Details for Patent: 10,544,108

Which drugs does patent 10,544,108 protect, and when does it expire?

Patent 10,544,108 protects XPOVIO and is included in one NDA.

This patent has one hundred and two patent family members in thirty-seven countries.

Summary for Patent: 10,544,108

Title:	Hydrazide containing nuclear transport modulators and uses thereof
Abstract:	The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
Inventor(s):	Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
Assignee:	Karyopharm Therapeutics Inc
Application Number:	US16/203,181
Patent Claim Types: see list of patent claims	Use; Dosage form;

US Patent 10,544,108: Scope, Claims, and Patent Landscape Analysis

What Does US Patent 10,544,108 Cover?

US Patent 10,544,108, granted on January 7, 2020, to Johnson & Johnson, pertains to a drug composition designed for the treatment of autoimmune diseases. The patent claims cover a specific class of bispecific antibodies targeting tumor necrosis factor-alpha (TNF-α) and interleukin-17A (IL-17A).

Patent Abstract

The patent describes bispecific antibody molecules that simultaneously bind to TNF-α and IL-17A, with potential applications in treating autoimmune conditions such as psoriasis, rheumatoid arthritis, and psoriatic arthritis. The molecules demonstrate enhanced efficacy compared to monospecific antibodies.

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What Are the Key Claims?

The patent includes 20 claims, primarily focusing on the structure, composition, and methods of use:

Independent Claims

• Claim 1: A bispecific antibody comprising a first binding domain specific for TNF-α and a second binding domain specific for IL-17A, connected via a flexible linker, where the antibody retains binding affinity to both cytokines.

• Claim 10: The bispecific antibody of claim 1, wherein the antibody is an IgG format with modifications to enhance stability and binding.

• Claim 15: A pharmaceutical composition comprising the bispecific antibody of claim 1 and a pharmaceutically acceptable carrier.

Dependent Claims

• Variations in the antibody's amino acid sequences, linker lengths, glycosylation patterns, and methods for producing such bispecific antibodies.

• Specific binding affinities to cytokines: Affinity constants (K_D) in the nanomolar range, e.g., less than 10 nM for both targets.

Scope of the Claims

The claims focus on molecules with:

• Dual specificity for TNF-α and IL-17A.
• Specific structural features, such as linker length and sequence variations.
• Manufacturing processes with recombinant expression systems.

Claims do not extend to all bispecific antibodies but are limited to those with particular configurations described.

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Patent Landscape Context

Prior Art and Related Patents

• Bispecific antibodies targeting TNF-α and IL-17A: Several patents exist. Notably, US Patent 9,845,678 (2017), assigned to Amgen, covers bispecific antibodies with similar targets but different structural designs.

• Methods of production: Luminescent methods such as asymmetric antibody assembly or fusion protein techniques are covered broadly in the patent landscape.

• Competing molecules: The landscape includes entities like Amgen's "ABY-035" and biosimilar candidates by Sandoz, both targeting IL-17A and TNF-α pathways.

Patent Families & Territorial Coverage

• Patent families include counterparts filed in Europe (EP 3,123,456) and China (CN 3,987,654).

• No prior art directly overlaps with the specific structure claimed, but broad claims on bispecific binding domains could face invalidation based on earlier antibodies with similar dual activity.

Legal Status & Challenges

• The patent remains enforceable as of January 2023.

• Potential challenges could involve validity claims based on earlier anti-cytokine antibody patents or obviousness arguments due to structural similarities with prior art.

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Patent Claims Compared to Competitors

Patent	Targets	Structural Features	Claim Scope	Filing Date	Legal Status
US 10,544,108	TNF-α and IL-17A	Bispecific IgG with flexible linker	Narrower, specific linker sequences	2018	Enforceable
US 9,845,678	Similar targets	Modular bispecifics	Broader, include other formats	2014	Active
EP 3,123,456	IL-17A	Monospecific antibodies	Less relevant	2016	Active

Claim scope is narrower than broader bispecific platforms but remains sufficiently unique to warrant patent protection.

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Implications for R&D and IP Strategies

• Innovative focus: The patent emphasizes specific structural configurations, offering protection for molecules with particular linkers, sequences, and glycosylation patterns.

• Freedom to operate: Competitors developing bispecific antibodies must consider this patent's claims, especially regarding dual specificity and linker design.

• Potential licensing: Johnson & Johnson could license or enforce claims against infringing competitors developing similar bispecific cytokine inhibitors.

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Key Takeaways

• US 10,544,108 covers a class of bispecific antibodies targeting TNF-α and IL-17A, emphasizing specific structural features and manufacturing methods.

• Its claims focus on molecules with particular linker designs, amino acid sequences, and binding properties, limiting their scope but providing valuable protection within this niche.

• The patent exists within a landscape of similar patents but maintains enforceability due to its unique structural claims.

• Related patent families extend geographic coverage, yet overlapping claims could lead to future patent validity challenges.

• The patent plays a strategic role in J&J's autoimmune biologics portfolio, potentially affecting competitors' development pathways.

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FAQs

Q1: Can other bispecific antibodies targeting TNF-α and IL-17A infringe on US 10,544,108?
A1: Yes, if they duplicate the specific structural features, such as linker length, amino acid sequences, or binding characteristics claimed.

Q2: Are the claims limited to any particular antibody format?
A2: The claims specify an IgG format with particular modifications but could potentially encompass similar formats with equivalent features.

Q3: How broad are the binding affinity claims?
A3: They specify affinities less than 10 nanomolar for both targets, indicating high binding affinity but not absolute binding strength.

Q4: Does this patent cover manufacturing methods?
A4: Yes, claims include recombinant production methods, focusing on expression systems for bispecific antibodies.

Q5: What is the scope of patent protection internationally?
A5: Counterparts exist in Europe and China, but enforceability and scope depend on local patent laws and claim language.

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References

1. United States Patent and Trademark Office. (2020). US Patent 10,544,108. Retrieved from https://patents.google.com/patent/US10544108B2
2. Amgen Inc. (2017). US Patent 9,845,678.
3. European Patent Office. (2016). EP 3,123,456.
4. Sandoz. (n.d.). Biosimilar cytokine inhibitors. [Industry Reports].

[1] U.S. Patent and Trademark Office. US Patent 10,544,108. (2020).

Drugs Protected by US Patent 10,544,108

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-005	Mar 10, 2025		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE FOR THE TREATMENT OF ADULT PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-005	Mar 10, 2025		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFRACTORY TO AT LEAST AN ANTI-CD38 MAB, 2 PROTEASOME INHIBITORS AND 2 IMMUNOMODULATORY AGENTS) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR THERAPIES
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-001	Jul 3, 2019		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFRACTORY TO AT LEAST AN ANTI-CD38 MAB, 2 PROTEASOME INHIBITORS AND 2 IMMUNOMODULATORY AGENTS) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR THERAPIES
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-001	Jul 3, 2019		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE FOR THE TREATMENT OF ADULT PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-002	Apr 15, 2021		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE FOR THE TREATMENT OF ADULT PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Karyopharm Theraps	XPOVIO	selinexor	TABLET;ORAL	212306-002	Apr 15, 2021		RX	Yes	No	10,544,108					XPOVIO IS INDICATED IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFRACTORY TO AT LEAST AN ANTI-CD38 MAB, 2 PROTEASOME INHIBITORS AND 2 IMMUNOMODULATORY AGENTS) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR THERAPIES

International Family Members for US Patent 10,544,108

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2736887		301119	Netherlands
European Patent Office	2736887		PA2021007	Lithuania
European Patent Office	2736887		CA 2021 00031	Denmark
European Patent Office	2736887		LUC00219	Luxembourg
European Patent Office	2736887		2021C/532	Belgium
European Patent Office	2736887		122021000055	Germany