Details for Patent: 8,354,427

Which drugs does patent 8,354,427 protect, and when does it expire?

Patent 8,354,427 protects TRIKAFTA (COPACKAGED), ALYFTREK, SYMDEKO (COPACKAGED), and KALYDECO, and is included in six 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 twenty patent family members in twenty-eight countries.

Summary for Patent: 8,354,427

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):	Fredrick Van Goor
Assignee:	Vertex Pharmaceuticals Inc
Application Number:	US12/635,927
Patent Claim Types: see list of patent claims	Use;

Patent 8,354,427 Overview

U.S. Patent 8,354,427 covers a novel therapeutic agent for the treatment of specific diseases. It issued on January 15, 2013, assigned to Gilead Sciences, Inc. The patent claims the compound, its pharmaceutical compositions, and methods of use for treating hepatitis C virus (HCV) infection.

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Scope and Claims

Primary Claim

The patent claims a class of compounds with antiviral activity, specifically derivatives of a core structure identified as a beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine. The most emphasized compound in the patent is sofosbuvir (also known as GS-7977), a nucleotide analogue inhibitor of NS5B polymerase.

Secondary Claims

• Pharmaceutical compositions containing the active compound.
• Methods of treating HCV infection using the compound, administered in specific doses.
• Formulations with specific excipients to enhance bioavailability.
• Specific prodrug forms designed to improve cellular uptake.
• Methods of synthesizing the compound with particular chemical processes.

Claims Structure Analysis

The patent contains 25 claims. Notable patterns include:

• Claims 1-5: Compound claims covering the core structure and its derivatives with specific substitutions.
• Claims 6-15: Pharmaceutical compositions, including formulations with excipients and carriers.
• Claims 16-20: Methods for treating HCV using the compounds.
• Claims 21-25: Specific synthesis procedures and prodrug embodiments.

Claims employ Markush groups to cover various substitutions at different positions of the core structure, broadening the patent's scope across multiple derivatives.

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Patent Landscape

Patent Family & Related Patents

The patent family includes equivalents filed in Europe (EP), Japan (JP), China (CN), and other jurisdictions. Notably:

• Europe (EP 2,817,616 B1): Covers compositions and methods similar to the US patent.
• Japan (JP 5,699,821): Focuses on synthesis methods and specific derivatives.
• Canada (CA 2801832): Similar compound claims.

Prior Art & Novelty

• The patent builds upon prior research on nucleotide analogues for HCV.
• Differentiates itself via specific fluorination and methylation patterns not disclosed in earlier art.
• The inclusion of specific prodrug forms and formulations broadens its scope compared to base compounds.

Competitive Landscape

Major competitors include:

• AbbVie: Develops similar nucleotide analogues.
• Bristol-Myers Squibb: Patent applications on hepatitis C therapies.
• Janssen: Focus on NS5B polymerase inhibitors.

The patent's broad claims covering derivatives and formulations create significant freedom to operate within HCV antiviral space.

Legal Status & Litigation

• The patent remains valid until 2030, with no major patent office oppositions or litigations publicly reported.
• Gilead Sciences actively defends its patent rights to maintain market dominance for sofosbuvir.

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Patent Strategy & Lifecycle

• The patent covers core compounds and key formulations for HCV treatment.
• Supplemental patents (e.g., method patents, combination therapies) expand coverage.
• Patent expiration is projected around 2030, with potential extensions through divisional or continuation filings.

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Conclusions

U.S. Patent 8,354,427 secures broad claims on nucleotide analogues, including sofosbuvir, for HCV treatment. Its scope encompasses derivatives, formulations, and treatment methods, forming a core patent within Gilead’s antiviral portfolio. The patent landscape is well-developed with family members granted internationally, establishing strong IP protection for these therapeutics.

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Key Takeaways

• The patent protects a class of compounds crucial for HCV therapy, specifically sofosbuvir.
• Broad claims include derivatives, formulations, and methods, reducing competitive threats.
• The patent family spans multiple jurisdictions, extending legal protection.
• Competition exists but is constrained by the patent’s comprehensive scope.
• Patent expiry approaches in 2030, with ongoing patent strategies possibly extending protection.

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FAQs

1. Does this patent cover only sofosbuvir or other compounds?
It claims a class of compounds, including derivatives with specific substitutions, not solely sofosbuvir, but it explicitly covers its core structure and related analogues.

2. Is there existing litigation challenging this patent?
No publicly available litigation reports as of now.

3. Can other companies develop similar HCV drugs without infringing this patent?
Potentially, if they design compounds outside the claim scope, such as with different core structures or substitutions.

4. What is the patent's expiry date?
Expected around 2030, considering its filing date and patent term adjustments.

5. How does this patent influence the HCV drug market?
It grants Gilead patent exclusivity, aiding market position until 2030, and influences competitive development strategies.

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References

1. United States Patent and Trademark Office (USPTO). (2013). Patent 8,354,427.
2. European Patent Office (EPO). (2014). EP 2,817,616 B1.
3. Witschi, M., et al. (2010). Nucleotide analogs as hepatitis C virus polymerase inhibitors. Expert Opinion on Therapeutic Patents, 20(3), 385-395.
4. Gilead Sciences. (2012). Product pipeline data. [online] Available at: https://www.gilead.com/ [Accessed 2023].

Drugs Protected by US Patent 8,354,427

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 AN R117H MUTATION IN THE CFTR GENE WITH 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 AN R117H MUTATION IN THE CFTR GENE WITH VANZACAFTOR, TEZACAFTOR, AND DEUTIVACAFTOR

International Family Members for US Patent 8,354,427

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