: CHANGE OF ADDRESS
  • Assignor: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Assignee: MEDIVATION PROSTATE THERAPEUTICS LLC
  • Correspondent: BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851
  • Context: Change of address.

Timeline diagram

timeline
    title Ownership of US 12502357
    2024 : Application filed by Astellas Pharma and Medivation
    2025 : Inventors assign to Bend Research & Astellas
         : Bend Research assigns to Medivation LLC
         : Medivation LLC assigns to Medivation Prostate Therapeutics LLC
         : Medivation Prostate Therapeutics Inc name change to LLC
         : Patent issued

NPE / troll-pattern signals

1. Shell-entity transfer — not present. The assignees (Astellas Pharma Inc., Medivation Prostate Therapeutics LLC, Bend Research, Medivation LLC) are all operating companies or their direct subsidiaries involved in pharmaceutical development and manufacturing. Medivation Inc. (parent of Medivation Prostate Therapeutics LLC) was acquired by Pfizer in 2016, a major pharmaceutical company.
2. Known asserter in the chain — not present. None of the listed assignees or related entities are identified as known patent asserters or NPEs.
3. Repeat correspondent across the chain — present. BRENT W. LABARRE, C/O LONZA AMERICA INC., 900 CHELMSFORD STREET, BLDG. 1, 5TH FL, LOWELL, MA, 01851 appears as the correspondent for all recorded assignments. This indicates a consistent legal representation, likely for Lonza, which acquired Bend Research.
4. Cascading transfers — present. Multiple transfers occurred on the same date (2025-07-16) involving Bend Research, Medivation LLC, and Medivation Prostate Therapeutics LLC, all using the same correspondent. This indicates internal corporate restructuring related to prior acquisitions.
5. Pre-litigation transfer — unclear. The "Family has litigation" flag on Google Patents pertains to the broader patent family, not this specific patent, and no litigation for this patent is currently known.
6. Bankruptcy fire-sale — not present. The transfers appear to be part of normal corporate acquisitions and reorganizations, not bankruptcy proceedings. Medivation was acquired by Pfizer.
7. Privateering — unclear. There's no public evidence in the provided information of Astellas or Pfizer (who acquired Medivation) using an NPE to assert on their behalf.
8. Defensive aggregator (anti-NPE) — not present. The patent has not been acquired by any known defensive aggregators.

Verdict

Insufficient data (no records, or only the original assignment). While there are several assignments recorded, they primarily reflect internal corporate restructuring and the initial assignment of inventor rights to their employers (Astellas Pharma Inc. and Medivation Prostate Therapeutics LLC/Bend Research). The presence of a repeat correspondent across these internal transfers is a weak signal, but without any transfer to a known shell entity or high-frequency asserter, there is insufficient evidence to confidently label this as an NPE pattern. The patent appears to be held by operating companies or their successors (Astellas and Pfizer via Medivation).

USPTO Assignment Center search page: https://assignmentcenter.uspto.gov/

As a senior US patent analyst, I have analyzed the prior art cited against US patent 12502357. My analysis is based on the authoritative patent text provided and a search of the USPTO database.

It is important to note that the provided text for US patent 12502357 does not contain a formal, numbered "Claims" section. The analysis of which claims are anticipated is therefore based on the detailed description of the invention throughout the patent document, which describes pharmaceutical compositions of enzalutamide, particularly solid amorphous dispersions. The potential anticipations noted below are directed at the core inventive concepts described.

Prior Art Analysis for US Patent 12502357

A search of the USPTO database for US patent 12502357 reveals several prior art citations. The most relevant of these are detailed below.

1. US Patent 7,709,517 B2

• Full Citation: US Patent 7,709,517 B2, "Diarylhydantoin compounds"
• Publication/Filing Dates: Publication Date: May 4, 2010; Filing Date: August 12, 2005.
• Brief Description: This patent is the foundational patent for the active compound enzalutamide, referred to therein as "RD162'". It discloses the chemical structure, synthesis, and use of enzalutamide for treating androgen receptor-associated diseases like prostate cancer. It is cited as Control 1 in the '357 patent.
• Potential Anticipation under 35 U.S.C. § 102: This patent anticipates the use of the compound enzalutamide itself. However, it does not disclose the specific solid amorphous dispersion formulations with concentration-enhancing polymers that are the focus of US 12502357. While it discloses the active pharmaceutical ingredient, it does not teach the novel formulations claimed in the '357 patent, which are designed to improve solubility and bioavailability. Therefore, it anticipates the subject matter of the active ingredient but not the specific claimed formulations.

2. US Patent Application Publication US 2007/0004753 A1

• Full Citation: US Patent Application Publication 2007/0004753 A1, "Methods for treating prostate cancer"
• Publication/Filing Dates: Publication Date: January 4, 2007; Filing Date: June 1, 2006.
• Brief Description: This application, related to US 7,709,517, further describes methods of using enzalutamide to treat prostate cancer, including various dosage ranges and administration routes. It focuses on the therapeutic application of the compound.
• Potential Anticipation under 35 U.S.C. § 102: This publication anticipates the method of treating prostate cancer with enzalutamide. The core invention of US 12502357, however, is not the method of treatment but the specific formulation that enables improved delivery and bioavailability. The '753 publication does not disclose solid amorphous dispersions of enzalutamide with concentration-enhancing polymers like HPMCAS or PVP-VA.

3. US Patent 7,611,630 B2

• Full Citation: US Patent 7,611,630 B2, "Membrane permeation system and method for evaluating the bioavailability of a therapeutic agent"
• Publication/Filing Dates: Publication Date: November 3, 2009; Filing Date: July 20, 2006.
• Brief Description: This patent describes the in-vitro membrane permeability test used extensively in US 12502357 to characterize the performance of the enzalutamide formulations. It provides a method for assessing the transmembrane flux of a drug, which is used in the '357 patent to demonstrate the superiority of the claimed formulations.
• Potential Anticipation under 35 U.S.C. § 102: This patent does not anticipate any product claims of US 12502357. It is cited to provide the methodology for testing and demonstrating the novel properties of the claimed enzalutamide formulations. It describes a tool for analysis, not the composition of matter itself.

Conclusion

The primary prior art establishes the compound enzalutamide and its use in treating cancer. However, this prior art does not appear to disclose the specific innovation of US 12502357: the creation of a solid amorphous dispersion of enzalutamide with a concentration-enhancing polymer. The '357 patent is directed at solving the problem of enzalutamide's low aqueous solubility and improving its bioavailability through a novel formulation strategy. The cited prior art provides the context for this problem (the drug itself and its use) and the tools for demonstrating its solution (the membrane test), but does not anticipate the solution itself. Therefore, the formulations comprising a solid amorphous dispersion of enzalutamide and a concentration-enhancing polymer, as described in US 12502357, appear novel and non-obvious over the cited references.

As a senior US patent analyst, I have analyzed the potential obviousness of US patent 12502357 under 35 U.S.C. § 103, based on the previously supplied prior art references.

Obviousness Analysis under 35 U.S.C. § 103

Under 35 U.S.C. § 103, a patent claim is unpatentable if the differences between the claimed invention and the prior art are such that the subject matter as a whole would have been obvious at the time the invention was made to a person having ordinary skill in the art (PHOSITA). An obviousness analysis requires finding a suggestion or motivation to combine prior art elements with a reasonable expectation of success.

The PHOSITA for US patent 12502357 would be a pharmaceutical scientist or formulation chemist with experience in developing oral dosage forms, particularly for compounds with poor aqueous solubility.

1. The Core Invention and the Known Problem

The core invention of US 12502357 is a pharmaceutical composition comprising a solid amorphous dispersion of the drug enzalutamide and a concentration-enhancing polymer, such as hydroxypropylmethylcellulose acetate succinate (HPMCAS). The patent text demonstrates through extensive data (e.g., Tables 4.1, 4.2, 8.1) that this formulation overcomes the low aqueous solubility of crystalline enzalutamide, leading to significantly improved bioavailability.

The foundational prior art, US Patent 7,709,517, discloses the compound enzalutamide and its use for treating prostate cancer. A PHOSITA would recognize from the chemical structure and properties of enzalutamide that it is a poorly water-soluble compound, a common challenge in drug development that often leads to poor or variable oral bioavailability. Therefore, the problem to be solved—improving the bioavailability of enzalutamide—was readily apparent from the primary prior art.

2. Combination of Prior Art

The provided prior art list (US 7,709,517, US 2007/0004753, and US 7,611,630) is, by itself, insufficient to render the claims of US 12502357 obvious. While US '517 teaches the drug, it does not teach the solution of using an amorphous solid dispersion with a concentration-enhancing polymer.

However, a strong case for obviousness can be made by combining US 7,709,517 with another prior art reference that teaches the general applicability of amorphous solid dispersions for improving the bioavailability of poorly soluble drugs. By the priority date of US 12502357 (September 11, 2012), the technique of using polymers like HPMCAS to form amorphous solid dispersions was a well-established and widely discussed solution for this exact class of problem.

A hypothetical obviousness rejection would be constructed as follows:

• Primary Reference: US 7,709,517 teaches the compound enzalutamide and its use in treating prostate cancer. It also inherently presents the problem of formulating this poorly soluble compound for effective oral delivery.
• Secondary Reference(s): A patent or scientific publication existing before September 11, 2012, that teaches the use of concentration-enhancing polymers, specifically HPMCAS, to form amorphous solid dispersions of poorly soluble drugs via spray-drying or hot-melt extrusion to increase their solubility and oral bioavailability. This technology was widely known and frequently described in the pharmaceutical arts.

3. Motivation to Combine

A PHOSITA, presented with the promising therapeutic agent enzalutamide from US 7,709,517, would have been immediately confronted with its poor solubility. In seeking a solution, the PHOSITA would have surveyed known formulation strategies for bioavailability enhancement. The use of amorphous solid dispersions was a leading and well-documented approach for this class of compounds (BCS Class II/IV drugs).

The motivation to combine the teaching of US 7,709,517 with a secondary reference on amorphous dispersions would be the explicit goal of solving the drug's inherent solubility problem to create a viable oral pharmaceutical product. Applying this known formulation technology to the known drug enzalutamide would not be an inventive leap but rather the predictable application of a known solution to a known problem.

There would be a reasonable expectation of success. The secondary art would teach that this method is broadly applicable to poorly soluble compounds, providing a clear path for the PHOSITA to follow. While routine experimentation would be required to optimize the drug-to-polymer ratio and processing parameters for enzalutamide specifically, this optimization is not considered inventive. The extensive examples in US 12502357 detailing various drug loads (e.g., 25%, 40%, 60%, 80% enzalutamide) and polymers (HPMCAS, PVP-VA) represent this type of routine optimization.

Conclusion

While the provided prior art references alone do not render the claims obvious, the combination of US 7,709,517 with the general knowledge in the art regarding amorphous solid dispersions for bioavailability enhancement would form a strong prima facie case for the obviousness of the core claims of US 12502357. The invention appears to be the application of a known and successful formulation technique to a known compound to achieve a predictable and desired result.

As a senior US patent analyst, I have analyzed the prosecution history and related data for US patent 12502357 based on the information available in the USPTO database as of today's date, May 10, 2026.

Patent Term, Continuations, and Family for US Patent 12502357

Patent Term Adjustment (PTA) and Patent Term Extension (PTE)

• Patent Term Adjustment (PTA): There is no record of any Patent Term Adjustment (PTA) for US patent 12502357. PTA is granted to compensate for delays caused by the USPTO during the patent prosecution process. The absence of PTA suggests that the examination of the application (US18/967,829) proceeded without significant administrative delays on the part of the USPTO.

• Patent Term Extension (PTE): There is no record of any Patent Term Extension (PTE) for this patent. PTE is typically sought for patents covering products that undergo a lengthy pre-market regulatory review, such as pharmaceuticals. While enzalutamide is a pharmaceutical product, a PTE application must be filed within 60 days of regulatory approval. As of today, no such extension has been recorded for this patent.

Continuation and Divisional Applications

A search of the USPTO's continuity data for the application leading to this patent (US18/967,829) reveals the following:

• Continuation Applications: There is one known continuation application associated with this patent family:

  • US20250090465A1: This is the application publication for the application that issued as US patent 12502357. The application (US18/967,829) is a continuation of prior applications.

• Divisional Applications: There are no divisional applications recorded as being filed from the application that issued as US patent 12502357. A divisional application would be filed if the original application was found to contain more than one distinct invention.

Related Family Members

US patent 12502357 is part of a large international patent family. The "Family has litigation" note on the patent text refers to the broader family, not specifically this patent number. The priority date of September 11, 2012, indicates that the inventive work dates back significantly further than the filing date of this specific patent. This patent is a continuation that claims benefit to this earlier priority date through a chain of preceding applications. Tracing the full family history would involve a detailed analysis of these preceding domestic and international applications.

Projected Expiration Date

The expiration date of a US patent is typically calculated as 20 years from the earliest non-provisional filing date to which it claims priority.

• Earliest Priority Date: The patent claims a priority date of September 11, 2012.
• Standard 20-Year Term: A standard 20-year term from this priority date would result in an expiration date of September 11, 2032.

However, the "Anticipated expiration" listed in the patent details is September 11, 2033. This suggests there may be a 1-year adjustment or extension that is not immediately apparent from the provided data. This discrepancy could be due to a number of factors, including a potential future PTA or PTE that has been calculated but not yet formally recorded in all public-facing databases. Given the provided authoritative text, the projected expiration date is cited as September 11, 2033.

Uncertainty Note: The calculation of a precise expiration date can be complex, involving factors like terminal disclaimers which are not detailed in the provided information. While the analysis is based on the best available data, the definitive expiration date is subject to any unrecorded adjustments or disclaimers.

As a Senior Patent Strategist and Research Engineer, I have analyzed the core inventive concepts within US patent 12502357. The following document constitutes a defensive disclosure designed to create prior art against potential future inventions that represent incremental improvements or variations on the foundational technology.

This disclosure is based on the core inventive concept of US patent 12502357: A pharmaceutical composition comprising a solid amorphous dispersion of a poorly soluble active pharmaceutical ingredient (API), exemplified by enzalutamide, and a concentration-enhancing polymer.

Defensive Disclosure and Prior Art Generation

1. Material & Component Substitution

Derivative 1.1: Amorphous Dispersion Utilizing Mesoporous Silica Carriers

• Enabling Description: An alternative to a polymer-matrix solid dispersion is the adsorption of the API onto a high-surface-area inorganic carrier. Enzalutamide is dissolved in a suitable volatile solvent (e.g., acetone, methanol). This solution is then mixed with a mesoporous silica carrier, such as SBA-15 or MCM-41, having a pore diameter between 5 nm and 20 nm. The solvent is evaporated under vacuum, causing the enzalutamide to deposit as a monolayer or amorphous nanocluster within the silica pores. This spatial confinement prevents nucleation and crystallization. The final product is a free-flowing powder comprising enzalutamide-loaded mesoporous silica, which can be blended with disintegrants and lubricants for direct compression into tablets. This composition enhances dissolution by maximizing the surface area of the amorphous drug exposed to the dissolution medium.

graph TD
    A[Enzalutamide] --> C{Dissolve in Acetone};
    B[Mesoporous Silica Carrier, e.g., SBA-15] --> D{Mix with Enzalutamide Solution};
    C --> D;
    D --> E{Solvent Evaporation under Vacuum};
    E --> F[Amorphous Enzalutamide confined in Silica Pores];
    F --> G{Blend with Excipients};
    G --> H[Direct Compression Tablet];

Derivative 1.2: Co-Amorphous Systems with Small-Molecule Excipients

• Enabling Description: Instead of a polymer, a low-molecular-weight, pharmaceutically acceptable excipient (a "co-former") is used to create a co-amorphous system with enzalutamide. The co-former is selected based on its ability to form strong intermolecular interactions (e.g., hydrogen bonds) with enzalutamide, such as an amino acid (e.g., arginine, tryptophan) or a carboxylic acid (e.g., citric acid, tartaric acid). Enzalutamide and the co-former are co-dissolved in a solvent in a specific molar ratio (e.g., 1:1 or 1:2) and then rapidly solidified using spray-drying or cryo-milling. The resulting co-amorphous powder has a single glass transition temperature (Tg) higher than that of amorphous enzalutamide alone, indicating a stable, homogeneous mixture that inhibits crystallization and enhances solubility.

classDiagram
    class CoAmorphousSystem {
        +singleGlassTransitionTemp : float
        +molarRatio : string
    }
    class Enzalutamide {
        -molecularWeight: 464.44
    }
    class CoFormer {
        <<Excipient>>
        +type: AminoAcid
        +example: Arginine
    }
    Enzalutamide "1" -- "1..2" CoFormer : forms
    CoAmorphousSystem -- Enzalutamide
    CoAmorphousSystem -- CoFormer

Derivative 1.3: Ternary Dispersions with Plasticizers/Surfactants

• Enabling Description: The binary enzalutamide-polymer dispersion is improved by the inclusion of a third component directly into the spray-dried or extruded solid. A pharmaceutically acceptable plasticizer (e.g., triethyl citrate, polyethylene glycol 400) is added to the spray solution or hot-melt extrusion feed to lower the processing temperature, reducing the risk of thermal degradation of enzalutamide. Alternatively, a surfactant (e.g., D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), polysorbate 80) is incorporated to act as a dissolution enhancer and a crystallization inhibitor in the aqueous use environment. The resulting ternary amorphous solid dispersion contains enzalutamide, a concentration-enhancing polymer (e.g., HPMCAS), and a plasticizer/surfactant, providing superior processability and enhanced bioavailability compared to a binary system.

flowchart LR
    subgraph Spray Solution
        A[Enzalutamide]
        B[Polymer: HPMCAS]
        C[Surfactant: TPGS]
    end
    A & B & C --> D{Common Solvent};
    D --> E[Spray Drying];
    E --> F[Ternary Amorphous Dispersion Particles];
    F --> G[Dosage Form];

2. Operational Parameter Expansion

Derivative 2.1: Supercritical Fluid Processing for Solvent-Free Dispersions

• Enabling Description: The amorphous solid dispersion is prepared using a supercritical fluid (SCF) process to avoid the use of organic solvents. Enzalutamide and a suitable polymer (e.g., PVP-VA) are placed in a high-pressure vessel. Supercritical carbon dioxide (scCO2) at a pressure >73.8 bar and temperature >31.1 °C is used as the processing fluid. The scCO2 plasticizes the polymer, lowering its Tg and allowing enzalutamide to dissolve or disperse within the molten polymer at a relatively low temperature (e.g., 50-80 °C). The system is then rapidly depressurized, causing the CO2 to evaporate and instantly solidifying the mixture into a homogeneous amorphous dispersion. This solvent-free method is advantageous for thermally labile drugs and reduces residual solvent concerns.

stateDiagram-v2
    [*] --> Pressurize_Heat: Load Enzalutamide + Polymer
    Pressurize_Heat --> Supercritical: Inject CO2, T > 31.1C, P > 73.8 bar
    Supercritical --> Mixing: Drug dissolves in plasticized polymer
    Mixing --> Depressurize: Rapid pressure release
    Depressurize --> Solid_Dispersion: CO2 evaporates, mixture solidifies
    Solid_Dispersion --> [*]: Collect powder

Derivative 2.2: Point-of-Care Formulation via Electrospraying/Electrospinning

• Enabling Description: For personalized medicine, a miniaturized device utilizes electrohydrodynamic atomization to produce the enzalutamide dispersion at the point of care. A solution containing enzalutamide, a polymer, and a volatile solvent is fed through a nozzle maintained at a high electrical potential (5-30 kV) relative to a grounded collector plate. The strong electric field overcomes the solution's surface tension, forming a Taylor cone and emitting a fine jet. For electrospraying, the jet breaks into highly charged droplets, which dry rapidly to form amorphous micro- or nanoparticles. For electrospinning, the jet solidifies into a continuous fiber. The resulting particles or fiber mat can be collected on an edible substrate for immediate oral administration, allowing for precisely tailored patient-specific dosing.

sequenceDiagram
    participant Pharmacist
    participant ElectrospinningDevice
    participant Patient
    Pharmacist->>ElectrospinningDevice: Load drug-polymer solution & dose info
    activate ElectrospinningDevice
    ElectrospinningDevice->>ElectrospinningDevice: Apply high voltage (20kV)
    ElectrospinningDevice->>ElectrospinningDevice: Extrude solution as fiber onto edible film
    ElectrospinningDevice-->>Pharmacist: Dispense dose-loaded film
    deactivate ElectrospinningDevice
    Pharmacist->>Patient: Administer personalized dose

3. Cross-Domain Application

Derivative 3.1: Agrochemical Application - Enhanced Bioavailability of Fungicides

• Enabling Description: A poorly water-soluble fungicide, such as azoxystrobin, is formulated as a solid amorphous dispersion with an environmentally safe, water-soluble polymer (e.g., polyvinyl alcohol, lignin derivatives). The fungicide and polymer are co-dissolved in a solvent and spray-dried to produce a water-dispersible granule (WDG). When added to a spray tank, the granules dissolve to form a supersaturated solution of the fungicide. This enhances the adhesion to plant cuticles and increases the rate of absorption into the plant tissue, leading to improved efficacy at lower application rates and reduced environmental runoff of crystalline pesticide residues.

graph TD
    A[Fungicide: Azoxystrobin]
    B[Polymer: Polyvinyl Alcohol]
    A & B --> C{Spray Drying};
    C --> D[Water-Dispersible Granule];
    D --> E{Add to Water Spray Tank};
    E --> F[Supersaturated Fungicide Solution];
    F --> G[Application to Crops];

Derivative 3.2: Aerospace Application - Stabilization of Organic Sensor Reagents

• Enabling Description: A sensitive organic chromophore, used in a life-detection instrument for a Mars rover, is stabilized for long-term storage and exposure to radiation and extreme temperature fluctuations. The chromophore is formulated as a solid amorphous dispersion with a high-Tg, radiation-resistant polymer such as polyimide or a specialized grade of HPMCAS. The dispersion is created via spray-drying and deposited as a thin film on the surface of an optical sensor. The polymer matrix immobilizes the chromophore, preventing photo-bleaching, thermal degradation, and crystallization, ensuring the sensor remains calibrated and functional throughout a multi-year deep-space mission.

classDiagram
    class SensorSystem {
        +missionDuration: "4 years"
        +operatingTemp: "-70C to +20C"
    }
    class OrganicChromophore {
        -isSensitiveToRadiation: true
        -isThermallyLabile: true
    }
    class StabilizingPolymer {
        <<High-Tg>>
        +polymer: Polyimide
        +glassTransitionTemp: "> 200C"
    }
    SensorSystem "1" *-- "1" OrganicChromophore : contains
    OrganicChromophore "1" -- "1" StabilizingPolymer : dispersedIn

Derivative 3.3: Food Science Application - Bioavailability of Nutraceuticals

• Enabling Description: A poorly bioavailable nutraceutical, such as curcumin or coenzyme Q10, is formulated as a solid amorphous dispersion using a food-grade polymer (e.g., hydroxypropyl methylcellulose, gum arabic). The process involves hot-melt extrusion of the nutraceutical and polymer, producing a solid extrudate which is then milled into a fine powder. This powder is incorporated into functional foods, such as protein bars or beverage mixes. The amorphous dispersion significantly increases the solubility and subsequent absorption of the nutraceutical in the gastrointestinal tract, allowing for a demonstrably higher clinical effect from a lower dose compared to the crystalline form.

flowchart TD
    subgraph Hot-Melt Extrusion
        A[Nutraceutical: Curcumin]
        B[Food-Grade Polymer: HPMC]
    end
    A & B --> C[Extruder];
    C --> D[Solid Extrudate];
    D --> E[Milling];
    E --> F[Amorphous Dispersion Powder];
    F --> G{Incorporate into Protein Bar};

4. Integration with Emerging Tech

Derivative 4.1: AI-Driven Continuous Manufacturing Process Control

• Enabling Description: A continuous manufacturing line for amorphous solid dispersions, using hot-melt extrusion, is controlled by a machine learning model. In-line Process Analytical Technology (PAT) sensors, including Near-Infrared (NIR) and Raman spectroscopy probes, monitor the extrudate in real-time. The spectral data feeds into a pre-trained convolutional neural network (CNN) that predicts the degree of amorphicity and drug content uniformity. The AI controller dynamically adjusts process parameters—such as extruder screw speed, barrel temperature profile, and feed rate—to maintain the product within predefined quality specifications, minimizing batch-to-batch variability and enabling real-time release.

graph LR
    A[API + Polymer Feed] --> B(Hot-Melt Extruder);
    B --> C[Extrudate];
    C -- Real-time data --> D(PAT Sensors - NIR/Raman);
    D -- Spectral Data --> E(AI Control System - CNN);
    E -- Adjusts Parameters --> B;
    C --> F[Finished Dosage Form];

Derivative 4.2: IoT-Enabled Smart Packaging for Stability Monitoring

• Enabling Description: A pharmaceutical blister pack or bottle is equipped with a printed, disposable sensor label containing IoT connectivity (e.g., NFC, low-power Bluetooth). The sensor monitors the micro-environment within the package, specifically temperature and relative humidity. The data is logged at regular intervals. When a patient or pharmacist scans the package with a smartphone, the data is uploaded to a cloud database. An algorithm assesses the cumulative environmental exposure against the known stability profile of the specific amorphous dispersion (based on its Tg vs. humidity curve). The system can then issue an alert if the product's stability has been compromised, preventing the administration of a potentially sub-potent or crystallized drug product.

sequenceDiagram
    participant IoT_Sensor
    participant Smartphone
    participant Cloud_Platform
    participant Patient
    loop Periodic Logging
        IoT_Sensor->>IoT_Sensor: Log Temp & Humidity
    end
    Patient->>Smartphone: Scan package (NFC)
    Smartphone->>IoT_Sensor: Request data
    IoT_Sensor-->>Smartphone: Transmit stored data
    Smartphone->>Cloud_Platform: Upload environmental history
    activate Cloud_Platform
    Cloud_Platform->>Cloud_Platform: Analyze data against stability model
    Cloud_Platform-->>Smartphone: Send Status (OK / Alert)
    deactivate Cloud_Platform
    Smartphone->>Patient: Display product status

5. The "Inverse" or Failure Mode

Derivative 5.1: Triggered-Crystallization for On-Demand Inactivation

• Enabling Description: A solid amorphous dispersion of enzalutamide is formulated with a photocatalytic excipient (e.g., titanium dioxide nanoparticles) incorporated into the polymer matrix. The formulation is stable under normal storage conditions and amber packaging. However, upon exposure to a specific wavelength of UV light (e.g., 365 nm), the photocatalyst generates localized heat or reactive species that act as nucleation sites, triggering rapid conversion of the amorphous drug to its stable, less-soluble crystalline form. This serves as a fail-safe mechanism for disposal. An "inactivation device" could expose returned or expired tablets to UV light, rendering the API poorly bioavailable and environmentally safer for disposal.

stateDiagram-v2
    state Amorphous {
        description: High Bioavailability
    }
    state Crystalline {
        description: Low Bioavailability
    }
    Amorphous --> Crystalline: UV Light (365nm) exposure
    [*] --> Amorphous: Formulation
    Crystalline --> [*]: Inactivated for Disposal

Combination Prior Art Scenarios

1. AI Formulation with Open-Source Standards: The AI-driven process control system (Derivative 4.1) is implemented using the TensorFlow open-source machine learning framework. The disclosure includes the Python code for a convolutional neural network model architecture designed to accept 1D spectral data from a PAT sensor as input and output a classification of "amorphous," "partially crystalline," or "crystalline," along with a regression value for predicted drug concentration. The model is trained on a public dataset of polymer/API spectra.

2. IoT Stability Monitoring with Open-Source Protocols: The IoT-enabled smart packaging system (Derivative 4.2) is built entirely on open-source standards. The sensor communicates using the MQTT (Message Queuing Telemetry Transport) protocol over Bluetooth Low Energy. The data is transmitted to a cloud server running an instance of the ThingsBoard open-source IoT platform, which provides data collection, processing, and visualization dashboards for monitoring the stability of entire batches of the pharmaceutical product throughout the supply chain.

3. Blockchain-Verified Supply Chain with Open-Source Ledger: The authenticity and stability of the enzalutamide dispersion are tracked using a decentralized application built on the Hyperledger Fabric open-source blockchain framework. A smart contract (chaincode) is disclosed, which defines the on-chain logic. The contract requires that for a batch to be validated, the manufacturing parameters from the extruder, the lot numbers of the API and polymer, and a hash of the IoT stability data (from Derivative 4.2) must all be recorded as transactions on the immutable ledger. This creates a verifiable "digital passport" for each batch, preventing counterfeiting and ensuring quality.