Details for Patent: 10,086,011

Which drugs does patent 10,086,011 protect, and when does it expire?

Patent 10,086,011 protects EPCLUSA and is included in one NDA.

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

This patent has thirty-four patent family members in nineteen countries.

Summary for Patent: 10,086,011

Title:	Combination formulation of two antiviral compounds
Abstract:	Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.
Inventor(s):	Eric Gorman, Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Lauren Wiser, Vahid Zia
Assignee:	Gilead Sciences Inc
Application Number:	US15/670,283
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,086,011
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

Scope and Claims Analysis for US Patent 10,086,011 (Hepatitis C): What Is Covered, What Drives Claim Validity, and How the Patent Landscape Impacts Generic and Licensing Risk

US Patent 10,086,011 is a US method-of-treatment patent with product-definition claim elements. It focuses on a specific fixed-dose composition for treating hepatitis C that combines (i) a “solid dispersion” of “Compound I” in a copovidone polymer matrix at a defined internal ratio (Compound I:copovidone ~1:1; Compound I substantially amorphous), together with (ii) defined proportions and solid-state attributes of substantially crystalline sofosbuvir (XRPD peaks), plus (iii) defined excipients and (iv) a defined treatment regimen duration (about 12 weeks), and (v) tablet dosage form details in dependent claims.

From a freedom-to-operate (FTO) standpoint, the claim scope is narrow on formulation and solid-state identity. It is broad enough to catch any hepatitis C method that uses a substantially similar composition, even if the overall sofosbuvir dose differs only within the listed weight ranges, and even if “Compound I” is not named in the claims except as “Compound I” by formula.

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What is US Patent 10,086,011 and what is the core invention scope?

Executive summary: The patent claims a hepatitis C treatment method that uses a therapeutically effective amount of a tablet-formulation-like composition containing a specific amorphous “Compound I” solid dispersion in copovidone and a defined fraction of substantially crystalline sofosbuvir characterized by XRPD peak positions, plus microcrystalline cellulose, croscarmellose sodium, and magnesium stearate, with treatment typically for about 12 weeks.

Claim architecture

The claims are drafted as method claims but incorporate composition limitations. Independent claim 1 covers a composition defined by weight ranges, including:

• Solid dispersion component (a): 1–25% w/w of a solid dispersion where Compound I is dispersed in copovidone; Compound I:copovidone weight ratio is about 1:1; Compound I is substantially amorphous.
• Sofosbuvir component (b): 35–45% w/w substantially crystalline sofosbuvir.
• Excipients (c–e):
  • 30–40% w/w microcrystalline cellulose
  • 1–5% w/w croscarmellose sodium
  • 0.5–2.5% w/w magnesium stearate
• Treatment endpoint: dependent claim 9 adds about 12 weeks.

Independent claim 10 tightens to specific “about” percentages:

• 20% w/w solid dispersion containing Compound I in copovidone at 1:1 ratio and substantially amorphous Compound I
• 40% w/w crystalline sofosbuvir
• 35.5% w/w microcrystalline cellulose
• 3% w/w croscarmellose sodium
• 1.5% w/w magnesium stearate

Independent claim 14 narrows further to an amount-per-dose example:

• 200 mg solid dispersion (Compound I:copovidone ~1:1; amorphous Compound I)
• 400 mg substantially crystalline sofosbuvir
• 355 mg microcrystalline cellulose
• 30 mg croscarmellose sodium
• 15 mg magnesium stearate

Dependent claim scope boosters

• XRPD identity features for “substantially crystalline sofosbuvir” (claims 2, 3, 11, 12, 17, 18): peak positions near 6.1° and 12.7° 2θ±0.2, and optionally 20.1° and 20.8° 2θ±0.2.
• Duration constraint: about 12 weeks (claims 9, 13, 19).
• Dosage form / coating: tablet with film coating (claim 15), coating is polyvinylalcohol-based (claim 16).

What is and is not claimed (based on the text provided)

• The claims are not drafted as nucleoside analog synthesis patents.
• They do not explicitly claim a drug substance process or a method step beyond “administering” the composition.
• They require both (i) a specific solid-state sofosbuvir descriptor and (ii) the specific copovidone/Compound I solid dispersion descriptor.

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Which portions of the claim are likely determinative for infringement?

Executive summary: For an accused hepatitis C regimen to infringe, the composition used in “administering” must match the claimed formulation architecture, and the accused sofosbuvir must meet the XRPD-defined crystalline peak conditions in the relevant dependent claims.

Partitioning the claim into infringement-critical features

1. The “solid dispersion” of Compound I in copovidone

   • 1–25% w/w (claim 1) or 20% w/w (claim 10) or 200 mg per dose (claim 14)
   • internal weight ratio Compound I:copovidone = ~1:1
   • Compound I is substantially amorphous

2. Sofosbuvir solid state

   • “substantially crystalline sofosbuvir” with XRPD peak inclusion (claims 2/3/11/12/17/18)
   • If an accused product does not meet the XRPD criteria for the dependent claims, it may still fall under independent claims 1/10/14 if those independent claims do not incorporate the XRPD peaks as limitations (they do not, per your text; XRPD appears only in dependent claims).

3. Fixed excipient proportions

   • microcrystalline cellulose: 30–40% w/w (or 35.5% in dependent independent form)
   • croscarmellose sodium: 1–5% w/w (or 3%)
   • magnesium stearate: 0.5–2.5% w/w (or 1.5%)

4. Treatment duration (dependent)

   • about 12 weeks

5. Tablet film coating (dependent)

   • film coating: polyvinylalcohol-based

Practical infringement mapping

• To infringe claim 1 or 10, an accused hepatitis C regimen must administer a composition within the claimed weight ranges / “about” values including the solid dispersion feature with amorphous Compound I in copovidone at 1:1 ratio.
• To infringe claims 2/3, 11/12, 17/18, the accused sofosbuvir crystalline form must generate XRPD peaks at the specified 2θ positions within ±0.2 and meet the peak set for the particular dependent claim.
• To infringe claims 15–16, the accused dosage form must be a tablet with film coating and the coating must be polyvinyl alcohol-based.

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How broad are the weight-range claims versus the “about fixed composition” claims?

Executive summary: Claims 1, 10, and 14 create three layers of scope: (i) broad weight ranges (claim 1), (ii) tighter fixed “about” percentages (claim 10), and (iii) example-level per-dose amounts plus dosage form narrowing in dependent claims (claim 14).

Weight range coverage (claim 1)

• Solid dispersion: 1–25% w/w
• Sofosbuvir: 35–45% w/w
• Microcrystalline cellulose: 30–40% w/w
• Croscarmellose sodium: 1–5% w/w
• Magnesium stearate: 0.5–2.5% w/w

This claim can cover multiple formulation variants as long as they preserve:

• the copovidone solid dispersion with Compound I at ~1:1 ratio and amorphous character, and
• the “substantially crystalline” sofosbuvir designation (without requiring the dependent XRPD peaks unless those dependent claims are asserted).

Fixed formulation “about” coverage (claim 10)

• Solid dispersion ~20%
• Sofosbuvir ~40%
• Microcrystalline cellulose ~35.5%
• Croscarmellose sodium ~3%
• Magnesium stearate ~1.5%

This is narrower than claim 1 and is likely directed to a specific commercial formulation.

Per-dose example scope (claim 14)

• Example-level mass totals (200 mg dispersion, 400 mg sofosbuvir, etc.)
• Still a “method of treating hepatitis C” claim, so infringement depends on the administered amount matching the example.

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What does the XRPD limitation do to enforceability and design-around options?

Executive summary: The XRPD peak requirements in dependent claims are strong, testable structural limitations that can be used both for infringement proof and for formulation design-around by selecting a different sofosbuvir solid form or modifying crystallinity characteristics.

Dependent XRPD claim sets

• Set A (two peaks): ~6.1° and 12.7° 2θ±0.2 (claims 2, 11, 17)
• Set B (four peaks): ~6.1°, 20.1°, 20.8°, plus 12.7° (claims 3, 12, 18)
  • Your text lists 6.1 and 20.1 and 20.8 explicitly in claim 3/12/18; claim 3/12/18 also include 12.7° from claim 1 base? The dependent claim text provided includes 6.1, 20.1, 20.8 (±0.2). Claim 2/11/17 clearly includes both 6.1 and 12.7.

Design-around levers suggested by the claim language

• Use a sofosbuvir solid state that does not show the claimed XRPD peak pattern within ±0.2.
• Use sofosbuvir that is not “substantially crystalline” (e.g., amorphous or different polymorph where the peaks shift or disappear).
• Avoid the specific crystalline sofosbuvir identity only matters if the asserted claims include the XRPD-dependent limitations.

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How does “about 12 weeks” affect the claim scope for real-world treatment protocols?

Executive summary: Duration is not the primary independent claim differentiator; it appears only in dependent claims. It can still matter in litigation because infringement of dependent claims depends on the claimed regimen timing.

• Claim 9, 13, 19: about 12 weeks

Practical implication: a regimen that uses the same composition but follows a materially different treatment duration could avoid dependent-claim infringement while still risking infringement of independent composition claims.

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What is the practical scope of the tablet and polyvinylalcohol-based film coating claims?

Executive summary: Claims 15 and 16 narrow protection to a coated tablet where the coating is polyvinyl alcohol-based. It targets dosage-form and manufacturing selections.

• Claim 15: film-coated tablet
• Claim 16: polyvinylalcohol-based coating

This limits the claim set that can attach to alternative dosage forms (e.g., different coating systems or non-tablet dosage forms).

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What does the patent landscape likely look like around this composition claim? (US-focused guidance from the claim scope)

Executive summary: Based on claim elements, the relevant US landscape is driven by:

• sofosbuvir solid-state patents/polymorph or crystallinity disclosures,
• copovidone/co-formulation solid dispersion patents involving “amorphous drug in polymer matrix,”
• excipient proportion and tablet formulation patents,
• and combination/regimen or use patents.

Given the claims explicitly cover a method of treating hepatitis C using a specific formulation that contains sofosbuvir, any landscape analysis for US risk typically clusters by: (i) sofosbuvir solid state, (ii) solid dispersion of Compound I in copovidone, and (iii) tablet formulation/excipients and coatings.

Landscape clustering by claim feature (use in diligence)

1. Sofosbuvir solid-state identity cluster

   • Polymorph/crystal form patents
   • XRPD-based characterization patents
   • Crystallinity-preserving formulation patents
   • If the XRPD peaks match known sofosbuvir solid forms, competitors may have alternative crystal forms or amorphous strategies.

2. Copovidone solid dispersion cluster

   • Solid dispersion compositions comprising drug dispersed in copovidone
   • Solid dispersion ratio claims, polymer-to-drug ratio constraints
   • Amorphous drug stabilization approaches

3. Tablet formulation / excipient cluster

   • Microcrystalline cellulose proportions
   • Croscarmellose sodium disintegrant proportion claims
   • Magnesium stearate lubricant proportion claims
   • Film coating and coating composition patents (polyvinyl alcohol-based coating)

4. Regimen timing cluster

   • “about 12 weeks” duration statements
   • Treatment regimen claims or clinical protocol disclosures (especially if linked to specific patient populations or genotype strategies, though not shown in your text)

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What are the likely strongest claim elements for validity and enforcement?

Executive summary: The most litigation-relevant limitations are the ones that are objective and testable: the amorphous status of Compound I, the internal 1:1 weight ratio in the copovidone solid dispersion, and the XRPD peak positions.

Validity leverage points

• Objective testability: XRPD peaks provide measurable infringement evidence for dependent claims.
• Specific composition architecture: internal 1:1 ratio in copovidone plus amorphous Compound I is narrower than generic “solid dispersion in polymer.”
• Combination of features: even if prior art exists for amorphous solid dispersions and separately for sofosbuvir crystals, the combination with defined excipients and XRPD may affect obviousness.

Infringement leverage points

• Laboratory testing can map an accused product to:
  • compound amorphous content and polymer matrix composition
  • internal weight ratio after isolation or compositional analysis
  • XRPD peak profile for crystalline sofosbuvir in the formulation

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Where are the clearest design-around pathways based on the claim wording?

Executive summary: The claim invites design-around by changing any of the objective formulation identity features that appear in the independent claims.

Primary design-around options suggested by the claims

1. Change the copovidone solid dispersion architecture

   • Do not use copovidone as the polymer matrix.
   • Avoid Compound I:copovidone weight ratio of ~1:1.
   • Use a solid dispersion where Compound I is not “substantially amorphous.”

2. Alter sofosbuvir solid-state form

   • If targeting avoidance of dependent XRPD claims, select a solid form that lacks the specified peaks within ±0.2.

3. Change excipient proportion bands

   • Shift microcrystalline cellulose, croscarmellose sodium, or magnesium stearate outside the claimed ranges (claim 1) or away from the fixed “about” values (claim 10).

4. Avoid dosage-form limitations

   • If avoiding claims 15–16, change the coating type or coating polymer system.

5. Avoid regimen duration

   • If staying on independent claims but avoiding dependent claims, treat for a different duration than “about 12 weeks.”

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How does the claim structure affect licensing and settlement posture?

Executive summary: Because the independent claims hinge on formulation identity and weight ranges, licensing is most likely to be negotiated on:

• formulation copying risk (solid dispersion with Compound I in copovidone at ~1:1 and amorphous),
• crystal form risk (XRPD-defined crystalline sofosbuvir),
• and manufacturing specifics (tablet coating system).

Settlement leverage generally increases when:

• an accused or generic candidate uses a similar tablet formulation and solid-state profile; and
• the alternative approach still needs sofosbuvir in crystalline form and similar excipient systems.

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Key Takeaways

• US Patent 10,086,011 protects a hepatitis C treatment method tied to a specific composition: amorphous “Compound I” solid dispersion in copovidone (Compound I:copovidone ~1:1) plus substantially crystalline sofosbuvir with defined composition bands and, in dependent claims, XRPD peak sets.
• Independent claims 1, 10, and 14 create a scope ladder: broad weight ranges (claim 1) to fixed “about” percentages (claim 10) to per-dose mass example (claim 14).
• The most enforceable limitations are objective: the amorphous status, the 1:1 solid dispersion ratio, and XRPD peak positions for crystalline sofosbuvir.
• Dependent claims add practical narrowing: about 12 weeks treatment duration and a polyvinylalcohol film coating tablet format.
• Design-around centers on changing any of the independent claim-defining formulation elements: polymer matrix/ratio/amorphous character, sofosbuvir solid state, or excipient proportions.

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FAQs

1. Can a generic avoid this patent by using a different tablet coating while keeping the same solid dispersion and excipient ranges?
   Changing coating can avoid claims 15–16 but not independent claims 1/10/14 if the core composition elements remain.

2. If an accused product uses the same weight ratios but sofosbuvir XRPD peaks shift slightly, does it avoid the dependent XRPD claims?
   It can, because the dependent claims require peak positions at 2θ with ±0.2 tolerance.

3. Does “substantially crystalline sofosbuvir” in the independent claims require matching XRPD peaks?
   Your provided text suggests XRPD peak limitations appear only in dependent claims; independent claims still require the “substantially crystalline” descriptor.

4. Is infringement determined at the manufacturing stage or only at the time of administration?
   The patent claims “a method … comprising administering,” so infringement is tied to the regimen where the administered composition meets the claimed formulation limitations.

5. How can competitors reduce risk against both claim 10 and claim 1?
   They must move outside the claimed formulation architecture: avoid the copovidone/Compound I 1:1 amorphous solid dispersion, adjust sofosbuvir crystallinity/solid state, and shift excipient proportions outside the defined ranges.

Drugs Protected by US Patent 10,086,011

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Gilead Sciences Inc	EPCLUSA	sofosbuvir; velpatasvir	TABLET;ORAL	208341-002	Mar 19, 2020		RX	Yes	No					Y
Gilead Sciences Inc	EPCLUSA	sofosbuvir; velpatasvir	TABLET;ORAL	208341-001	Jun 28, 2016		RX	Yes	Yes					Y

International Family Members for US Patent 10,086,011

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	095133
Australia	2014311827
Australia	2017276223
Australia	2019264624
Canada	2921160