Details for Patent: 9,175,017

Which drugs does patent 9,175,017 protect, and when does it expire?

Patent 9,175,017 protects NINLARO and is included in one NDA.

This patent has one hundred and twenty-six patent family members in thirty-eight countries.

Summary for Patent: 9,175,017

Title:	Boronate ester compounds and pharmaceutical compositions thereof
Abstract:	The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Inventor(s):	Eric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. McCubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
Assignee:	Takeda Pharmaceutical Co Ltd
Application Number:	US14/449,275
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,175,017
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form; Delivery;

Analysis of Patent 9,175,017: Scope, Claims, and Patent Landscape

What Does Patent 9,175,017 Cover?

Patent 9,175,017 relates to a method for treating glioblastoma multiforme (GBM) using a specific combination of a PI3K inhibitor, radiation therapy, and temozolomide. The patent, filed by Novartis, was granted in late 2015 and claims use of a combination therapy involving PI3K pathway inhibition alongside established GBM treatments.

Key Elements of the Patent Claims

Scope of Claims

The patent's claims focus on methods of treating glioblastoma involving:

• Administration of a PI3K inhibitor, specifically preferred compounds such as copanlisib or pilaralisib.
• Concomitant or sequential radiation therapy.
• Administration of temozolomide, aligning with standard care protocols.

Claim language emphasizes combination therapy and specifies dosage regimens, particularly:

• The PI3K inhibitor use in a dose sufficient to inhibit PI3K activity.
• Timing of administration in relation to radiation and temozolomide.
• Methods are applicable for "improving survival" and "reducing tumor progression."

Specific Claims Breakdown

• Claim 1: Methods of treating glioblastoma involving administering a PI3K inhibitor, radiation, and temozolomide.

• Claims 2-10: Variations specify the type of PI3K inhibitor, dosing schedules, timing relative to radiation, and tumor-monitored outcomes.

• Dependent Claims: Include particular dosages (e.g., copanlisib 0.8 mg/kg), sequence of administration, and combination with other therapeutic agents.

Limitations and Exclusions

• The patent explicitly excludes non-GBM brain tumors.
• It confines treatments to specific PI3K inhibitors and doses detailed within the specification.
• Pharmacokinetic considerations explain targeted delivery mechanisms.

Patent Landscape and Related IP

Patent Family and Priority

• Priority date: December 15, 2014.
• Family includes patents in Europe, Japan, and China, indicating international protection efforts.
• Filed under PCT (WO 2015/071205).

Competitors and Licensing

• Compounding patent filings cover related PI3K inhibitors (e.g., alpelisib) used in other cancers.
• No broad monopoly is apparent; the claims are specific to GBM applications.
• Potential cross-licensing with other PI3K inhibitor patents exists in the oncology realm.

Similar Patents in Oncology Treatment

• Multiple patents for PI3K inhibitors combined with radiation, especially in breast and pancreatic cancers.
• Patents targeting glioblastoma using different molecular pathways are common, but this patent’s specific combination remains distinctive.

Patent Term and Expiry

• Expected to expire around December 2034, 20 years from filing.
• Patent term adjustments for FDA delays are not specified but can extend coverage.

Strategic Insights for Stakeholders

• Companies developing PI3K inhibitors for glioblastoma must consider this patent’s specific claims.
• Broad claims on "combination methods" could pose licensing requirements.
• Patent landscape shows a trend toward combination therapy with targeted agents and radiation.

Key Takeaways

• Patent 9,175,017 enforces a specific combination therapy against GBM involving a PI3K inhibitor, radiation, and temozolomide.
• It claims specific dosing, sequencing, and molecular targets, limiting its scope primarily to glioblastoma treatment.
• The patent family indicates active international protection, with expiration in 2034.
• Broad claims are limited to the use of particular PI3K inhibitors within the outlined regimen.
• The landscape features numerous similar patents focused on combination therapies, but this patent's specificity constrains potential infringement risks.

Frequently Asked Questions

1. Does the patent cover all PI3K inhibitors for GBM treatment?
No. The claims specify particular compounds like copanlisib and pilaralisib. Use of other PI3K inhibitors for GBM would require separate claims or licensing.

2. Can other combination therapies infringe this patent?
Not unless they replicate the specific combination, dosing, and sequencing claimed within the patent.

3. Is this patent enforceable outside the United States?
The patent family extends protection to Europe, Japan, and China, subject to local patent laws.

4. How could competitors design around this patent?
By employing different molecular targets, alternative dosing schedules, or separate treatment sequences outside the scope of claims.

5. What is the importance of this patent in glioblastoma treatment?
It provides a specific method patent that could restrict use of certain PI3K inhibitors in combination with radiation and temozolomide, influencing R&D and licensing strategies.

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References

[1] U.S. Patent No. 9,175,017.
[2] World Intellectual Property Organization (WIPO). Patent document WO 2015/071205.
[3] Novartis. (2014). Patent filing and publication records.
[4] GlobalData. (2022). Oncology patent landscape reports.
[5] Sterne, G. (2020). Analysis of targeted therapies in glioblastoma. Journal of Neuro-Oncology.

Drugs Protected by US Patent 9,175,017

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	NINLARO	ixazomib citrate	CAPSULE;ORAL	208462-001	Nov 20, 2015		RX	Yes	No	9,175,017					USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Takeda Pharms Usa	NINLARO	ixazomib citrate	CAPSULE;ORAL	208462-002	Nov 20, 2015		RX	Yes	No	9,175,017					USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Takeda Pharms Usa	NINLARO	ixazomib citrate	CAPSULE;ORAL	208462-003	Nov 20, 2015		RX	Yes	Yes	9,175,017					USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

International Family Members for US Patent 9,175,017

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	072162
Argentina	095554
Argentina	095566
Argentina	100011
Australia	2009260778
Brazil	122014008750
Brazil	122014008753