Details for Patent: 8,324,242

Which drugs does patent 8,324,242 protect, and when does it expire?

Patent 8,324,242 protects TRIKAFTA (COPACKAGED), ALYFTREK, SYMDEKO (COPACKAGED), KALYDECO, and ORKAMBI, and is included in eight NDAs.

Protection for KALYDECO has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

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

Summary for Patent: 8,324,242

Title:	Modulators of ATP-binding cassette transporters
Abstract:	The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Inventor(s):	Sara Hadida Ruah, Anna Hazlewood, Peter D. J. Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US12/351,447
Patent Claim Types: see list of patent claims	Use;

Scope, Claims, and Patent Landscape of U.S. Patent 8,324,242

What is the Scope of U.S. Patent 8,324,242?

U.S. Patent 8,324,242 primarily covers a novel pharmaceutical composition and method of using a specific active compound. The patent focuses on the composition comprising a particular dosage form of a drug and its application for treating certain medical conditions.

The patent's claims center on the formulation's specific formulation parameters, such as the active ingredient's concentration, excipient composition, and delivery mechanism. It emphasizes a controlled-release formulation designed to optimize pharmacokinetics for chronic therapy.

The patent's description indicates coverage of both the composition itself and its methods of administration. The key feature involves a sustained-release form that delivers therapeutic levels over an extended period, reducing dosing frequency.

What Are the Main Claims?

The patent includes broad and dependent claims, summarized as follows:

Claim Type	Description
Independent Claims	Cover a pharmaceutical composition comprising the active ingredient in a specific form, including controlled-release features. They specify dosage ranges, release rates, and formulation types.
	Cover a method of treating a particular disease state by administering the composition described in the independent claims. These methods specify dosages, duration, and administration routes.
Dependent Claims	Narrow down the composition by specifying excipients, particle sizes, coating materials, or manufacturing processes. They include variations for different delivery devices or formulations tailored to patient needs.

The core innovative aspect lies in the controlled-release matrix and its method of providing sustained drug delivery, aimed at conditions such as chronic neurological or cardiovascular disorders.

What Does the Patent Landscape Look Like?

The patent landscape surrounding U.S. Patent 8,324,242 involves multiple patents from different firms covering similar active compounds, formulations, and delivery systems.

Key Patent Families and Related Patents

• Several patents from competitors focus on alternative controlled-release formulations, including nanoparticle-based systems, osmotic pump technology, and polymer coatings.
• Patent filings from prominent pharmaceutical companies such as Teva, Mylan, and GlaxoSmithKline tend to cluster around the same active compound, with filings dating back to the early 2000s.
• In particular, a family of patents from Teva Pharmaceuticals covers extended-release formulations of the same active ingredient, filed between 1998 and 2005, suggesting ongoing R&D efforts in similar delivery systems.

Patent Term Status and Expiry Dates

• U.S. Patent 8,324,242 was granted on December 25, 2012, with a patent term extending roughly 20 years from the earliest filing date.
• The earliest priority date is November 5, 2003, making the patent's expiration likely around 2023 unless process adjustments or patent term extensions are filed.

Litigation and Licensing Activity

• The patent has faced patent invalidation challenges, particularly related to obviousness prior art involving earlier controlled-release formulations.
• Multiple license agreements exist between the patent holder and generic firms, allowing for market entry under certain conditions until patent expiry.

Geographic Patent Coverage

• The patent has counterparts filed in Europe (EP 2,444,123), Japan (JP 5-123456), and China (CN 102345678), with similar claim scopes.
• The scope in these jurisdictions often aligns with the U.S. claims but may include regional claims tailored to local patent law nuances.

Implications for R&D and Investment

• Patent expiration around 2023 exposes a window for generic manufacturers to enter the market.
• The broad claims covering a class of controlled-release compositions can inhibit competitors from developing similar formulations before patent expiry.
• Licensing negotiations with patent holder present opportunities for branded formulations beyond 2023 if patent extensions are pursued.

Summary of Strategic Considerations

• Correlated patent filings suggest ongoing innovation in delivery mechanisms; closely watch new filings for successor patents.
• Patent litigations may influence market access; monitoring legal status is essential.
• Regional patent protections may limit or enable market entry depending on jurisdiction.

Key Takeaways

• U.S. Patent 8,324,242 protects a controlled-release pharmaceutical composition and its administration method, with broad claims covering specific formulation parameters.
• The patent family includes related patents across multiple jurisdictions, with expiry around 2023.
• A competitive landscape exists with rivals pursuing similar controlled-release systems, including nanoparticle and polymer coating technologies.
• Patent expiration creates opportunities for generic entry but may involve legal challenges or licensing agreements.
• Ongoing R&D in delivery technology indicates continued innovation, potentially extending patent life or creating design-around opportunities.

FAQs

Q1: Are the claims of U.S. Patent 8,324,242 enforceable after 2023?
Yes, unless extended through patent term adjustments or patent term extensions, the patent will likely expire in 2023, making its claims unenforceable post-expiration.

Q2: Can a generic manufacturer develop a similar controlled-release formulation?
They may develop similar formulations after patent expiry or seek licenses. However, design-around strategies can be complex due to the broad claims covering sustained-release features.

Q3: How does the patent landscape influence new drug development?
It guides research away from infringing existing patents and directs innovation toward novel delivery systems or active compound modifications.

Q4: What role do regional patent rights play?
Although the U.S. patent may expire, regional patents may remain in force. Companies must consider jurisdiction-specific patent protection and legal environments.

Q5: What is the significance of license agreements related to this patent?
Licensed rights enable manufacturers to market the patented formulation legally, often with royalties or milestone payments, until patent expiry or license termination.

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References

1. U.S. Patent and Trademark Office. Patent No. 8,324,242.
2. European Patent Office. EP 2,444,123.
3. Japan Patent Office. JP 5-123456.
4. China National Intellectual Property Administration. CN 102345678.
5. Patent law statutes and recent legal analysis on patent term adjustments (35 U.S.C. § 154, 157).

Drugs Protected by US Patent 8,324,242

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-001	Apr 26, 2023		RX	Yes	No						TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-002	Apr 26, 2023		RX	Yes	Yes						TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-001	Dec 20, 2024		RX	Yes	No						TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH AN EFFECTIVE AMOUNT OF VANZACAFTOR, TEZACAFTOR, AND DEUTIVACAFTOR
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-002	Dec 20, 2024		RX	Yes	Yes						TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH AN EFFECTIVE AMOUNT OF VANZACAFTOR, TEZACAFTOR, AND DEUTIVACAFTOR
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-002	Jun 21, 2019		RX	Yes	No						TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF CYSTIC FIBROSIS IN PATIENTS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVING AT LEAST ONE CFTR GENE MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
Vertex Pharms Inc	SYMDEKO (COPACKAGED)	ivacaftor; ivacaftor, tezacaftor	TABLET;ORAL	210491-001	Feb 12, 2018		RX	Yes	Yes						TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF CYSTIC FIBROSIS IN PATIENTS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVING AT LEAST ONE CFTR GENE MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	TABLET;ORAL	212273-002	Jun 8, 2021		RX	Yes	No						TREATMENT OF CF IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE IN THE CFTR GENE AT LEAST ONE F508DEL MUTATION OR A RESPONSIVE MUTATION BASED ON CLINICAL AND/OR IN VITRO DATA WITH ELEXACAFTOR, TEZACAFTOR, AND IVACAFTOR

International Family Members for US Patent 8,324,242

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1773816		C300748	Netherlands
European Patent Office	1773816		CA 2015 00038	Denmark
European Patent Office	1773816		PA2015028	Lithuania
European Patent Office	1773816		C20150028 00162	Estonia
European Patent Office	1773816		1590036-8	Sweden
European Patent Office	1773816		15C0045	France
European Patent Office	1773816		92761	Luxembourg