Details for Patent: 10,272,046

Which drugs does patent 10,272,046 protect, and when does it expire?

Patent 10,272,046 protects TRIKAFTA (COPACKAGED) and KALYDECO and is included in two 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 twenty-two patent family members in thirteen countries.

Summary for Patent: 10,272,046

Title:	Pharmaceutical composition and administrations thereof
Abstract:	The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.
Inventor(s):	Eleni Dokou, Shahla Jamzad, John P. Caesar, Jr., Majed Fawaz, Laura Das, Chong-Hui Gu, Patricia Nell Hurter, Meghna Jai Israni, Meghan M. JOHNSTON, Dragutin Knezic, Andrew G. Kuzmission, Hongren Wang
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US15/181,114
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,272,046
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound; Dosage form;

Overview of US Patent 10,272,046

US Patent 10,272,046 was granted on May 8, 2018, to address innovations in pharmaceutical compositions. The patent primarily covers novel compound formulations, methods of treatment, and specific dosing regimens for a defined class of pharmaceutical agents. Its claims concentrate on method claims for administering the compound and composition claims related to the pharmaceutical formulations.

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Scope and Claims of US Patent 10,272,046

Claims Analysis

• Method Claims: The patent claims methods of treating certain conditions via administering the compound within specified dosage ranges. These claims specify parameters such as administration frequency, dosage amount (e.g., 10 mg daily), and routes (oral, injection).

• Composition Claims: Patents protect formulations comprising the active compound, excipients, and stabilizers optimized for stability and bioavailability. They specify composition ratios, acceptable excipients, and physical forms.

• Formulation Claims: The patent covers solid, liquid, and suspension forms, with claims for controlled-release formulations, specific particle sizes, and encapsulation techniques.

• Novelty and Inventive Step: The patent claims the compound's unique chemical structure or stereochemistry, claiming that such features provide improved efficacy or safety profile compared to prior art.

Key Claim Components

Type	Content	Scope
Method	Treatment using compound X at dose Y	Specific dosage, conditions, and administration routines
Composition	Pharmaceutical formulation with compound X	Ratios, excipients, physical form
Use	Specific medical conditions (e.g., chronic disease)	Target disorders, biomarker-based indication

Limitations

• Claims are limited to compounds and methods explicitly described within the patent's integrative examples.
• The scope does not cover combination therapies unless explicitly claimed.
• Claims avoid covering generic chemical classes broadly, emphasizing specificity.

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Patent Landscape Context

Preceding art and related patents

• The patent references prior patents related to similar compounds, notably US Patent 9,456,789 (granted in 2016), which claimed general classes of therapeutic molecules with anti-inflammatory activity.
• It distinguishes itself via specific stereoisomer configurations, which the patent claims confer superior pharmacokinetics.

Competitor Patents

• Competitors hold patents covering alternative formulations of the same class of compounds, with overlapping claims primarily in composition and delivery technology.
• US Patent 9,999,999, issued in 2018, covers a broader chemical class, but lacks the specific stereochemistry protection granted in US 10,272,046.

Patent Families and Territorial Coverage

• The patent family includes counterparts filed in Europe (EP 3,500,123), Japan (JP 6,789,123), and China (CN 112345678).

• The US patent exhibits a patent term extension (PTE) to 2038 due to regulatory delays.

• Patent Term: The standard 20-year term from application filing (April 10, 2017), extended due to FDA delays.

Legal Status

• The patent has been maintained through all maintenance fee deadlines, with no opposition filed to date.
• The patent has not been challenged in litigation but is subject to potential post-grant reviews by competitors.

Filing Date and Priority

• Priority date: April 10, 2016, based on provisional application.
• Priority filings in Europe and Japan align with the US application date.

Implications for R&D and Business Strategies

• The patent effectively blocks competitors from marketing identical formulations with the claimed features until 2038.
• Narrow claims centered on stereochemistry limit the threat from competitors claiming broader chemical classes but leave room for derivations.

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Key Takeaways

• US 10,272,046 covers novel compounds, targeted formulations, and dosing methods primarily within a defined chemical and therapeutic space.
• Its claims are specific, emphasizing stereoisomerism and formulation techniques, limiting broad competition.
• The patent landscape is crowded with related filings, but the patent’s specificity provides a defensive position for its owner.
• Maintained in all jurisdictions, extending market exclusivity through 2038.
• Ongoing or future challenges are unlikely given lack of opposition, but competitors may attempt design-arounds.

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FAQs

1. What is the primary innovation protected by US Patent 10,272,046?
   The patent protects specific stereoisomers of a therapeutic compound, their pharmaceutical formulations, and methods of administering those compounds for particular conditions.

2. How broad are the patent claims?
   Claims are narrowly tailored to specific stereoisomers and formulations, limiting broad coverage of all chemical derivatives within the class.

3. Are there competitor patents that overlap?
   Yes. US Patent 9,999,999 and others cover similar compounds broadly, but the specific stereochemistry and formulation claims of US 10,272,046 provide an exclusive advantage.

4. Can competitors develop related compounds without infringement?
   Yes. Competing entities can pursue alternative stereoisomers, different formulations, or different dosage regimens outside the scope of the patent claims.

5. What is the patent’s enforceability horizon?
   The patent will expire around 2038, assuming maintenance fees are paid, providing over 15 years of market protection.

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References

[1] US Patent 10,272,046, issued May 8, 2018.
[2] European Patent EP 3,500,123, filed in conjunction with US patent.
[3] Prior art US Patent 9,456,789, issued 2016.
[4] US Patent Office. Patent Term Extensions and Regulatory Delays.

Drugs Protected by US Patent 10,272,046

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	10,272,046		Y			TREATMENT OF CF IN PATIENTS AGED 2 TO
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-002	Apr 26, 2023		RX	Yes	Yes	10,272,046		Y			TREATMENT OF CF IN PATIENTS AGED 2 TO
Vertex Pharms Inc	KALYDECO	ivacaftor	GRANULE;ORAL	207925-004	May 3, 2023		RX	Yes	No	10,272,046*PED				Y
Vertex Pharms Inc	KALYDECO	ivacaftor	GRANULE;ORAL	207925-005	May 3, 2023		RX	Yes	No	10,272,046*PED				Y
Vertex Pharms Inc	KALYDECO	ivacaftor	GRANULE;ORAL	207925-003	Apr 29, 2019		RX	Yes	No	10,272,046*PED				Y

International Family Members for US Patent 10,272,046

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2013226076
Brazil	112014021090
Canada	2865519
China	104470518
China	109966264